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Simple and sensitive method for the quantification of total bilirubin in human serum using 3-methyl-2-benzothiazolinone hydrazone hydrochloride as a chromogenic probe.
We here describe a new spectrophotometric method for measuring total bilirubin in serum. The method is based on the cleavage of bilirubin giving formaldehyde which further reacts with diazotized 3-methyl-2-benzothiazolinone hydrazone hydrochloride giving blue colored solution with maximum absorbance at 630 nm. Sensitivity of the developed method was compared with Jendrassik-Grof assay procedure and its applicability has been tested with human serum samples. Good correlation was attained between both methods giving slope of 0.994, intercept 0.015, and R(2)=0.997. Beers law obeyed in the range of 0.068-17.2 ?M with good linearity, absorbance y=0.044 C(bil)+0.003. Relative standard deviation was 0.006872, within day precision ranged 0.3-1.2% and day-to-day precision ranged 1-6%. Recovery of the method varied from 97 to 102%. The proposed method has higher sensitivity with less interference. The obtained product was extracted and was spectrally characterized for structural confirmation with FT-IR, ąH NMR. PMID:20829101
Nagaraja, Padmarajaiah; Avinash, Krishnegowda; Shivakumar, Anantharaman; Dinesh, Rangappa; Shrestha, Ashwinee Kumar
Simple and sensitive method for the quantification of total bilirubin in human serum using 3-methyl-2-benzothiazolinone hydrazone hydrochloride as a chromogenic probe
NASA Astrophysics Data System (ADS)
We here describe a new spectrophotometric method for measuring total bilirubin in serum. The method is based on the cleavage of bilirubin giving formaldehyde which further reacts with diazotized 3-methyl-2-benzothiazolinone hydrazone hydrochloride giving blue colored solution with maximum absorbance at 630 nm. Sensitivity of the developed method was compared with Jendrassik-Grof assay procedure and its applicability has been tested with human serum samples. Good correlation was attained between both methods giving slope of 0.994, intercept 0.015, and R2 = 0.997. Beers law obeyed in the range of 0.068-17.2 ?M with good linearity, absorbance y = 0.044 Cbil + 0.003. Relative standard deviation was 0.006872, within day precision ranged 0.3-1.2% and day-to-day precision ranged 1-6%. Recovery of the method varied from 97 to 102%. The proposed method has higher sensitivity with less interference. The obtained product was extracted and was spectrally characterized for structural confirmation with FT-IR, 1H NMR.
High performance liquid chromatographic determination of methyl ethyl ketone in urine as its 3-methyl-2-benzothiazolinone hydrazone derivative
Microsoft Academic Search
Summary A HPLC method for the determination of methyl ethyl ketone (MEK) in urine after derivatization with 3-methyl-2-benzothiazolinone hydrazone is proposed. The calibration curve for the ketone was linear, ranging between 0.23–10 mg\\/L, with a detection limit of 0.025 mg\\/L. The results were compared to those obtained by GC-MS, coupled to the headspace technique. MEK derivatization and the derivative purification processes
G. Gori; P. Meneghetti; A. Sturaro; G. Parvoli; L. Doretti; G. B. Bartolucci
Spectrophotometric determination of nicoumalone, acebutolol hydrochloride and procainamide hydrochloride.
A sensitive spectrophotometric method is described for the determination of nicoumalone (NIC), acebutolol hydrochloride (ACBH) or procainamide hydrochloride (PAH) either in pure form or in pharmaceutical formulations. The method is based on the oxidative coupling reaction through the involvement of an aromatic primary amino group (released through reduction in NIC or hydrolysis in ACBH or existing free in PAH) in the drug with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of ferric chloride [Fe(III)]. The resulting chromophores are measured at 620 nm for NIC and ACBH and 580 nm for PAH. The concentration measurements are reproducible within a relative standard deviation of 1%. PMID:18965260
Sastry, C S; Rao, T T; Sailaja, A
Characterization of carbohydrates in mucilage samples from the northern Adriatic Sea.
Carbohydrate contents in seawater, mucilage, and mucilage interstitial waters were analyzed during episodes of mucilage formation in the summers of 2000 and 2001 in the northern Adriatic Sea off Pesaro and in the Gulf of Trieste using 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) and 2,4,6-tripyridyl-s-triazine (TPTZ) assays. The significant presence of polysaccharides in seawater in the presence of mucilage has an important impact on the agglomeration processes forming gelatinous material (macrogels). Characterization of oligosaccharides in the water-soluble fraction of mucilage using HPLC/RI revealed maltose and pentaose as the main components. PMID:12748753
Penna, Nunzio; Capellacci, Samuela; Ricci, Fabio; Kovac, Nives
Spectrophotometric Determination of Adefovir Dipivoxil in bulk and Pharmaceutical Formulation
Two selective and sensitive spectrophotometric methods have been developed for the estimation of adefovir dipivoxil in bulk and pharmaceutical preparations. Adefovir dipivoxil was subjected to acid hydrolysis and the hydrolysed product used for the estimation. The methods are based on the reaction with 3-methyl-2-benzothiazolinone hydrazone in the presence of ferric chloride, to form a colored species with absorption maxima at
An Optical Biosensor based on Immobilization of Laccase and MBTH in Stacked Films for the Detection of Catechol
The fabrication of an optical biosensor by using stacked films where 3-methyl- 2-benzothiazolinone hydrazone (MBTH) was immobilized in a hybrid nafion\\/sol-gel silicate film and laccase in a chitosan film for the detection of phenolic compounds was described. Quinone and\\/or phenoxy radical product from the enzymatic oxidation of phenolic compounds was allowed to couple with MBTH to form a colored azo-dye
Jaafar Abdullah; Musa Ahmad; Lee Yook Heng; Nadarajah Karuppiah; Hamidah Sidek
Stacked films immobilization of MBTH in nafion\\/sol-gel silicate and horseradish peroxidase in chitosan for the determination of phenolic compounds
The stacked-film immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion\\/sol-gel silicate film and\\u000a horseradish peroxidase (HRP) in chitosan, performed in order to allow the determination of phenolic compounds, was investigated\\u000a via an optical method. The stacked films were deposited onto a microscope glass slide by a spin-coating technique. The quinone\\u000a or free radical product formed by the enzymatic reactions of
A novel use of oxidative coupling reactions for determination of some statins (cholesterol-lowering drugs) in pharmaceutical formulations
New, accurate and reliable spectrophotometric methods for the assay of three statin drugs, atorvastatin calcium (AVS), fluvastatin sodium (FVS) and pravastatin sodium (PVS) in pure form and pharmaceutical formulations have been described. All methods involve the oxidative coupling reaction of AVS, FVS and PVS with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored products with ?max at 566, 615 and 664 nm, respectively. Beer's law was obeyed in the ranges of 2.0-20.0, 4.9-35.4 and 7.0-30.0 ?g mL -1 for AVS-MBTH, FVS-MBTH and PVS-MBTH, respectively. Molar absorptivities for the above three methods were found to be 3.24 × 10 4, 1.05 × 10 4 and 0.68 × 10 4 L mol -1 cm -1, respectively. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed methods have been applied to the determination of the components in commercial forms with no interference from the excipients. A comparative study between the suggested procedures and the official methods for these compounds in the commercial forms showed no significant difference between the two methods.
Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed
Glucosamine hydrochloride
... forms of glucosamine. Glucosamine hydrochloride is used for osteoarthritis, knee pain, back pain, and glaucoma. However, no ... effectiveness ratings for GLUCOSAMINE HYDROCHLORIDE are as follows:Osteoarthritis. There is conflicting evidence about the effectiveness of ...
Purification and Characterization of Cystathionine g-Lyase from Lactococcus lactissubsp.cremorisSK11: Possible Role in Flavor Compound Formation during Cheese Maturation
Chemicals. All enzyme substrates and inhibitors were obtained from Sigma Chemical Co. (St. Louis, Mo.); 5,59-dithiobis(2-nitrobenzoic acid) (DTNB), 3-methyl-2-benzothiazolinone hydrazone, pyridoxal-59-phosphate (PLP), 2,2-di- hydroxy-1,3-indanedione (nynhydrin), 2-(N-morpholino)ethanesulfonic acid (MES), 1,3-bis(tris(hydroxymethyl)methylamino)propane (bis-Tris-propane), and a-ketobutyrate were obtained from Sigma Chemical Co. The amino acid derivatization reagent kit, involving 6-aminoquinolyl-N-hydroxysuccinimidyl car- bamate (AQC), was obtained from Waters Associates (Milford, Mass.). Tris and EDTA were
Autoxidation of hydrazones. Some new insights.
Autoxidation of hydrazones is a generally occurring reaction, leading mostly to the formation of alpha-azohydroperoxides. All structural kinds of hydrazones, having at least one hydrogen atom on nitrogen, are prone to autoxidation; however, there are marked differences in the rate of the reaction. Hydrazones of aliphatic ketones are 1-2 orders of magnitude more reactive than analogous derivatives of aromatic ketones. Even less reactive are the hydrazones of chalcones, which function also as efficient inhibitors of autoxidation of other hydrazones. These differences can be attributed to the reduction of the rate of the addition of oxygen to a hydrazonyl radical, which is a reversible reaction. In the case of conjugated ketones, it becomes endothermic, making this elementary step slow down and the chain termination reactions become important. Substituents influence the stability of hydrazonyl radicals and, consequently, the bond dissociation energies of the N-H bonds. In acetophenone phenylhydrazones, the substituents placed on the ring of hydrazine moiety exhibit a higher effect (Hammett rho = -2.8) than those on the ketone moiety (rho = -0.82), which denotes higher importance of the structure with spin density concentrated on nitrogen in delocalized hydrazonyl radical. Electronic effects of the substituents also affect the transition state for the abstraction of hydrogen atom by electrophilic peroxy radicals; NBO analysis display a negative charge transfer of about 0.4 eu from hydrazone to a peroxy radical in the transition state. PMID:17696476
Harej, Maja; Dolenc, Darko
The mechanisms of the electrochemical reduction of azines of acetaldehyde, acetophenone, benzophenone, and fluorenone in DMFA were discussed. It was shown by the ESR method that the dianion of fluorenone gives an electron to the initial molecule in solution, with the formation of two radical particles.
Yu. P. Kitaev; V. Kh. Ivanova; A. Sh. Mukhtarov; L. N. Orlova; A. V. Ladygin
Duloxetine hydrochloride
In August 2004, duloxetine hydrochloride (Cymbalta; Eli Lilly), a selective serotonin- and noradrenaline-reuptake inhibitor, was approved by the US FDA for the treatment of major depressive disorder. It has since become the first such antidepressant to be approved by the FDA for an indication outside of psychiatry, when its approval for use in the treatment of diabetic peripheral neuropathic pain
Peter Kirkpatrick; Anathea B. Waitekus
Nicotinic acid hydrazones: a novel anticonvulsant pharmacophore
A series of aryl acid hydrazones of substituted aromatic acid hydrazides (D\\u000a 1 to D\\u000a 20) were synthesised and evaluated for anticonvulsant activity. Aryl acid hydrazones of Nicotinic acid hydrazide (D\\u000a 8, D\\u000a 9, and D\\u000a 10) have displayed excellent protection in maximal electroshock screen. These compounds have also exhibited excellent binding\\u000a properties with Lys 329 residue of gamma amino
Reema Sinha; U. V. Singh Sara; R. L. Khosa; James Stables; Jainendra Jain
Endogenous generation of hydralazine from labile hydralazine hydrazones.
The hypothesis that the pharmacologically active hydralazine hydrazones (HH) are endogenously hydrolyzed to parent hydralazine (H) was tested in a series of in vitro and in vivo systems. The stable hydrazones H alpha-ketoglutaric acid hydrazone and H pyruvic acid hydrazone did not hydrolyze to H in vitro (buffer or plasma), were inactive in vivo and did not generate urinary metabolites of parent H. By contrast, the labile HH, H acetaldehyde hydrazone and acetone hydrazone (HAH) generated H in vitro. H acetaldehyde hydrazone produced in vitro effects that were equipotent to the H concentration measured in the dose solutions. When administered to conscious rats and rabbits, the labile hydrazones reduced blood pressure. This effect was more gradual in onset than that of H. The hypotensive effects of HH were significantly greater than predicted by the amount of H contained in the dose solutions. Metabolic studies were conducted with the labile HH, HAH. After administration of HAH to rabbits, the proportional excretion of the urinary H metabolite, H pyruric acid hydrazone, was equal to that observed after the administration of H. We conclude that HH are inactive, except when hydrolyzed to H. The hydrolysis of certain HH, including HAH and H acetaldehyde hydrazone, in vivo may be nearly complete. Differences in the pharmacodynamic properties between labile HH and H may be related to the time course of generation of H, sequestration of hydrolysis in physiologically inactive sites or other unrecognized mechanisms. PMID:7086698
Clementi, W A; McNay, J L; Talseth, T; Haegele, K D; Ludden, T M; Musgrave, G E
Chelating agents as potential antitumorals: alpha-(N)-heterocyclic hydrazones and bis-alpha-(N)-heterocyclic hydrazones.
A number of pyruvic acid and methylpyruvate alpha-(N)-heterocyclic hydrazones has been synthesized. Bis-heterocyclic hydrazones were obtained from reaction with pyruvic carboxaldehyde. Some complexes of Ni(II) were prepared and characterized as neutral complexes. All these compounds have been evaluated for cytotoxicity against P388 and HL-60 leukemia. PMID:9507672
Savini, L; Massarelli, P; Chiasserini, L; Nencini, C; Pellerano, C
21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.
Code of Federal Regulations, 2010 CFR
...hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522...hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a...phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b)...
Characterization of monophenolase activity of polyphenol oxidase from iceberg lettuce.
Polyphenol oxidase (EC 188.8.131.52), a thylakoid membrane-bound enzyme, was isolated by sonication of osmotically shocked chloroplasts from iceberg lettuce (Lactuca sativa). The enzyme showed monophenolase activity when assayed on (p-hydroxyphenyl)propionic acid with 3-methyl-2-benzothiazolinone hydrazone in a reliable continuous spectrophotometric method, with high sensitivity, accuracy, and precision. The monophenolase activity showed a lag period before the steady-state rate (V(ss)) was reached. Both kinetic parameters, the lag period and the steady-state rate, depended on the pH, the enzyme and substrate concentrations, and the presence of catalytic amounts of o-diphenol. This activity shows inhibition by high substrate concentration. The experimental results correspond with the mechanism previously described for PPO from other sources. Kinetic constants K(m), V(max), and K(i) were determined. PMID:10563992
Chazarra, S; García-Carmona, F; Cabanes, J
Optical determination of L-tyrosine based on eggshell membrane immobilized tyrosinase.
An optical biosensor based on the eggshell membrane immobilized tyrosinase is described for the detection of L-tyrosine (L-Tyr). The detection scheme was based on the measurement of absorption value of color adduct resulting from the reaction of 3-methyl-2-benzothiazolinone hydrazone and dopa-quinone produced from the enzymatic oxidation of L-Tyr. The prepared biosensor demonstrated optimum activity at pH 7, optimum temperature range of 20-40 degrees C and a linear response for the L-Tyr concentration in range of 5-200 microM. It also showed good operation stability for repeated measurements (over 300 times) and storage stability after it had been kept at 4 degrees C for 3 months. PMID:21313820
Li, Yong Jin
A Comparison of Alkylhydrazines and Their B6-Hydrazones as Convulsant Agents.
National Technical Information Service (NTIS)
A comparative study was made of the toxicity and convulsion activity of 1,1-dimethylhydrazine (UDMH), monomethylhyrazine (MMH), and their pyridoxal and pyridoxal-5-phosphate hydrazones. The hydrazones of UDMH are more toxic than UDMH itself when 3 criteri...
A. Furst W. R. Gustavson
Synthesis, Characterization and Antimicrobial Activity of Long-Chain Hydrazones
Fatty acids containing hetero atoms are regarded as potential antimicrobial agents. Thus eight different hydrazones 2a-d and 3a-d were synthesized from four fatty acid hydrazides namely undecanoic hydrazide (1a), octadecanoic hydrazide (1b), 12-hydroxyoctadecanoic hydrazide (1c) and 9-hydroxyoctadecanoic hydrazide (1d) by condensing them with car- bonyl group of methyl acetoacetate and acetylacetone. The structural elucidation of these compounds is based on
Abdul Rauf; Mudasir R. Banday; Rayees H. Mattoo
Anticancer activity of new coumarin substituted hydrazide-hydrazone derivatives.
Drug resistance is a major impediment for cancer treatment, to overcome it we designed and synthesized sixteen coumarins bearing hydrazide-hydrazone moiety and evaluated them against human drug-resistant pancreatic carcinoma (Panc-1) cells and drug-sensitive (hepatic carcinoma; Hep-G2 and leukemia; CCRF) cell lines in vitro. The 6-brominated coumarin hydrazide-hydrazone derivatives (BCHHD) 7c, 8c and 10c were more potent than doxorubicin (DOX) against resistant Panc-1 cells. BCHHD 7c showed significant cytotoxicity against all tested cells (IC50: 3.60-6.50 ?M) on comparison with all other coumarin hydrazide-hydrazone derivatives (CHHD), whereas BCHHD's 8c and 10c showed significant antiproliferative activity only against resistant Panc-1 cells with IC50 of 2.02 ?M and 2.15 ?M, respectively. All the investigated BCHHD's were able to activate caspases 3/7 and they could induce apoptosis in resistant Panc-1 cells. Microarray analysis showed that BCHHD 7c induced the expression of apoptotic- and cell cycle arrest (G2/M)- genes in resistant Panc-1 cells. Moreover, BCHHD 7c induced the up-regulation of CDKN1A, DDIT4, GDF-15 and down-regulation of CDC2, CDC20, CDK2 genes. Based on our results, we conclude that 7c could be a potent anticancer drug to overcome drug resistance in cancer and it could be highly beneficial for patients in the clinic. PMID:24607878
Nasr, Tamer; Bondock, Samir; Youns, Mahmoud
Diaryl Hydrazones as Multifunctional Inhibitors of Amyloid Self-Assembly†
PubMed Central
The design and application of an effective, new class of multifunctional small molecule inhibitors of amyloid self-assembly are described. Several compounds, based on the diaryl hydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and were characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of A? fibrillogenesis and oligomer formation and the reverse processes, the disassembly of preformed fibrils and oligomers. Since the structure of the hydrazone-based inhibitors mimic the redox features of the antioxidant resveratrol the radical scavenging effect of the compounds was evaluated by colorimetric assays against 2,2-diphenyl-lpicrylhydrazyl (DPPH) and superoxide radicals. The hydrazone scaffold was active in all of the different assays. The structure-activity relationship revealed that the substituents on the aromatic rings had considerable effect on the overall activity of the compounds. The inhibitors showed strong activity in the fibrillogenesis inhibition and disassembly, and even greater potency in the inhibition of oligomer formation and oligomer disassembly. Supporting the quantitative fluorometric and colorimetric assays, size exclusion chromatographic studies indicated that the best compounds practically eliminated or substantially inhibited the formation of soluble, aggregated A? species, as well. Atomic Force Microscopy was also applied to monitor the morphology of A? deposits. The compounds also possessed the predicted antioxidant properties; approximately 30% of the synthesized compounds showed equal or better radical scavenging effect than resveratrol or ascorbic acid.
Torok, Bela; Sood, Abha; Bag, Seema; Tulsan, Rekha; Ghosh, Sanjukta; Borkin, Dmitry; Kennedy, Arleen R.; Melanson, Michelle; Madden, Richard; Zhou, Weihong; LeVine, Harry; Torok, Marianna
Fluorescence Quenchers for Hydrazone and Oxime Orthogonal Bioconjugation
We describe the synthesis and properties of new fluorescence quenchers containing aldehyde, hydrazine and aminooxy groups, allowing convenient bioconjugation as oximes or hydrazones. Conjugation to oligonucleotides proceeded in high yield with aniline as catalyst. Kinetics studies of conjugation show that, under optimal conditions, a hydrazine or aminooxy quencher can react with aldehyde-modified DNA to form a stable hydrazone or oxime adduct in as little as five minutes. The resulting quencher-containing DNAs were assessed for their ability to quench the emission of fluorescein in labeled complements and compared to the commercially available dabcyl and Black Hole Quencher 2 (BHQ2), which were conjugated as phosphoramidites. Results show that the new quenchers possess slightly different absorbance properties compared to dabcyl and are as efficient as the commercial quenchers in quenching fluorescein emission. Hydrazone-based quenchers were further successfully incorporated into molecular beacons and shown to give high signal:background in single nucleotide polymorphism detection in vitro . Finally, aminooxy and hydrazine quenchers were applied to quenching of an aldehyde-containing fluorophore associated with living cells, demonstrating cellular quenching within one hour.
Crisalli, Pete; Hernandez, Armando R.; Kool, Eric T.
Tissue Monoamine Oxidase Inhibitions by Convulsigenic Doses of Hydrazines and Related B6-Hydrazones.
Convulsigenic doses (0.42 to 1.68 mM./kg.) of the pyridoxal hydrazone of unsymmetrical dimethylhydrazine (UDMH) I.P. produced from 13% to 32% inhibition of rat brain monoamine oxidase (MAO). Administration of the hydrazones of monomethylhydrazine (MMH) an...
A. A. Wykes
Configurational and constitutional information storage: multiple dynamics in systems based on pyridyl and acyl hydrazones.
The C=N group of hydrazones can undergo E/Z isomerization both photochemically and thermally, allowing the generation of a closed process that can be tuned by either of these two physical stimuli. On the other hand, hydrazine-exchange reactions enable a constitutional change in a given hydrazone. The two classes of processes: 1) configurational (physically stimulated) and 2) constitutional (chemically stimulated) give access to short-term and long-term information storage, respectively. Such transformations are reported herein for two hydrazones (bis-pyridyl hydrazone and 2-pyridinecarboxaldehyde phenylhydrazone) that undergo a closed, chemically or physically driven process, and, in addition, can be locked or unlocked at will by metal-ion coordination or removal. These features also extend to acyl hydrazones derived from 2-pyridinecarboxaldehyde. Similarly to the terpydine-like hydrazones, such acyl hydrazones can undergo both constitutional and configurational changes, as well as metal-ion coordination. All these types of hydrazones represent dynamic systems capable of acting as multiple state molecular devices, in which the presence of coordination sites furthermore allows the metal ion-controlled locking and unlocking of the interconversion of the different states. PMID:21207621
Chaur, Manuel N; Collado, Daniel; Lehn, Jean-Marie
Interference in assays for hydralazine in humans by a major plasma metabolite, hydralazine pyruvic acid hydrazone.
The present study showed that published spectrophotometric and GLC methods for hydralazine in plasma do not distinguish between the drug and a major plasma metabolite, hydralazine pyruvic acid hydrazone. These methods involve the acid treatment of the sample, which hydrolyzes that hydrazone back to hydralazine. A specific GLC assay for the hydrazone was developed and involves its selective extraction from plasma and transformation to 3-trifluoromethyl-s-triazolo[3,4-a]phthalazine. This derivative could be sensitively measured by GLC using an electron-capture detector. With this procedure, it was shown that most "apparent hydralazine" in plasma is the hydrazone, which forms rapidly from hydralazine and endogenous pyruvic acid. Previous work indicated that the hydrazone was inactive when administered intravenously to rabbits. PMID:27629
Reece, P A; Stanley, P E; Zacest, R
Novel dehydrogenase catalyzes oxidative hydrolysis of carbon-nitrogen double bonds for hydrazone degradation.
Hydrazines and their derivatives are versatile artificial and natural compounds that are metabolized by elusive biological systems. Here we identified microorganisms that assimilate hydrazones and isolated the yeast, Candida palmioleophila MK883. When cultured with adipic acid bis(ethylidene hydrazide) as the sole source of carbon, C. palmioleophila MK883 degraded hydrazones and accumulated adipic acid dihydrazide. Cytosolic NAD+- or NADP+-dependent hydrazone dehydrogenase (Hdh) activity was detectable under these conditions. The production of Hdh was inducible by adipic acid bis(ethylidene hydrazide) and the hydrazone, varelic acid ethylidene hydrazide, under the control of carbon catabolite repression. Purified Hdh oxidized and hydrated the C=N double bond of acetaldehyde hydrazones by reducing NAD+ or NADP+ to produce relevant hydrazides and acetate, the latter of which the yeast assimilated. The deduced amino acid sequence revealed that Hdh belongs to the aldehyde dehydrogenase (Aldh) superfamily. Kinetic and mutagenesis studies showed that Hdh formed a ternary complex with the substrates and that conserved Cys is essential for the activity. The mechanism of Hdh is similar to that of Aldh, except that it catalyzed oxidative hydrolysis of hydrazones that requires adding a water molecule to the reaction catalyzed by conventional Aldh. Surprisingly, both Hdh and Aldh from baker's yeast (Ald4p) catalyzed the Hdh reaction as well as aldehyde oxidation. Our findings are unique in that we discovered a biological mechanism for hydrazone utilization and a novel function of proteins in the Aldh family that act on C=N compounds. PMID:18096698
Itoh, Hideomi; Suzuta, Tetsuya; Hoshino, Takayuki; Takaya, Naoki
Spectrophotometric determination of clobetasol propionate, halobetasol propionate, quinagolide hydrochloride, through charge transfer complexation.
Two spectrophotometric procedures are described for the determination of clobetasol propionate(I), halobetasol propionate(II) (corticosteroids) and quinagolide hydrochloride(III) (prolactin inhibitor). For corticosteroid drugs, the procedures are based on the formation of phenyl hydrazones of the corticosteroids which are subsequently subjected to charge transfer complexation reaction with either 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) as pi-acceptor or with iodine as sigma-acceptor. Prolactin inhibitor was reacted directly with the previous reagents. The molar ratios of the reactants were established and the experimental conditions were studied giving maximum absorption at 588 and 290 nm with DDQ and iodine methods, respectively for the three drugs. The concentration ranges were 20-150,50-300, and 20-80 microg ml(-1) in DDQ method for (I), (II), and (III), respectively and 13-20,15-40, and 8-32 microg ml(-1) in iodine method for (I), (II) and (III), respectively. PMID:11836053
Mostafa, Azza A; Bebawy, Lories I; Refaat, Heba H
Synthesis of Macrocyclic Bis-Hydrazone and Their Use in Metal Cations Extraction
Two new macrocyclic hydrazone Schiff bases were synthesized by reaction of succindihydrazide and adipdihydrazide with acetylacetone. Hydrazones have been characterized by elemental analyses and IR, mass, 1H?NMR, and 13C?NMR spectral data. Hydrazones have been studied by liquid-liquid extraction towards the s-metal ions (Li+, Na+, and K+) and d-metal ions (Cu2+ and Cr3+) from aqueous phase to organic phase. The effect of chloroform and dichloromethane as organic solvents over the metal chlorides extraction was investigated at 25 ± 0.1°C by using flame atomic absorption. We found differences between the two solvents in extraction selectivity.
Kandil, Farouk; Chebani, Mohamad Khaled; Al Zoubi, Wail
Pyridinyl hydrazone derivatives of thiacalix[4]arene as selective extractants of transition metal ions
The recognition ability of pyridinyl hydrazone derivatives of cone- and 1,3-alternate tetrathiacalix[4]arenes towards transition and alkali metals has been investigated by picrate extraction method. The stoichiometry\\u000a of complexes and the extraction constants have been determined. It has been found that hydrazones do not extract alkali metal\\u000a ions but show an excellent affinity towards transition and heavy metal cations. The removal
Sergey N. PodyachevNadezda; Nadezda E. Burmakina; Victor V. Syakaev; Svetlana N. Sudakova; Wolf D. Habicher; Alexander I. Konovalov
Preparation of dialdehyde cellulose hydrazone derivatives andevaluating their efficiency for sewage wastewater treatment
The cellulose hydrazone derivative is a novel product prepared from dialdehyde cellulose with 2-hydrazino-3,5,6,7tetrahydrocyclopentanethieno[2,3-d]-pyrimidin-4(4H)-one under suitably selected conditions. It was found that the reaction of dialdehyde cellulose with the 2-hydrazino derivative decreased progressively in the series cellulose powder, viscose wood pulp and cotton linter. The principal objective of this research was to evaluate the effectiveness of dialdehyde cellulose hydrazone derivatives
Magda G. El Meligy; Sh. El Rafie; Khadiga M. Abu-Zied
The antibacterial activity of some sulfonamides and sulfonyl hydrazones, and 2D-QSAR study of a series of sulfonyl hydrazones
Benzenesulfonicacid-1-methylhydrazide (1) and its four aromatic sulfonyl hydrazone derivatives (1a-1d), N-(3-amino-2-hydroxypropyl)benzene sulfonamide (2) and N-(2-hydroxyethyl)benzenesulfonamide (3) were synthesized and their structures were determined by IR, 1H NMR, 13C NMR, and LCMS techniques. Antibacterial activities of new synthesized compounds were evaluated against various bacteria strains by microdilution and disk diffusion methods. The experimental results show that presence of OH group on sulfonamides reduces the antimicrobial activity, and antimicrobial activities of the sulfonyl hydrazones (1a-1d) are smaller than that of the parent sulfonamide (1), except Candida albicans. In addition, 2D-QSAR analysis was performed on 28 aromatic sulfonyl hydrazones as antimicrobial agents against Escherichia coli and Staphylococcus aureus. In the QSAR models, the most important descriptor is total point-charge component of the molecular dipole for E. coli, and partial negative surface area (PNSA-1) for S. aureus.
Aslan, H. Güzin; Özcan, Servet; Karacan, Nurcan
Group X Aldehyde Dehydrogenases of Pseudomonas aeruginosa PAO1 Degrade Hydrazones
Hydrazones are natural and synthetic compounds containing a C=N-N moiety. Here we found that the opportunistic pathogen Pseudomonas aeruginosa PAO1 produced NAD+- or NADP+-dependent hydrazone dehydrogenase (HDH), which converts hydrazones to the corresponding hydrazides and acids rather than to the simple hydrolytic product aldehydes. Gene cloning indicated that the HDH is part of the group X aldehyde dehydrogenase (ALDH) family, which is distributed among bacteria, although the physiological roles of the ALDH family remain unknown. The PAO1 strain upregulated HDH in the presence of the hydrazone adipic acid bis(ethylidene hydrazide) (AEH). Gene disruption of the HDH-encoding hdhA (PA4022) decreased growth rates in culture medium containing AEH as the sole carbon source, and this effect was more obvious in the double gene disruption of hdhA and its orthologous exaC (PA1984), indicating that these genes are responsible for hydrazone utilization. Recombinant proteins of group X ALDHs from Escherichia coli, Paracoccus denitrificans, and Ochrobactrum anthropi also acted as HDHs in that they produced HDH activity in the cells and degraded hydrazones. These findings indicated the physiological roles of group X ALDHs in bacteria and showed that they comprise a distinct ALDH subfamily.
Taniyama, Kosuke; Itoh, Hideomi; Takuwa, Atsushi; Sasaki, Yasuyuki; Yajima, Shunsuke; Toyofuku, Masanori; Nomura, Nobuhiko
Group X aldehyde dehydrogenases of Pseudomonas aeruginosa PAO1 degrade hydrazones.
Hydrazones are natural and synthetic compounds containing a C=N-N moiety. Here we found that the opportunistic pathogen Pseudomonas aeruginosa PAO1 produced NAD(+)- or NADP(+)-dependent hydrazone dehydrogenase (HDH), which converts hydrazones to the corresponding hydrazides and acids rather than to the simple hydrolytic product aldehydes. Gene cloning indicated that the HDH is part of the group X aldehyde dehydrogenase (ALDH) family, which is distributed among bacteria, although the physiological roles of the ALDH family remain unknown. The PAO1 strain upregulated HDH in the presence of the hydrazone adipic acid bis(ethylidene hydrazide) (AEH). Gene disruption of the HDH-encoding hdhA (PA4022) decreased growth rates in culture medium containing AEH as the sole carbon source, and this effect was more obvious in the double gene disruption of hdhA and its orthologous exaC (PA1984), indicating that these genes are responsible for hydrazone utilization. Recombinant proteins of group X ALDHs from Escherichia coli, Paracoccus denitrificans, and Ochrobactrum anthropi also acted as HDHs in that they produced HDH activity in the cells and degraded hydrazones. These findings indicated the physiological roles of group X ALDHs in bacteria and showed that they comprise a distinct ALDH subfamily. PMID:22267508
Taniyama, Kosuke; Itoh, Hideomi; Takuwa, Atsushi; Sasaki, Yasuyuki; Yajima, Shunsuke; Toyofuku, Masanori; Nomura, Nobuhiko; Takaya, Naoki
Endotoxin-Binding Affinity of Sevelamer Hydrochloride
Background: Sevelamer hydrochloride has been shown to attenuate circulating biomarkers of inflammation in patients with chronic kidney failure. We hypothesize that sevelamer hydrochloride binds bacterial endotoxin (ET) resulting in a decrease in ET levels and cytokine production. Methods: To assess the ET-binding affinity of sevelamer hydrochloride, purified Escherichia coli ET was incubated with sevelamer hydrochloride (0–50 mg\\/ml). After incubation, ET
Mary C. Perianayagam; Bertrand L. Jaber
Simple hydrazone building blocks for complicated functional materials.
Conspectus The ability to selectively and effectively control various molecular processes via specific stimuli is a hallmark of the complexity of biological systems. The development of synthetic structures that can mimic such processes, even on the fundamental level, is one of the main goals of supramolecular chemistry. Having this in mind, there has been a foray of research in the past two decades aimed at developing molecular architectures, whose properties can be modulated using external inputs. In most cases, reversible conformational, configurational, or translational motions, as well as bond formation or cleavage reactions have been used in such modulations, which are usually initiated using inputs including, irradiation, metalation, or changes in pH. This research activity has led to the development of a diverse array of impressive adaptive systems that have been used in showcasing the potential of molecular switches and machines. That being said, there are still numerous obstacles to be tackled in the field, ranging from difficulties in getting molecular switches to communicate and work together to complications in integrating and interfacing them with surfaces and bulk materials. Addressing these challenges will necessitate the development of creative new approaches in the field, the improvement of the currently available materials, and the discovery of new molecular switches. This Account will describe how our quest to design new molecular switches has led us to the development of structurally simple systems that can be used for complicated functions. Our focus on the modular and tunable hydrazone functional group was instigated by the desire to simplify the structure and design of molecular switches in order to circumvent multistep synthesis. We hypothesized that by avoiding this synthetic bottleneck, which is one of the factors that hinder fast progress in the field, we can expedite the development and deployment of our adaptive materials. It should be noted though that designing structurally simple switches cannot be an end goal by itself! Therefore, we showed that our molecules can be used in applications that are beyond a simple molecular switching event (i.e., the control of the photophysical properties of liquid crystals and multistep switching cascades). While focusing on these switches, we discovered that the hydrazones can be easily transformed, using straightforward one-step reactions, into visible light activated azo switches, and two different families of fluorophores that can be used in sensing applications. These findings demonstrate that our approach of developing simple systems for sophisticated functions is not limited to the field of molecular switches and machines but can also encompass other adaptive materials. PMID:24766362
Tatum, Luke A; Su, Xin; Aprahamian, Ivan
Photostabilization of papaverine hydrochloride solutions.
Abstract: The stability of aqueous and non-aqueous papaverine hydrochloride solutions exposed to the UV radiation is poor. In order to enhance its photo-stability suitable light absorbers may be used. There werefour photo-protectors considered in this work: 4-aminobenzoic acid, sodium benzoate, methyl 4-hydroxybenzoate and propyl 4-hydroxybenzoate, whose UV absorption spectra characteristics match to some extent with the UV spectrum of papaverine. Approximately 20 mg/mL papaverine chloroform solutions with the above non-toxic additives in the concentrations 0.01; 0.05; 0.10% were exposed to the UV light of 254 nm. High performance capillary electrophoresis was used to determine the papaverine hydrochloride concentration loss as a function of time exposition to the light. It was found that papaverine hydrochloride photolysis proceeds according to the first-order kinetics. Methyl 4-hydroxybenzoate was found to be the best UV radiation-protective agent, and at the concentration 0.10%, the reaction rate constant decreases from 0.143 h(-1) to 0.028 h(-1). Both 4-hydroxybenzoate esters develop a more efficient UV radiation-protective activity than sodium benzoate, because the latter additive molar extinction coefficient is less significant. However, in spite of a high value of 4-aminobenzoic acid molar absorptivity coefficient, it is an unsuitable photo-protector for papaverine hydrochloride solutions, because its UV absorption spectrum does not match with that of papaverine. PMID:20635526
Piotrowska, Karolina; Hermann, Tadeusz W; Pawelska, Alicja
Quinazolin-4-yl-sulfanylacetyl-hydrazone derivatives; Synthesis, molecular structure and electronic properties
Four new acetylhydrazone derivatives of quinazoline have been synthesized and characterized. The molecular structures and relative stabilities of four possible isomers for each acetylhydrazone are calculated using DFT/B3LYP/6-31G(d,p) method. The calculations results predicted higher stability of the E-isomers compared to the Z-isomers in the gas phase. The syn-E isomer is the predominant form in gaseous phase for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti-E is the most stable isomer. The latter is stabilized by two strong intramolecular H-bonds instead of one in the others. The electronic and spectroscopic properties of the most stable isomers were also calculated using the same level of theory. The calculated atomic polar tensor (APT) charges indicated an increase of the positive charge density at the H-sites involved in the H-bonding interactions. The HOMO and LUMO energies are negative indicating that the compounds under investigation are stable. The electronic transition from the ground state to the excited state belongs to ?-?* transition. The calculated vibrational spectra showed strong red shifts and increase in the vibrational intensity of the Nsbnd H and Osbnd H stretching modes due to the intramolecular H-bonding interactions. In DMSO solution, the NMR spectra of the studied hydrazones revealed that such polar solvents stabilize the syn isomers for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti isomer is the major.
Hagar, Mohamed; Soliman, Saied M.; Ibid, Farahate; El Ashry, El Sayed H.
Synthesis and antibacterial activity against ralstonia solanacearum for novel hydrazone derivatives containing a pyridine moiety
Background Ralstonia solanacearum, one of the most important bacterial diseases on plants, is a devastating, soil-borne plant pathogen with a global distribution and an unusually wide host range. In order to discover new bioactive molecules and pesticides acting on tobacco bacterial wilt, we sought to combine the active structure of hydrazone and pyridine together to design and synthesize a series of novel hydrazone derivatives containing a pyridine moiety. Results A series of hydrazone derivatives containing a pyridine moiety were synthesized. Their structures were characterized by 1 H-NMR, 13 C-NMR, IR, and elemental analysis. The preliminary biological activity tests showed that compound 3e and 3g exhibited more than 80% activity against Ralstonia solanacearum at 500 mg/L, especially compound 3g displayed relatively good activity to reach 57.0% at 200 mg/L. Conclusion A practical synthetic route to hydrazone derivatives containing a pyridine moiety by the reaction of intermediates 2 with different aldehydes in ethanol at room temperature using 2-chloronicotinic acid and 2-amino-5-chloro-3-methylbenzoic acid as start materials is presented. This study suggests that the hydrazone derivatives containing a substituted pyridine ring could inhibit the growth of Ralstonia solanacearum.
Pharmacokinetics of hydralazine, apparent hydralazine and hydralazine pyruvic acid hydrazone in humans.
Hydralazine is an antihypertensive vasodilator agent. Lack of specific assay techniques for its measurement have delayed elucidation of its pharmacokinetic profile. This study compares the plasma profiles of hydralazine, measured both by a specific and by a previously published nonspecific assay and of a major plasma metabolite, hydralazine pyruvic acid hydrazone. After po and iv administration of hydralazine, peak hydralazine levels were lower (7-33%) and plasma half lives were shorter (15-31%) when measured by the specific technique. The mean plasma half life of the pyruvic acid hydrazone was 156 min and mean urinary clearance, 28 ml/min. The plasma profile of hydralazine and of the major metabolite, the pyruvic acid hydrazone, do not appear to correspond to the duration of antihypertensive effect of administered hydralazine. PMID:515498
Shepherd, A M; Ludden, T M; Haegele, K D; Talseth, T; McNay, J L
Antimicrobial studies of hydrazone complexes of Hg(II) and Fe(II) divalent metal ions.
The antibacterial, antifungal and antitubercular activities of Hg(II) and Fe(II) complexes of hydrazone were studied. All the complexes have been screened against Staphylococcus aureus, Salmonella typhi, Candida albicans, Aspergillus niger, Saccharomyces cerevisiae and Mycobacterium tuberculosis H37Rv and found to be more toxic than the parent ligand. The activity increased in the order [5-methyl-3-oximino-hexan-2-one-hydrazone]2 Fe(II) < [5-methyl-3-oximino-hexan-2-one-hydrazone]2 Hg(II) < 3-oximino-hexan-2-one-phenylhydrazone]2 Fe(II) < [5-methyl-3-oximino-hexan-2-one-phenylhydrazone]2 Hg(II) for antibacterial and antifungal activity. PMID:14556484
Donde, K J; Patil, V R; Malve, S P
Synthesis, spectral studies and structure of 2-hydroxyacetophenone nicotinic acid hydrazone
2-Hydroxyacetophenone nicotinic acid hydrazone (H 2ApNH) was synthesized as a part of our work, in search for non-linear optical crystal based on hydrazones, and studied spectroscopically. Complete NMR assignments for the hydrazone was made using COSY homonuclear and HMQC heteronuclear correlation techniques. Solid state reflectance was also studied in order to understand the electronic structure of the synthesized compound. The crystal and molecular structures of H 2ApNH were determined. The compound crystallizes into an orthorhombic lattice with a non-centrosymmetric space group Pca2 1 with two crystallographically unique molecules of in an asymmetric unit. The geometry reveals quasi co planarity in the whole molecular skeleton with localization of the double bonds in the C?N-N-C?O with an E-configuration.
Sreeja, P. B.; Sreekanth, A.; Nayar, Chandini R.; Prathapachandra Kurup, M. R.; Usman, A.; Razak, I. A.; Chantrapromma, S.; Fun, H. K.
Dioxouranium(VI) complexes of aliphatic (mono- and di-) hydrazone-oximes
Summary Uranyl acetate dihydrate reacts with several hydrazone-oximes, derived from aliphatic (mon-annd di-) hydrazides and 2,3-butanedione monoxime in the absence of NaOAc, to form complexes of general formulae [UO2(HL)2] and [UO2(HL)2SZ] (where H2L=aliphatic acid monohydrazone-oximes; S=EtOH and Z=H2O). With aliphatic acid dihydrazone and monomaleoyl-hydrazone-oximes, different complexes have been synthesized in 50% EtOH and in the absence of NaOAc. The products
Aďcha Yacouta-Nour; Abobaker K. T. Maki; Monsen M. Mostafa; Kamal M. Ibrahim; Ashraf A. El-Bindary
Synthesis, characterization and anti-tubercular activity of ferrocenyl hydrazones and their ?-cyclodextrin conjugates.
A series of ferrocenyl hydrazones and their ?-cyclodextrin (CD) inclusion complexes were prepared and evaluated for antitubercular activity under low and high iron conditions. The inclusion complexes were characterized by Fourier Transform Infrared (FTIR), Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), (1)H NMR, Scanning Electron Microscopy (SEM) and Cyclic Voltammetric (CV) studies. The inclusion complexes exhibited improved aqueous solubility as well as enhanced hydrolytic and thermal stability. They were also found to exhibit greater antitubercular activity than the parent ferrocenyl hydrazones against Mycobacterium tuberculosis under high iron conditions. When grown under low iron conditions these compounds exhibited lower activity suggesting requirement of iron-dependant peroxidase activation. PMID:24751257
Dandawate, Prasad; Vemuri, Kiranmayi; Khan, Ejazuddin M; Sritharan, Manjula; Padhye, Subhash
Asymmetric Synthesis of 2-Substituted Oxetan-3-ones via Metalated SAMP/RAMP Hydrazones
2-Substituted oxetan-3-ones can be prepared in good yields and enantioselectivities (up to 84% ee) by the metalation of the SAMP/RAMP hydrazones of oxetan-3-one, followed by reaction with a range of electrophiles that include alkyl, allyl, and benzyl halides. Additionally, both chiral 2,2- and 2,4-disubstituted oxetan-3-ones can be made in high ee (86–90%) by repetition of this lithiation/alkylation sequence under appropriately controlled conditions. Hydrolysis of the resultant hydrazones with aqueous oxalic acid provides the 2-substituted oxetan-3-ones without detectable racemization.
Lanthanide Complexes of Substituted ?-Diketone Hydrazone Derivatives: Synthesis, Characterization, and Biological Activities
A series of ?-diketone hydrazone derivatives have been synthesized through condensation of ?-diketone with aromatic aldehydes followed by reaction with phenylhydrazine. The structure of the ligands and intermediates are well defined through elemental and spectroscopic analyses. These hydrazones are potential ligands toward lanthanide metal ions. New complexes of trivalent Scandium, Yttrium, Lanthanum, and Cerium have been synthesized. The composition of these complexes is discussed on the basis of elemental analyses, IR, magnetic moments, and thermal analyses. The prepared complexes were screened for antibacterial and antifungal properties and have exhibited potential activity.
Hegazy, W. H.; Al-Motawaa, I. H.
21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.
...2010-04-01 2010-04-01 false Levamisole hydrochloride effervescent tablets...FORM NEW ANIMAL DRUGS § 520.1242e Levamisole hydrochloride effervescent tablets...Each tablet contains 907 milligrams of levamisole hydrochloride. (b) Sponsor....
Betahistine hydrochloride in Méniére's disease
A double-blind, placebo-controlled, cross-over clinical trial was performed to assess the effect of betahistine hydrochloride (Serc) in Méničre's disease. The diagnosis was based on paroxysmal attacks of rotational vertigo, with tinnitus, and a fluctuating sensori-neural deafness, together with the results of auditory and vestigular tests. Twenty-eight patients were admitted to the trial over 3 years. Twenty-two patients completed the trial.
I. J. Frew; G. N. Menon
Influence of structural factors on the magnetic properties of the binuclear copper complexes with salicylaldehyde hydrazone and bis(hydrazone)-2,6-diformylphenol: Quantum-chemical calculations
The structures and magnetic properties of the binuclear copper complexes of salicylaldehyde mono- and bis(hydrazone) derivatives\\u000a were studied by the quantum-chemical density functional theory (B3LYP\\/6-311++g(d,p)) using the broken-symmetry technique. The change in the degree of deprotonation of the ligands was found to exert an insignificant\\u000a effect on the magnetic properties, whereas the coordination of solvent molecules substantially weakened the antiferromagnetic
A. G. Starikov; V. A. Kogan; V. V. Lukov; V. I. Minkin; R. M. Minyaev
Studies on the synthesis and crystal structure of a magnesium complex with pyruvic acid isonicotinoyl hydrazone
A magnesium complex with pyruvic acid isonicotinoyl hydrazone (H2L), having the general formula [MgL(H2O)31 · H2O, has been synthesized and its crystal structure determined by X-ray diffraction analyses. The structural parameters and typical IR spectra bands for H2L complexes with Mg and other metals are discussed.
Kaibei Yu
Synthesis and crystal structure of a barium complex with pyruvic acid isonicotinoyl hydrazone
A barium complex with pyruvic acid isonicotinoyl hydrazone (H2L) has been synthesized and its crystal structure was determined by X-ray diffraction analyses. There is one complex unit, Ba(HL)2(H2O), with eight lattice water molecules in the asymmetric unit. The nine-coordinated barium has a distorted, monocapped square antiprism configuration.
Conformational analysis of 2 -diphenylacetyl- 1,3 - indandione- 1 -hydrazone and its derivatives
Conformational analysis in solution of 2-diphenylacetyl-1,3-indandione-1-hydrazone (DI- PAIN, 1) and its derivatives was achieved by NMR, FT-IR and fluorescence spectroscopy. The spectral evidence indicates that the enamine tautomer is the only isomeric form adopted in solution.
Partridge, Ashton C.; Charlesworth, John M.
EPA Science Inventory
An environmentally benign aqueous protocol for the synthesis of cyclic, bi-cyclic, and heterocyclic hydrazones using polystyrene sulfonic acid (PSSA) as a catalyst has been developed; the simple reaction proceeds efficiently in water in the absence of any organic solvent under mi...
Synthesis and antifungal activity of novel pyrazolecarboxamide derivatives containing a hydrazone moiety
Background The plant pathogenic fungus (such as Gibberella zeae, Fusarium oxysporum and Cytospora mandshurica) causes devastating disease in agriculture. The pathogenic fungus is responsible for billions of dollars in economic losses worldwide each year. In order to discover new fungicidal molecule with good fungicidal activity against G. zeae, F. oxysporum, and C. mandshurica, we sought to combine the active sub-structure of hydrazone and pyrazole amide derivatives together to design and synthesize novel pyrazole amide derivatives containing a hydrazone moiety. Results A series of novel pyrazole amide derivatives bearing hydrazone moiety were synthesized. Their structures were characterized by 1?H-NMR, 13?C-NMR, IR, and elemental analysis. The preliminary biological assays revealed that most of the synthesized compounds exhibit favorable antifungal activities against G. zeae. The activity of compounds 7a, 7f, 7g, 7h, 7i, 7j, 7l and 7q were 40.82%, 47.78%, 50.32%, 40.82%, 49.05%, 48.73%, 40.19% and 45.89%, respectively, and the synthesized compounds showed certain antifungal activities against F. oxysporum and C.mandshurica. Conclusion A practical synthetic route to pyrazole amide derivatives containing a hydrazone moiety were synthesized by the condensation of intermediates 5-chloro-N-(4-subsititued-2-(hydrazinecarbonyl)-6-methylphenyl)-1,3-dimethyl-1?H-pyrazole-4-carboxamide with different aldehydes or ketones in ethanol at room temperature is presented, the results of the study suggested that the pyrazole amide derivatives containing hydrazone moieties could inhibit the growth of G. zeae, F. oxysporium and C. mandshurica to a certain extent.
Potentially cytotoxic new copper(II) hydrazone complexes: synthesis, crystal structure and biological properties.
A new set of penta-coordinated copper(II) hydrazone complexes containing solvated methanol were synthesized by reacting the hydrazone ligands, 2-acetylpyridine benzoyl hydrazone (HL1) and 2-acetylpyridine thiophene-2-carboxylic acid hydrazone (HL2), with [CuCl2(DMSO)2] and characterized by different spectral methods. Single crystal X-ray diffraction studies of the complexes revealed that both of them, [CuCl(L1)(MeOH)] (1) and [CuCl(L2)(MeOH)] (2), have square pyramidal geometry around the cupric ion, in which the hydrazone is coordinated through NNO atoms along with a molecule of methanol in the apical position. Interaction of the ligands HL1 and HL2 along with the corresponding copper complexes 1 and 2 with calf thymus DNA (CT-DNA) has been estimated by absorption and emission titration methods which revealed that the compounds interacted with CT-DNA through intercalation. Binding of the compounds, i.e., free ligands and complexes (1) and (2) with bovine serum albumin (BSA) protein investigated using UV-visible, fluorescence and synchronous fluorescence spectroscopic methods indicated that there occurred strong binding of copper complexes to BSA over the ligands. Further, the cytotoxicity of the compounds examined in vitro on a panel of cancerous cell lines such as a human cervical cancer cell line (HeLa), a pancreatic cancer cell line (PANC-1), an Ehrlich ascites cancer cell line (EAC) and Dalton's lymphoma ascitic cancer cells (DLA) and a normal mouse embryonic fibroblasts cell line (NIH3) demonstrated that the complexes 1 and 2 possessed superior cytotoxicity than that of well-known commercial anticancer drug cisplatin to the tumor cells but are less toxic to the normal cell line and have emerged as potential candidates for further studies. PMID:23529726
Alagesan, Mani; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy
Preparation of magnetite/poly(styrene-divinylbenzene) nanoparticles for selective enrichment-determination of fenitrothion in environmental and biological samples.
In the present study, a cross-linked nano-sized spherical magnetic poly(styrene-divinylbenzene) is synthesized and used as an adsorbent for enrichment-determination of fenitrothion. A miniemulsion polymerization procedure was used to prepare the adsorbent. The magnetic adsorbent was characterized by FT-IR, SEM and TEM. The prepared magnetic adsorbent nanoparticles were mixed with magnetite nanoparticles for faster and more efficient magnetic precipitation. The reduced fenitrothion was coupled with 3-methyl-2-benzothiazolinone hydrazone and then the blue colored complex was extracted. The blue derivative of fenitrothion was eluted by a 1 mL aliquot of 1-propanol prior to spectrophotometry at 571 nm. Beer's law was obeyed in the range of 2-230 ng mL(-1) of fenitrothion with relative standard deviation and recovery in the ranges of 0.9-5.1% and 97.2-100.0%, respectively. Selectivity of the method was evaluated, and the method was successfully applied to the determination of fenitrothion in various water, soil, urine and human plasma samples. PMID:22882834
Eskandari, Habibollah; Naderi-Darehshori, Ali
Spectrophotometric methods for the determination of nifurtimox in bulk form and pharmaceutical formulations.
Three simple and sensitive methods for the assay of Nifurtimox (NIF) which is an active antitrypanocide were developed. These methods are based on the formation of coloured species by treating either its reduction product with 3-methyl-2-benzothiazolinone hydrazone (MBTH) in the presence of ferric chloride (method A) or its hydrolysis product with 2-thiobarbituric acid (TBA) (method B) or by oxidizing it with excess N-bromosuccinamide (NBS) and determining the consumed NBS using p-N-methylaminophenol sulphate (metol)-isonicotinic acid hydrazide (INH) (method C). All variables have been optimized and the reaction mechanisms presented. Regression analysis of Beer's plot showed good correlation in the concentration range of 2.5-10, 2.5-30 and 1.25-7.5 microg/ml for methods A, B and C, respectively. No interference was observed from the additives and the validity of the methods was tested by analysing the tablets. Recoveries were 99.2-100.9%. PMID:18966156
Sastry, C S; Rao, K R; Krishna, D M; Sastry, B S; Prasad, D S
Spectrophotometric methods for the determination of omeprazole in bulk form and pharmaceutical formulations.
Four simple and sensitive methods for the assay of omeprazole (OMZ) were developed. These methods are based on the formation of colored species by treating OMZ with 3-methyl-2-benzothiazolinone hydrazone (MBTH) following oxidation with ferric chloride (method A) or m-aminophenol following oxidation with chloramine-T (CAT) (method B) or Folin-Ciocalteau reagent (FC) (method D), or by oxidizing OMZ with excess N-bromosuccinimide (NBS) and determining the consumed NBS with a decrease in color intensity of Celestine blue (CB) (method C). All variables have been optimized. Regression analysis of Beer's plots showed good correlation in the concentration range of 1.0-10, 2.0-32, 0.4-2.4 and 0.8-10 mug ml(-1) for methods A, B, C and D, respectively. No interference was observed for formulation additives and the validity of each method was tested by analysing capsules containing OMZ. Recoveries were 98.7-100.1%. PMID:18966856
Sastry, C S; Naidu, P Y; Murty, S S
Synthesis, characterization and crystal structures of the organotin(IV) compounds with the Schiff base ligands of pyruvic acid thiophene-2-carboxylic hydrazone and salicylaldehyde thiophene-2-carboxylic hydrazone
A series of organotin (IV) compounds of the type [R3SnL]2, R is Me (1), Bu (2), [R2SnL]2, R is Ph (3), Me (4), Bu (5), L is pyruvic acid thiophene-2-carboxylic hydrazone, and R2SnL, R is Me (6), Bu (7), Ph (8), L is salicylaldehyde thiophene-2-carboxylic hydrazone have been synthesized in 1:1 molar ratio. All compounds were characterized by elemental analysis,
Han Dong Yin; Shao Wen Chen; Lin Wei Li; Da Qi Wang
Thermoanalytical Investigation of Terazosin Hydrochloride
Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (?H*), entropy (?S*) and Gibbs free energy change of the decomposition (?G*) were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97%) and specialized official method (99.85%) indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 şC), water content (7.49%) and ash content (zero) in comparison to what were obtained using official method: (272 şC), (8.0%) and (0.02%) for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.
Attia, Ali Kamal; Mohamed Abdel-Moety, Mona
Yohimbine hydrochloride as an antagonist to xylazine hydrochloride-ketamine hydrochloride immobilization of white-tailed deer
USGS Publications Warehouse
Thirteen captive and one free-ranging white-tailed deer (Odocoileus virginianus) were immobilized one to six times each with ketamine hydrochloride and xylazine hydrochloride during winter and spring in northern Minnesota. Administration of 0.09 to 0.53 mg of yohimbine hydrochloride per kg IV after each trial reversed the immobilization. The deer raised their heads within a median time of 2.0 min, stood in 6.0 min and walked away in 9.5 min. No adverse side effects were observed for several weeks following the immobilization.
Mech, L.D.; DelGiudice, G.D.; Karns, P.D.; Seal, U.S.
Identification of hydrallazine and hydrallazine hydrazone metabolites in human body fluids and quantitative in vitro comparisons of their smooth muscle relaxant activity.
1 Serum and urine from hypertensive subjects on chronic oral hydrallazine therapy were studied using gas chromatographic/mass spectrometry techniques. 2 Metabolites resulting from acetylation, hydrolysis and conjugation reactions were detected. The acetone, pyruvate and alpha-ketoglutarate hydrazone were identified. 3 The activity of the pyruvate and alpha-ketoglutarate hydrazones were compared with that of hydrallazine using isolated rabbit aortic strips. 4 Both hydrazones were active under in vitro conditions, producing smooth muscle relaxant effects equal to those of hydrallazine. 5 It is concluded that hydrazone metabolites will contribute to the hypotensive effects of hydrallazine therapy in proportion to their relative abundance, persistence in vascular tissues and intrinsic activity.
Haegele, K D; McLean, A J; du Souich, P; Barron, K; Laquer, J; McNay, J L; Carrier, O
Structure-activity relationships of pyrrole hydrazones as new anti-tuberculosis agents.
Preliminary investigations of our research team have shown that some pyrrole hydrazones posses strong inhibitory activity against the tuberculosis bacilli, and thus represent a new perspective for development of anti-tuberculosis agents. In this work the anti-tuberculosis activity of an in-house series of pyrrole hydrazones was investigated by quantitative structure-activity relationships (QSAR) analysis and by pharmacophore modelling. Different constitutional, topological, physicochemical, and quantum-mechanical descriptors of the chemical structure were calculated. The QSAR models included the number of chlorine, fluorine and nitrogen atoms, molecular flexibility and shape indexes, and magnitudes of charged molecular surfaces areas and hydrophobic volumes, suggesting importance of these structural characteristics for the activity. Next, a pharmacophore analysis was applied. A possible pharmacophore responsible for the compound interactions with their biological target in the 3D space consisted of five features, including hydrophobic centres, a potential H-bond acceptor and a potential metal ligator. PMID:22530903
Lessigiarska, Iglika; Pajeva, Ilza; Prodanova, Penka; Georgieva, Maya; Bijev, Atanas
Spectroscopic and theoretical study of the o-vanillin hydrazone of the mycobactericidal drug isoniazid
A complete and detailed study of the hydrazone obtained from condensation of antituberculous isoniazid (hydrazide of the isonicotinic acid, INH) and o-vanillin (2-hydroxy-3-methoxybenzaldehyde, o-HVa) is performed. It includes structural and spectroscopic analyses, comparing experimental and theoretical results. The compound was obtained as a chloride of the pyridinic salt (INHOVA +Cl -) but it will be referred as INHOVA for the sake of simplicity. The conformational space was searched and optimized geometries were determined both in gas phase and including solvent effects. Vibrational (IR and Raman), electronic and NMR spectra were registered and assigned with the help of computational methods based on the Density Functional Theory. Isoniazid hydrazones are good candidates for therapeutic agents against tuberculosis with conserved efficiency and lower toxicity and resistance than parent INH.
González-Baró, Ana C.; Pis-Diez, Reinaldo; Parajón-Costa, Beatriz S.; Rey, Nicolás A.
Hydrazone Self-Crosslinking of Multiphase Elastin-Like Block Copolymer Networks
Biosynthetic strategies for the production of recombinant elastin-like protein (ELP) triblock copolymers have resulted in elastomeric protein hydrogels, formed through rapid physical crosslinking upon warming of concentrated solutions. However, the strength of physically crosslinked networks can be limited, and options for non-toxic chemical crosslinking of these networks are not optimal. In this report, we modify two recombinant elastin-like proteins with aldehyde and hydrazide functionalities. When combined, these modified recombinant proteins self-crosslink through hydrazone bonding without requiring initiators or producing by-products. Crosslinked materials are evaluated for water content and swelling upon hydration, and subject to tensile and compressive mechanical tests. Hydrazone crosslinking is a viable method for increasing the mechanical strength of elastin-like protein polymers, in a manner that is likely to lend itself to the biocompatible in situ formation of chemically and physically crosslinked ELP hydrogels.
Krishna, Urlam Murali; Martinez, Adam W.; Caves, Jeffrey M.; Chaikof, Elliot L.
Synthesis, characterization, molecular docking and cytotoxic activity of novel plumbagin hydrazones against breast cancer cells.
Novel plumbagin hydrazonates were prepared, structurally characterized and evaluated for anti-proliferative activity against estrogen receptor-positive MCF-7 and triple negative MDA-MB-231 and MDA-MB-468 breast cancer cell lines which exhibited superior inhibitory activity than parent plumbagin compound. Molecular docking studies indicated that hydroxyl groups on plumbagin and hydrazonate side chain favor additional hydrogen bonding interactions with amino acid residues in p50-subunit of NF-?B protein and these compounds inhibited NF-?B expression which may be responsible for the enhanced anti-proliferative activity. These compounds were found to be more effective against triple negative breast cancer cells and might serve as a starting point for building future strategies against triple negative breast cancers which are known for their increased drug resistance and poor prognosis of breast cancer patients. PMID:22483392
Dandawate, Prasad; Khan, Ejazuddin; Padhye, Subhash; Gaba, Himanshi; Sinha, Swati; Deshpande, Jyoti; Venkateswara Swamy, K; Khetmalas, Madhukar; Ahmad, Aamir; Sarkar, Fazlul H
Anion induced azo-hydrazone tautomerism for the selective colorimetric sensing of fluoride ion
The design, synthesis, characterization and their anion sensing properties of two receptors capable of exhibiting azo-hydrazone tautomerism are reported. The anion sensing properties have been investigated using electronic, fluorescence and nuclear magnetic spectral studies in addition to electrochemical and visual detection experiments. Both the receptors selectively bind fluoride ion with >100 nm red-shift in the electronic spectrum and the color changes from yellow to red. The results of the spectral studies revealed that the sensing mechanism involves fluoride ion induced change of chromophore from Cdbnd N (hydrazone form) to Ndbnd N (azo form) in these receptors leading to the visible color change. Density Functional Theory calculations were conducted to rationalize the optical response of the receptors.
Satheshkumar, A.; El-Mossalamy, E. H.; Manivannan, R.; Parthiban, C.; Al-Harbi, L. M.; Kosa, S.; Elango, Kuppanagounder P.
Anion induced azo-hydrazone tautomerism for the selective colorimetric sensing of fluoride ion.
The design, synthesis, characterization and their anion sensing properties of two receptors capable of exhibiting azo-hydrazone tautomerism are reported. The anion sensing properties have been investigated using electronic, fluorescence and nuclear magnetic spectral studies in addition to electrochemical and visual detection experiments. Both the receptors selectively bind fluoride ion with>100nm red-shift in the electronic spectrum and the color changes from yellow to red. The results of the spectral studies revealed that the sensing mechanism involves fluoride ion induced change of chromophore from CN (hydrazone form) to NN (azo form) in these receptors leading to the visible color change. Density Functional Theory calculations were conducted to rationalize the optical response of the receptors. PMID:24704596
Satheshkumar, A; El-Mossalamy, E H; Manivannan, R; Parthiban, C; Al-Harbi, L M; Kosa, S; Elango, Kuppanagounder P
21 CFR 520.2002 - Propiopromazine hydrochloride.
Code of Federal Regulations, 2013 CFR
...potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the order of a licensed veterinarian. [40 FR 13838, Mar. 27, 1975, as amended...
21 CFR 520.1962 - Promazine hydrochloride.
...FORM NEW ANIMAL DRUGS § 520.1962 Promazine hydrochloride. (a)(1) Chemical name. 10-[3-(Dimethylamino)propyl]phenothiazine monohydrochloride. (2) Specifications. Conforms to N.F. XII. (3) Sponsor. See No....
PEGylated polyamidoamine dendrimers with bis-aryl hydrazone linkages for enhanced gene delivery.
Surface modification of polyamidoamine (PAMAM) dendrimers with polyethylene glycol (PEG) often results in the decrease in their buffering capacity, which is essential for gene transfer. In this work, bis-aryl hydrazone bond, which possesses protonatable pyridine and amines, was explored as a new linkage for PEGylation of PAMAM dendrimers. PEGylated polyamidoamine (PAMAM) dendrimer G4.0 conjugates with bis-aryl hydrazone (BAH) linkages were synthesized following a two-step procedure: activation of PAMAM dendrimer G4.0 and monofunctional methoxypolyethylene glycol amine (MW=5000 Da) with succinimidyl 4-hydrazinonicotinate acetone hydrazone (SANH) and succinimidyl 4-formylbenzoate (SFB), respectively, and coupling of SFB-activated PEG to SANH-activated G4.0 to generate PEGylated G4.0 with bis-aryl hydrazone linkages (G4.0-BAH-PEG). It was found that the incorporation of BAH linkages into the vector significantly enhanced the buffering capacity of the vector even with a high degree of PEGylation (42 PEG chains per dendrimer). G4.0-BAH-PEG conjugates could complex with DNA plasmid tightly at low weight ratios and display dramatically improved cytocompatibility. According to gene transfection studies in 293T and HN12 cells, this new vector has been shown to be capable of both transfecting more cells and inducing higher gene expression than the parent dendrimer. This work demonstrates that the use of the BAH linkage in coupling of PEG to the dendrimer helps maintain or increase the buffering capacity of the functionalized dendrimer and results in enhanced transfection. PMID:20593893
Yuan, Quan; Yeudall, W Andrew; Yang, Hu
The iron chelator pyridoxal isonicotinoyl hydrazone inhibits mitochondrial lipid peroxidation induced by Fe(II)–citrate
Pyridoxal isonicotinoyl hydrazone (PIH) is able to prevent iron-mediated hydroxyl radical formation by means of iron chelation and inhibition of redox cycling of the metal. In this study, we investigated the effect of PIH on Fe(II)–citrate-mediated lipid peroxidation and damage to isolated rat liver mitochondria. Lipid peroxidation was quantified by the production of thiobarbituric acid-reactive substances (TBARS) and by antimycin
Natacha C. F Santos; Roger F Castilho; André R Meinicke; Marcelo Hermes-Lima
Hydrazone ligation strategy to assemble multifunctional viral nanoparticles for cell imaging and tumor targeting.
Multivalent nanoparticle platforms are attractive for biomedical applications because of their improved target specificity, sensitivity, and solubility. However, their controlled assembly remains a considerable challenge. An efficient hydrazone ligation chemistry was applied to the assembly of Cowpea mosaic virus (CPMV) nanoparticles with individually tunable levels of a VEGFR-1 ligand and a fluorescent PEGylated peptide. The nanoparticles recognized VEGFR-1 on endothelial cell lines and VEGFR1-expressing tumor xenografts in mice, validating targeted CPMV as a nanoparticle platform in vivo. PMID:20163184
Brunel, Florence M; Lewis, John D; Destito, Giuseppe; Steinmetz, Nicole F; Manchester, Marianne; Stuhlmann, Heidi; Dawson, Philip E
Quantitative analysis of hydralazine pyruvic acid hydrazone, the major plasma metabolite of hydralazine.
A specific, high-performance liquid chromatographic technique for the measurement of hydralazine pyruvic acid hydrazone is described. This method utilized reversed-phase chromatography for the separation of this hydrophilic metabolite of hydralazine from other fluid constituents present in serum, plasma, or urine of human volunteers and rabbits receiving hydralazine. Detection of the compound of interest is accomplished spectrophotometrically at 250 nm. PMID:7358814
Haegele, K D; Skrdlant, H B; Talseth, T; McNay, J L; Shepherd, A M; Clementi, W A
Pharmacokinetics of hydralazine and its acid-labile hydrazone metabolites in relation to acetylator phenotype
The pharmacokinetics of hydralazine (H) and its acid-labile hydrazone metabolites were compared in rapid and slow acetylators. Following a 20-mg intravenous infusion, the elimination half-life (t1\\/2ß) and the apparent volume of distribution of H did not differ between the two groups. Plasma clearance estimates approached hepatic blood flow. When a single 100-mg dose of H was given-orally, the area under
Danny D. Shen; James P. Hosler; Richard L. Schroder; Daniel L. Azarnoff
Synthesis, characterization, and in vitro antimicrobial evaluation of hydrazone and bishydrazone derivatives of isatin
A new series of hydrazone and bishydrazone derivatives was synthesized starting from adipic dihydrazide, oxalyl dihydrazide,\\u000a 4-hydroxybenzhydrazide, 2-furancarboxylic acid hydrazide, acetohydrazide, 4-pyridinecarboxylic acid hydrazide, and isatin.\\u000a The chemical structures were confirmed by means of 1H-NMR, UV, and IR spectral data and elemental analysis. The synthesized compounds were evaluated in vitro as antimicrobial\\u000a agents against representative strains of Gram-positive (clinical strains
Hadi Adibi; Mohammad Mehdi Khodaei; Parvaneh Pakravan; Ramin Abiri
Amorphous lercanidipine hydrochloride and uses thereof
US Patent & Trademark Office Database
The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous lercanidipine, as well as methods of providing rapid relief from hypertension by administering the substantially pure amorphous lercanidipine hydrochloride of the present invention to a patient in need of such treatment.
Bach adsorption study for the extraction of silver ions by hydrazone compounds from aqueous solution.
Sorbent materials based on a hydrazone Schiff base compound, C(14)H(11)BrN(4)O(4), were prepared either by immobilizing the ligand into sol-gel (SG1) or bonding to silica (SG2). The sorbent materials were characterized by FT-IR, EDX, SEM, TEM, and TGA. The sorption characteristics of a matrix of eight transition metal ions (Ag(+), Cu(2+), Co(2+), Ni(2+), Fe(3+), Pb(2+), Zn(2+), and Mn(2+)) using batch method were studied. Several key parameters that affected the extraction efficiency such as pH, contact time, metal ions concentration, and gel size (for SGl) were investigated and optimized. Under the optimized conditions, the physically immobilized hydrazone sorbent (SG1) exhibits highest selectivity towards Ag(+) ions, while the chemically bonded hydrazone sorbent (SG2) exhibits high extraction for all metal ions tested. However, for practical applications such as the removal and preconcentration of Ag(+), the physically immobilized sorbent (SG1) is preferred. PMID:22629138
Mohamad Ali, Abdussalam Salhin; Abdul Razak, Norfarhah; Ab Rahman, Ismail
Bach Adsorption Study for the Extraction of Silver Ions by Hydrazone Compounds from Aqueous Solution
Sorbent materials based on a hydrazone Schiff base compound, C14H11BrN4O4, were prepared either by immobilizing the ligand into sol-gel (SG1) or bonding to silica (SG2). The sorbent materials were characterized by FT-IR, EDX, SEM, TEM, and TGA. The sorption characteristics of a matrix of eight transition metal ions (Ag+, Cu2+, Co2+, Ni2+, Fe3+, Pb2+, Zn2+, and Mn2+) using batch method were studied. Several key parameters that affected the extraction efficiency such as pH, contact time, metal ions concentration, and gel size (for SGl) were investigated and optimized. Under the optimized conditions, the physically immobilized hydrazone sorbent (SG1) exhibits highest selectivity towards Ag+ ions, while the chemically bonded hydrazone sorbent (SG2) exhibits high extraction for all metal ions tested. However, for practical applications such as the removal and preconcentration of Ag+, the physically immobilized sorbent (SG1) is preferred.
Flow-injection chemiluminescence method for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride.
A sensitive and simple flow-injection chemiluminescence (FI-CL) method, which was based on the CL intensity generated from the redoxreaction of potassium permanganate (KMnO4)-formaldehyde in vitriol (H2SO4) medium, has been developed, validated and applied for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride. Besides oxidants and sensitizers, the effect of the concentration of H(2)SO(4), KMnO4 and formaldehyde was investigated. Under the optimum conditions, the linear range was 1.0 x 10(-2)-7.0 mg/L for naphazoline hydrochloride and 5.0 x 10(-2)-10.0 mg/L for oxymetazoline hydrochloride. During seven repeated inter-day and intra-day precision tests of 0.1, 1.0 and 10.0 mg/L samples, the relative standard deviations all corresponded to reference values. The detection limit was 8.69 x 10(-3) mg/L for naphazoline hydrochloride and 3.47 x 10(-2) mg/L for oxymetazoline hydrochloride (signal-to-noise ratio < or = 3). This method has been successfully implemented for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride in pharmaceuticals. PMID:19253271
Wang, Nan-Nan; Shao, Yan-Qing; Tang, Yu-Hai; Yin, He-Ping; Wu, Xiao-Zhong
Structural studies and investigation on the activity of imidazole-derived thiosemicarbazones and hydrazones against crop-related fungi.
New imidazole derived thiosemicarbazones and hydrazones were prepared by condensation of 4(5)-imidazole carboxaldehyde, 4-(1H-imidazole-1-yl)benzaldehyde and 4-(1H-imidazole-1-yl)acetophenone with a thiosemicarbazide or hydrazide. All compounds were characterized by quantitative elemental analysis, IR and NMR techniques. Eight structures were determined by single crystal X-ray diffraction. The antifungal activities of the compounds were evaluated. None of the compounds exhibited significant activity against Aspergillus flavus and Candida albicans, while 4(5)-imidazolecarboxaldehyde thiosemicarbazone (ImT) and 4-(1H-imidazole-1-yl)benzaldehyde thiosemicabazone (4ImBzT) were highly and selectively active against Cladosporium cladosporioides. 4(5)-Imidazolecarboxaldehyde benzoyl hydrazone (4(5)ImPh), 4(5)-imidazolecarboxaldehyde-para-chlorobenzoyl hydrazone (4(5)ImpClPh), 4(5)-imidazolecarboxaldehyde-para-nitrobenzoyl hydrazone (4(5)ImpNO2Ph), 4-(imidazole-1-yl)acetophenone-para-chloro-benzoyl hydrazone (4ImAcpClPh) and 4-(imidazole-1-yl)acetophenone-para-nitro-benzoylhydrazone (4ImAcpNO2Ph) were highly active against Candida glabrata. 4(5)ImpClPh and 4(5)ImpNO2Ph were very effective against C. cladosporioides. In many cases, activity was superior to that of the reference compound nystatin. PMID:24129274
Reis, Débora C; Despaigne, Angel A Recio; Da Silva, Jeferson G; Silva, Nayane F; Vilela, Camila F; Mendes, Isolda C; Takahashi, Jacqueline A; Beraldo, Heloisa
Radical cyclization in heterocycle synthesis. Part 13: Sulfanyl radical addition–cyclization of oxime ethers and hydrazones connected with alkenes for synthesis of cyclic ?-amino acids
A combination of sulfanyl radical addition–cyclization of the oxime ethers and hydrazones connected with alkenes and subsequent conversion of a phenylsulfanylmethyl group to a carboxyl group provides a novel method for the construction of the cyclic ?-amino acids. Upon treatment with thiophenol in the presence of AIBN, the oxime ethers and hydrazones smoothly underwent sulfanyl radical addition-cyclization to give the
Okiko Miyata; Kanami Muroya; Tomoko Kobayashi; Rina Yamanaka; Seiko Kajisa; Junko Koide; Takeaki Naito
Formation of 1,1-Dianions of Hydrazones by Certain Bases. N, N-Dialkylation with Halides. Decomposition to Form Hydrocarbons.
Hydrazones of ketones or aldehydes were converted by 2 equiv of potassium amide in liquid ammonia to 1,1-dipotassio salts, which were dialkylated with halides to form N,N-dialkyl derivatives. Dipotassiobenzophenone hydrazone was allowed to react with 1 eq...
E. M. Kaiser F. E. Henoch C. R. Hauser
21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.
...Proparacaine hydrochloride ophthalmic solution. 524.1982 Section 524.1982 Food and Drugs FOOD AND DRUG ADMINISTRATION...OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982 Proparacaine hydrochloride ophthalmic...
Spectrophotometric determination of oxprenolol hydrochloride as its Fe (III) complex.
A spectrophotometric determination of oxprenolol hydrochloride in pharmaceutical preparations is described. The method is based on the reaction of oxprenolol hydrochloride with Fe (III) ion in the presence of ammonium thiocyanate, in acid media. The complex formed between oxprenolol hydrochloride and Fe (III) ion was extracted with chloroform and assayed spectrophometrically at 477 nm. The results obtained are reproducible and hence the method is suitable for the determination of oxprenolol hydrochloride in pharmaceutical dosage forms. PMID:2400517
Radulovi?, D; Pe?anac, D; Zivanovi?, L; Agatonovi?-Kustrin, S
Liquid crystalline pharmacogel based enhanced transdermal delivery of propranolol hydrochloride
A novel pharmacogel was developed for the enhanced transdermal delivery of propranolol hydrochloride (PH). The synthesized prodrugs, propranolol palmitate hydrochloride (PPH) and propranolol stearate hydrochloride (PSH) self-assembled to form gel simply upon mixing alcoholic solution of prodrug with an aqueous solution in a specified ratio. By varying the ratio of prodrug, alcohol and water, three-component phase diagram was constructed which
Alok Namdeo; N. K Jain
21 CFR 522.1642 - Oxymorphone hydrochloride injection.
...2010-04-01 2010-04-01 false Oxymorphone hydrochloride injection. 522.1642...FORM NEW ANIMAL DRUGS § 522.1642 Oxymorphone hydrochloride injection. (a) Specifications...drug contains 1 or 1.5 milligrams of oxymorphone hydrochloride per milliliter of...
...2009-04-01 2009-04-01 false Oxymorphone hydrochloride injection. 522.1642...FORM NEW ANIMAL DRUGS § 522.1642 Oxymorphone hydrochloride injection. (a) Specifications...drug contains 1 or 1.5 milligrams of oxymorphone hydrochloride per milliliter of...
Antiproliferative effects of metal complexes of new isatin hydrazones against HCT116, MCF7 and HELA tumour cell lines.
New hydrazone ligands (HL) derived from 5-substituted isatins and 1-(4-(2-methoxybenzyl)-6-arylpyridazin-3-yl)hydrazines and its complexes with Co(II) and Cu(II) were synthesized. The new hydrazones and their complexes were characterized by means of elemental, spectral analyses and magnetic studies. Primary cytotoxicity evaluation of HL 5a and the new complexes showed that these complexes could act as anticancer agents since they reduced the growth of samples of human tumour cell lines (HCT116((Colon)), MCF7((Breast)) and HELA((Cervix))) to ?18.5 ?g/mL for the new complexes. PMID:21699460
Kandile, Nadia G; Mohamed, Mansoura I; Ismaeel, Hind M
Two Zn(II) and one Mn(II) complexes using two different hydrazone ligands: spectroscopic studies and structural aspects
Three new coordination complexes of Zn(II) and Mn(II) have been synthesised using two different tridentate N,N,O donor hydrazone\\u000a ligands, Hpbh and Hacpbh respectively. The complexes [Zn(pbh)2] (1) and [Zn(acpbh)2] (2) have been synthesized by the treatment of ZnSO4 · 7H2O with Hpbh and Hacpbh hydrazone ligands, respectively. The Mn(II) complex [Mn(acpbh)2] (3) was obtained on reacting Mn(NO3)2 · 4H2O with the ligand Hacpbh. The
Aurkie Ray; Sambuddha Banerjee; Soma Sen; Ray J. Butcher; Georgina M. Rosair; Maria T. Garland; Samiran Mitra
Synthesis, formulation, and clinical pharmacological evaluation of hydralazine pyruvic acid hydrazone in two healthy volunteers.
Hydralazine pyruvic acid hydrazone [2-(phthalazin-1-yl hydrazono)propionic acid; 1] is a major plasma metabolite of hydralazine in humans. A number of in vitro and animal studies have suggested that this hydrazone may have cardiovascular activity and could account for the prolonged antihypertensive effect of hydralazine in humans in the absence of detectable plasma levels of the parent drug. To study this possibility, the soluble sodium salt of hydralazine pyruvic acid hydrazone (2) was synthesized, its chemical purity and stability was checked, and an intravenous formulation was prepared. Isomeric forms were identified. Doses of 0.3, 0.6, and 1.1 mumol/kg of 2 were administered intravenously to one slow and one heterozygous fast acetylator of sulfamethazine. The slow acetylator received two additional doses of 0.06 and 0.14 mumol/kg. Peak plasma levels of 1 of 18 mumol/L were attained without tachycardia or hypotension in either subject. There was no evidence of nonlinearity in kinetics over the dose range studied and clearance remained constant in both subjects (0.517 +/- 0.033 mL/min/kg in the slow acetylator and 0.744 +/- 0.058 mL/min/kg in the fast acetylator). The distribution of 1 varied unpredictably with dose, and changes were reflected in the terminal half-life (3.47-5.97 h in the slow acetylator and 2.06-5.33 h in the fast acetylator). Only traces of the acetylated metabolite of hydralazine, 3-methyl-s-triazolo[3,4-a]phthalazine (3), were detected in the plasma of the subjects, suggesting that significant metabolism via this route was unlikely. An established and specific assay for hydralazine was further modified to allow measurement of levels as low as 1 nmol/L (0.2 ng/mL).(ABSTRACT TRUNCATED AT 250 WORDS) PMID:3989691
Reece, P A; Stafford, I; Prager, R H; Walker, G J; Zacest, R
Copper-catalyzed rearrangement of (Z)-propynal hydrazones via N-N bond cleavage.
Propynal hydrazones are successfully converted to the corresponding 3-aminoacrylonitriles in the presence of copper catalysts in good to high yields. As an example, (Z)-N-(hex-2-ynylidene)morpholin-4-amine reacted in the presence of 10 mol % Cu(OAc)(2) in acetonitrile at 25 °C to afford (E)-3-morpholinohex-2-enenitrile ((E)-2 h) in 77% yield via C-N bond formation and subsequent ?-elimination involving cleavage of N-N and C-H bonds. PMID:20718477
Nakamura, Itaru; Shiraiwa, Naozumi; Kanazawa, Ryo; Terada, Masahiro
A C3-symmetric colorimetric anion sensor bearing hydrazone groups as binding sites
Tris-hydrazone ( 1) functioned as a colorimetric chemosensor for a variety of anions such as F -, AcO - and H 2PO 4-. The anion binding could be easily detected by naked-eye according to color changes. The high binding ability of the receptor 1 to anions was further investigated by UV-vis absorption spectroscopy in DMSO. The results of job plot of the receptor 1 with different anions demonstrated that the stoichiometry of the complex between 1 and F - was 1:1 ( 1:anion) and the stoichiometry of the other complexes studied was 1:3 ( 1:anion).
Shao, Jie; Qiao, Yanhong; Lin, Hai; Lin, Huakuan
Syntheses and extraction properties of novel biscalixarene and thiacalix[4]arene hydrazone derivatives
By reacting thiacalix[4]arene with p-tosyloxyethoxylbenzaldehyde 1, 3-bis(benzaldehyde-4-oxyethyloxy)-p-tert-butylthiacalix[4]arene (2) were prepared in yield of 65%. Refluxing compound 2 with aniline, salicylic hydrazide, nicotinic hydrazide and isonicotinic hydrazide, novel ringopening 1,3-bis-arylformyl-hydrazone substituted thiacalix[4]arene derivatives (3a–3d) were obtained in yields of 77–89%. Refluxing compound 2 with o-phenylendiamine, oxalyl dihydrazide, malonic dihydrazide and adipic dihydrazide in "1 + 1" intermolecular condensation mode\\u000a under diluted condition, novel
Fafu Yang; Xia Zhao; Hongyu Guo; Jianrong Lin; Zhaohui Liu
Simultaneous Estimation of Metformin Hydrochloride and Pioglitazone Hydrochloride by RPHPLC Method from Combined Tablet Dosage Form
A high performance reverse phase liquid chromatographic procedure is developed for simultaneous estimation of metformin hydrochloride and pioglitazone hydrochloride in combined tablet dosage form. The mobile phase used was a combination of acetonitrile:water:acetic acid (60:40:0.3) and the pH was adjusted to 5.5 by adding triethylamine. The detection of the combined dosage form was carried out at 230 nm and a flow rate employed was 1 ml/min. Linearity was obtained in the concentration range of 0.015 to 0.120 ?g/ml of pioglitazone hydrochloride and 0.5 to 4.0 ?g/ml of metformin hydrochloride with a correlation coefficient of 0.9992 and 0.9975. The results of the analysis were validated statistically and recovery studies confirmed the accuracy and precision of the proposed method.
Sahoo, P. K.; Sharma, R.; Chaturvedi, S. C.
RP-HPLC and Spectrophotometric Estimation of Ambroxol Hydrochloride and Cetirizine Hydrochloride in Combined Dosage Form.
Rapid, precise, accurate, specific and sensitive reverse phase liquid chromatographic and absorbance ratio spectrophotometric methods have been developed for the simultaneous analysis of ambroxol hydrochloride and cetirizine hydrochloride in their tablet formulation. The chromatographic methods were standardized using a HIQ SIL-C(18) column (250×4.6 mm i.d., 10 ?m particle size) with UV detection at 229 nm and mobile phase consisting of methanol-acetonitrile-water (40:40:20, v/v/v). Ambroxol hydrochloride and cetirizine hydrochloride have absorbance maxima at 243 nm and 229 nm, respectively. The isoabsorptive wavelength for both the drugs was 236 nm. For absorbance ratio method developed, wavelengths selected were 243 nm and 236 nm. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of the developed method were compared by performing ANOVA. PMID:21394256
Bhatia, Neela M; Ganbavale, S K; Bhatia, M S; More, H N; Kokil, S U
RP-HPLC and Spectrophotometric Estimation of Ambroxol Hydrochloride and Cetirizine Hydrochloride in Combined Dosage Form
Rapid, precise, accurate, specific and sensitive reverse phase liquid chromatographic and absorbance ratio spectrophotometric methods have been developed for the simultaneous analysis of ambroxol hydrochloride and cetirizine hydrochloride in their tablet formulation. The chromatographic methods were standardized using a HIQ SIL-C18 column (250×4.6 mm i.d., 10 ?m particle size) with UV detection at 229 nm and mobile phase consisting of methanol-acetonitrile-water (40:40:20, v/v/v). Ambroxol hydrochloride and cetirizine hydrochloride have absorbance maxima at 243 nm and 229 nm, respectively. The isoabsorptive wavelength for both the drugs was 236 nm. For absorbance ratio method developed, wavelengths selected were 243 nm and 236 nm. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of the developed method were compared by performing ANOVA.
Bhatia, Neela M.; Ganbavale, S. K.; Bhatia, M. S.; More, H. N.; Kokil, S. U.
21 CFR 184.1676 - Pyridoxine hydrochloride.
...170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and snack foods as defined in § 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...
Novel colorimetric sensors for cyanide based on azo-hydrazone tautomeric skeletons
The monoazo dyes, 4-carboxyl-2, 6-dinitrophenylazohydroxynaphthalenes dyes (AZ-01, AZ-03 and AZ-04), were evaluated as a highly selective colorimetric chemosensor for cyanide ion. The recognition of cyanide ion gave an obvious colour change from light yellow to brownish red and upon dilution with acetone produced a purple to lilac colour. Optimum conditions for the reaction between the azo dyes and cyanide ion were established at 30 °C for 5 min, and different variables affecting the reaction were carefully studied and optimised. Under the optimum conditions, linear relationships between the CN- concentrations and light absorption were established. Using these azo-hydrazone molecular switch entities, excellent selectivity towards the detection of CN- in aqueous solution over miscellaneous competitive anions was observed. Such selectivity mainly results from the possibility of nucleophilic attack on the azo-hydrazone chemosensors by cyanide anions in aqueous system, which is not afforded by other competing anions. The cyanide chemosensor method described here should have potential application as a new family probes for detecting cyanide in aqueous solution.
Adegoke, Olajire A.; Adesuji, Temitope E.; Thomas, Olusegun E.
In vitro kinetic studies of the reaction of hydralazine and its acetone hydrazone with pyruvic acid.
To understand the reaction between hydralazine (HP) or its acetone hydrazone (HAH), a metabolite of HP and pyruvic acid, a new selective HPLC method for simultaneous determination of HP, HAH, and hydralazine pyruvic acid hydrazone (HPH) was developed. In vitro degradation of HAH and formation of HP and HPH were investigated at pH 7.4 and 37 degrees C in the presence or absence of pyruvic acid. Hydralazine degraded slowly according to an apparent first-order rate (7.46 x 10(-2)h-1). The degenerative reaction of HAH, accompanied by simultaneous hydrolysis to the parent drug HP, was also subject to apparent first-order loss (3.00 x 10(-1)h-1). In addition, HAH was partly converted to HP and HPH in the presence of pyruvic acid. For the formation pathway of HPH, a model that included the direct reaction of HAH with pyruvic acid and the secondary formation mediated by back-conversion to HP gave a better fit to the experimental data than the model consisting of the latter reaction only. About 10% of the HPH formed was generated by the direct reaction of HAH with pyruvic acid, based on the rate constants estimated. These results suggest that the formation of HPH is not all accomplished through back-conversion to HP. PMID:3373434
Iwaki, M; Ogiso, T; Ito, Y
Pharmacokinetics and biotransformation of hydralazine acetone hydrazone, a metabolite of hydralazine, in the rat.
The pharmacokinetics of hydralazine acetone hydrazone (HAH), which is a metabolite of hydralazine (HP), was investigated after iv administration to rats. Plasma concentrations of HAH, HP, and hydralazine pyruvic acid hydrazone (HPH) were simultaneously determined by a specific HPLC method. A five-compartment pharmacokinetic model was presented to elucidate the disposition of HAH and two products, HP and HPH. The parameters used in the model were obtained by administering each of the three compounds (10 mg/kg) separately. The proposed model described the experimental data well and the model parameters were close to the model-independent values. After HP administration, HPH appeared rapidly in plasma, but the HPH availability from HP amounted to only 17.8 +/- 3.7%, based on the comparison between the area under the plasma concentration curves of formed and iv HPH. The formation of HP from HAH in the systemic circulation was demonstrated, but formed HP disappeared rapidly. The fraction of HAH available to the systemic circulation as HPH was extremely low (7.8 +/- 2.2%), indicating that the conversion of HAH to HP was not so extensive. The present results support the hypotheses that HPH is formed via the direct reaction of HAH with pyruvic acid and that the secondary formation is mediated by conversion to HP. PMID:2600796
Hexa-arm star shaped hydrazone derivatives from hexakis(4-formylphenoxy)-cyclotriphosphazene core
A series of novel hexasubstituted cyclophosphazene hydrazones [N 3P 3( sbnd OC 6H 4sbnd psbnd CH dbnd N sbnd NH sbnd C(O) sbnd C 6H 4sbnd psbnd X) 6] (X = H, Br, Cl, F, OH, OCH 3, CH 3, NO 2, NH 2) were prepared by a sixfold condensation reaction of [N 3P 3( sbnd OC 6H 4sbnd psbnd CHO) 6] with para-substituted benzoic hydrazides [NH 2sbnd NH sbnd C(O) sbnd C 6H 4sbnd psbnd X] with excellent yields (91-98%). The structures of the compounds were confirmed by elemental analysis, FT-IR, 1H, 13C, 31P, 2D-HSQC NMR and mass spectrometry (MALDI-TOF). All the synthesized cyclophosphazene hydrazones exhibit high thermal stability. The crystal structure of a homogeneously substituted hexakis(4-formylphenoxy)-cyclotriphosphazene was determined by X-ray diffraction analysis. The compound crystallizes in the monoclinic system, space group P2 1/n with a = 16.558(3) Ĺ, b = 10.250(2) Ĺ, c = 23.429(5) Ĺ, ? = ? = 90.00°, ? = 90.461(4)°, V = 3976.5(14) Ĺ 3 and Z = 4. The R value is 0.0823 for 4290 observed reflections. The conformations of the 4-formylphenoxy-groups are different at the three phosphorus atoms.
Patil, Basavaraj R.; Machakanur, Shrinath S.; Badiger, Dayananda S.; Hunoor, Rekha S.; Gudasi, Kalagouda B.; Nethaji, Munirathinam; Annie Bligh, S. W.
Convenient Method for Reduction of CN Double Bonds in Oximes, Imines, and Hydrazones Using Sodium Borohydride–Raney Ni System
A practical method has been developed for reduction of C-N double bond in oximes, imines, and hydrazones with sodium borohydride catalyzed by Raney Ni. The reactions were carried out in basic aqueous solution, and the desired products were obtained in moderate yields after a simple procedure. This method can be applied to synthesize simpler aliphatic or aromatic amines and its
Yihua Yang; Shouxin Liu; Junzhang Li; Xia Tian; Xiaoli Zhen; Jianrong Han
Overestimation of rifampicin during colorimetric analysis of anti-tuberculosis products containing isoniazid due to formation of isonicotinyl hydrazone
When present together in fixed-dose combinations (FDC) of anti-tuberculosis drugs, rifampicin (R) and isoniazid (H) interact with each other to form isonicotinyl hydrazone (HYD). In a preliminary study, this product was found to possess similar colorimetric spectrum to that of rifampicin. Therefore, an investigation was undertaken to determine interference of HYD during analysis of rifampicin in FDC products by colorimetry.
T. T. Mariappan; K. C. Jindal; Saranjit Singh
Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops
Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H1 receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol®) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday®. It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future.
Uchio, Eiichi
Immobilisation of impala (Aepyceros melampus) with a ketamine hydrochloride/medetomidine hydrochloride combination, and reversal with atipamezole hydrochloride.
A combination of medetomidine hydrochloride (medetomidine) and ketamine hydrochloride (ketamine) was evaluated in 16 boma-confined and 19 free-ranging impalas (Aepyceros melampus) to develop a non-opiate immobilisation protocol. In free-ranging impala a dose of 220 +/- 34 microg/kg medetomidine and 4.4 +/- 0.7 mg/kg ketamine combined with 7500 IU of hyaluronidase induced recumbency within 4.5 +/- 1.5 min, with good muscle relaxation, a stable heart rate and blood pH. PaCO2 was maintained within acceptable ranges. The animals were hypoxic with reduced oxygen saturation and low PaO2 in the presence of an elevated respiration rate, therefore methods for respiratory support are indicated. The depth of sedation was adequate for minor manipulations but additional anaesthesia is indicated for painful manipulations. Immobilisation was reversed by 467 +/- 108 microg/kg atipamezole hydrochloride (atipamezole) intramuscularly, but re-sedation was observed several hours later, possibly due to a low atipamezole:medetomidine ratio of 2:1. Therefore, this immobilisation and reversal protocol would subject impalas to possible predation or conspecific aggression following reversal if they were released into the wild. If the protocol is used on free-ranging impala, an atipamezole:medetomidine ratio of 5:1 should probably be used to prevent re-sedation. PMID:15214689
Bush, M; Raath, J P; Phillips, L G; Lance, W
Optical and thermal properties of nickel(II) hydrazone complex for recordable blu-ray storage
A nickel(II) hydrazone complex was synthesized in order to obtain a suitable optical recording medium for the new generation recordable blu-ray disk. Smooth thin films of the nickel(II) hydrazone complex were prepared by using the spin-coating method. Absorption and reflectance spectra of the thin films were evaluated in the wavelength 300-700 nm. Thermal properties of the nickel(II) complex were investigated by thermogravimetry (TG) and differential scanning calorimetry (DSC). Optical constants (complex refractive indices N=n+ik) and thickness of the thin film, prepared on single-crystal silicon substrate, were investigated on a rotating analyzer-polarizer scanning ellipsometer in the wavelength 285-705 nm. In addition, in order to examine its possible use as a blu-ray recording medium, the spin-coated film of the nickel(II) complex was prepared on K9 glass substrate with a silver reflective layer, and was studied by static optical recording testing system with a 406.7 nm laser. It is found that the absorption spectra of the thin film has an strong absorption band in the wavelength region 360-420 nm and a moderate absorbance at the 405 nm side, which indicates that the absorption of the film is well matched with the laser wavelength of the 405 nm. The reflectance spectra show that a high reflectivity of the thin film at 405 nm wavelength can be obtained by an optimum film thickness and an appropriate metal reflective layer. The thin film of the nickel(II) complex gives a high n value of 1.62 and a low k value of 0.33, corresponding to the wavelength of the blue laser of 405 nm. Measurements of the thermal properties show that the nickel(II) complex holds a high thermal stability (~ 300 °C) and a sharp weight loss which are helpful to fabricate a small and sharp recording mark edge. The results of the static optical recording test, using the nickel(II) complex thin film as the recording layer, demonstrate that high reflectivity contrast (>50 %) can be obtained at an optimum laser writing power and pulse width. In addition, the recording marks are durable even after 20000 times readout. These preliminary results indicate that the nickel(II) hydrazone complex has great potential application for high-density discrecordable system at wavelength of the 405 nm.
Chen, Zhimin; Wu, Yiqun; Gu, Donghong; Gan, Fuxi
21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.
...isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c...isoflupredone acetate, tetracaine hydrochloride ointment. (a) Specifications. The...tetracaine hydrochloride in each gram of ointment. (b) Sponsor. See No....
77 FR 16036 - Determination That CITANEST (Prilocaine Hydrochloride) Injection, 1%, 2%, and 3%, and CITANEST...
Federal Register 2010, 2011, 2012, 2013
...Hydrochloride) Injection, 1%, 2%, and 3%, and CITANEST PLAIN (Prilocaine Hydrochloride...hydrochloride (HCl)) Injection, 1%, 2%, and 3%, and CITANEST PLAIN (prilocaine HCl...prilocaine HCl injection, 1%, 2%, and 3%, and prilocaine HCl injection,...
Hypotensive effect of the hydralazine--acetone hydrazone in conscious rabbits: evidence for its back-conversion to hydralazine in vivo.
The hydralazine--acetone hydrazone (HAH) has previously been identified as a metabolite of hydralazine (H) in humans. We compared the hypotensive effects of HAH and H in groups of hypertensive rabbits. Both compounds caused a dose-dependent depressor response, with a potency ratio of HAH to H of approximately 0.2. Upon their intravenous administration to anephric rabbits, both H and HAH produced sustained concentrations in plasma of the H-pyruvic acid hydrazone, demonstrating that back-conversion of HAH to H occurred in vivo. We conclude that HAH is hydrolyzed in vivo to yield parent H. The levels of the H-metabolite, the pyruvic acid hydrazone, suggest that the hypotensive effect of HAH could be explained entirely by generation of H in vivo. This combined pharmacokinetic and pharmacodynamic approach can be applied to other H-hydrazones to evaluate their backconversion to H in vivo. PMID:6177931
Talseth, T; McNay, J L; Haegele, K D
One-Pot Synthesis of Highly Functionalized Stable Ketenimines by Three-Component Reaction of Cyclohexyl Isocyanide, Dialkyl Acetylenedicarboxylates, and Benzoyl Hydrazones
The adduct produced in the reaction between cyclohexyl isocyanide and dialkyl acetylenedicarboxylates was trapped by benzoyl hydrazones to afford highly functionalized ketenimines in good yields. The reaction is characterized by mild conditions, high selectivity, and tolerance to various functional groups.
Mohammad Anary-Abbasinejad; Fatemeh Ghanea; Hossein Anaraki-Ardakani
Study on fluorescence characteristics of duloxetine hydrochloride.
The fluorescence characteristics of duloxetine hydrochloride are studied in this paper. The fluorescence emission spectra of duloxetine demonstrate that intramolecular charge-transfer takes place between thiophene ring and napthalenyloxy group upon irradiation. The effects of excitation light, solvent system, variation of solution pH value, metal ions and vitamin C on the fluorescence spectra of duloxetine hydrochloride are elucidated, respectively. A spectrofluorometric method of quantitative determination of duloxetine in dosage form is reported for the first time, the linear range is 7.14 x 10(-8)mol/L to 1.43 x 10(-5)mol/L, the linear correlation coefficient r is equal to 0.9997, and the detection limit is 3.5 x 10(-8)mol/L. The accuracy and the precision are satisfactory. PMID:18374628
Liu, Xiangping; Du, Yingxiang; Wu, Xiulan
Study on fluorescence characteristics of duloxetine hydrochloride
The fluorescence characteristics of duloxetine hydrochloride are studied in this paper. The fluorescence emission spectra of duloxetine demonstrate that intramolecular charge-transfer takes place between thiophene ring and napthalenyloxy group upon irradiation. The effects of excitation light, solvent system, variation of solution pH value, metal ions and vitamin C on the fluorescence spectra of duloxetine hydrochloride are elucidated, respectively. A spectrofluorometric method of quantitative determination of duloxetine in dosage form is reported for the first time, the linear range is 7.14 × 10 -8 mol/L to 1.43 × 10 -5 mol/L, the linear correlation coefficient r is equal to 0.9997, and the detection limit is 3.5 × 10 -8 mol/L. The accuracy and the precision are satisfactory.
Arrhythmogenic potential of dopexamine hydrochloride during halothane anaesthesia in dogs
Dopexamine hydrochloride (Dopacard®) is the novel synthetic catecholamine designed for use in the acute management of a low\\u000a cardiac output status. In addition to dopaminergic receptor stimulation, dopexamine hydrochloride is a potent ?2 adrenoreceptor agonist with negligible direct ?1 and no alpha adrenergic effect. The objective of this study was to compare the arrhythmogenic effects of dopexamine hydrochloride\\u000a and dopamine
Steven M. Neustein; Ivan Dimich; Ian Sampson; Ali Sadeghi; Craig Mezrow; Howard Shiang
Mucoadhesive bilayer tablets of propranolol hydrochloride
The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive\\u000a polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer.\\u000a The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling\\u000a index, in vitro drug release, ex vivo drug permeation, ex
Vishnu M. Patel; Bhupendra G. Prajapati; Harsha V. Patel; Karshanbhi M. Patel
Tapentadol hydrochloride: A centrally acting oral analgesic
Background: Tapentadol hydrochloride is a centrally acting oral analgesic approved by the US Food and Drug Administration in November 2008 for the treatment of moderate to severe acute pain. It is available as immediate-release 50-, 75-, and 100-mg tablets.Objective: The purpose of this article is to review animal studies, pharmacokinetic studies, drug-drug interaction studies, and Phase II\\/III trials of tapentadol
William E. Wade; William J. Spruill
Flow injection potentiometric determination of pipazethate hydrochloride.
New plastic membrane electrodes for pipazethate hydrochloride based on pipazethatium phosphotungstate, pipazethatium phosphomolybdate and a mixture of the two were prepared. The electrodes were fully characterized in terms of composition, life span, pH and temperature and were then applied to the potentiometric determination of the pipazethate ion in its pure state and pharmaceutical preparations under batch and flow injection conditions. The selectivity of the electrodes towards many inorganic cations, sugars and amino acids was also tested. PMID:11205518
Abdel-Ghani, N T; Shoukry, A F; el Nashar, R M
Potassium N-iodo p-toluenesulfonamide (TsNIK, Iodamine-T): a new reagent for the oxidation of hydrazones to diazo compounds.
A new reagent for the oxidation of hydrazones to diazo compounds is described. N-Iodo p-toluenesulfonamide (TsNIK, iodamine-T) allows the preparation of ?-diazoesters, ?-diazoamides, ?-diazoketones and ?-diazophosphonates in good yield and in high purity after a simple extractive work-up. ?-Diazoesters were also obtained in high yield from the corresponding ketones through a one-pot process of hydrazone formation/oxidation. PMID:24615944
Nicolle, Simon M; Moody, Christopher J
Particle size distribution of cocaine hydrochloride
A principal method for the detection of concealed shipments of cocaine hydrochloride relies upon the intake of an air sample taken near a surface onto an analytical instrument, and the detection of the narcotic present in the air or surface materials collected. The low vapor pressure of cocaine at normal temperatures indicates that particulate material present on the surfaces of target packages affords a higher probability of collection of detectable mass than does a vapor sample. An accurate representation of the particles in question is required, both for theoretical sampler design and for the performance of meaningful tests of instrument capabilities. Existing test methods for target particle preparation call for use of sand particles ranging in size from 20 to 100 micrometers in diameter, coated with a solution of cocaine hydrochloride. In this study, three seized samples and pharmaceutical cocaine hydrochloride were analyzed using an Aerosizer to measure the size distribution of the air-dispersed particles. The results obtained during these tests indicate that the actual size range of the particles is significantly smaller than the test particles cited. Results obtained in instrument evaluations using the larger target particles may therefore be misleading.
Kuhlman, Michael R.; Gooding, Rachel E.; Kogan, Vladimir G.; Bridges, Curtis
Bulk synthesis of exfoliated two-dimensional polymers using hydrazone-linked covalent organic frameworks.
Two-dimensional (2D) polymers assemble organic subunits into covalently linked, high-aspect-ratio networks with long-range order. Despite recent advances in 2D polymerization, scalable and general methods to access few- and single-layer materials are limited. Here we exfoliate a hydrazone-linked covalent organic framework (COF) to yield bulk quantities of few-layer two-dimensional (2D) polymers. Immersing the COF powder in several laboratory solvents exfoliates and disperses thin COF-43 samples, which maintain their characteristic periodic hexagonal structure. This phenomenon was characterized using infrared spectroscopy, dynamic light scattering, atomic force microscopy, transmission electron microscopy, and selected area electron diffraction. 2D COFs with reduced interlayer interaction energies offer a new means to access high-aspect-ratio 2D polymers whose structure may be designed using established principles of COF synthesis. PMID:24053107
Bunck, David N; Dichtel, William R
Synthesis of some novel hydrazone and 2-pyrazoline derivatives: Monoamine oxidase inhibitory activities and docking studies.
A novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively and reversibly. With the exception of 5i, which was a selective MAO-B inhibitor, all derivatives inhibited hMAO-A potently and selectively. According to the experimental Ki values, compounds 6e and 6h exhibited the highest inhibitory activity towards the hMAO-A, whereas compound 5j, which carries a bromine atom at R(4) of the A ring of the pyrazoline, appeared to be the most selective MAO-A inhibitor. Tested compounds were docked computationally into the active site of the hMAO-A and hMAO-B isozymes. The computationally obtained results were in good agreement with the corresponding experimental values. PMID:24986657
Evranos-Aksöz, Begüm; Yabano?lu-Çiftçi, Samiye; Uçar, Gülberk; Yelekçi, Kemal; Ertan, Rahmiye
Benzaldehyde, 2-hydroxybenzoyl hydrazone derivatives as inhibitors of the corrosion of aluminium in hydrochloric acid.
The effect of benzaldehyde, 2-hydroxybenzoyl hydrazone derivatives on the corrosion of aluminium in hydrochloric acid has been investigated using thermometric and polarization techniques. The inhibitive efficiency ranking of these compounds from both techniques was found to be: 2>3>1>4. The inhibitors acted as mixed-type inhibitors but the cathode is more polarized. The relative inhibitive efficiency of these compounds has been explained on the basis of structure of the inhibitors and their mode of interaction at the surface. Results show that these additives are adsorbed on an aluminium surface according to the Langmuir isotherm. Polarization measurements indicated that the rate of corrosion of aluminium rapidly increases with temperature over the range 30-55 degrees C both in the absence and in the presence of inhibitors. Some thermodynamic data of the adsorption process are calculated and discussed. PMID:10823698
Fouda, A S; Gouda, M M; El-Rahman, S I
Mapping Protein Surface Accessibility via an Electron Transfer Dissociation Selectively Cleavable Hydrazone Probe*
A protein's surface influences its role in protein-protein interactions and protein-ligand binding. Mass spectrometry can be used to give low resolution structural information about protein surfaces and conformations when used in combination with derivatization methods that target surface accessible amino acid residues. However, pinpointing the resulting modified peptides upon enzymatic digestion of the surface-modified protein is challenging because of the complexity of the peptide mixture and low abundance of modified peptides. Here a novel hydrazone reagent (NN) is presented that allows facile identification of all modified surface residues through a preferential cleavage upon activation by electron transfer dissociation coupled with a collision activation scan to pinpoint the modified residue in the peptide sequence. Using this approach, the correlation between percent reactivity and surface accessibility is demonstrated for two biologically active proteins, wheat eIF4E and PARP-1 Domain C.
Vasicek, Lisa; O'Brien, John P.; Browning, Karen S.; Tao, Zhihua; Liu, Hung-Wen; Brodbelt, Jennifer S.
Stability of paclitaxel with ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site administration.
The stability of paclitaxel with either ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site injection at room temperature was studied. Triplicate test solutions of paclitaxel 0.3 and 1.2 mg/mL were admixed 1:1 with ondansetron 0.03 and 0.3 mg/mL (as the hydrochloride salt) or ranitidine 0.5 and 2.0 mg/mL (as the hydrochloride salt). Also, paclitaxel 1.2 mg/mL was admixed 1:1:1 with ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL. The solutions were stored in glass containers at room temperature, and samples were removed at zero, one, two, and four hours for immediate assay. At the time of the assay and before any dilution, each sample was visually inspected for clarity, color, and precipitation, and the pH was determined. Drug concentrations were measured by stability-indicating high-performance liquid chromatographic procedures. Throughout the study, more than 90% of the initial concentrations of paclitaxel, ondansetron, and ranitidine remained in the solutions. No precipitates, color changes, or haziness was seen. The changes in pH were minor. Paclitaxel in concentrations of 0.3 and 1.2 mg/mL was stable when mixed with either ondansetron (0.03 or 0.3 mg/mL, as the hydrochloride salt) or ranitidine (0.5 or 2.0 mg/mL, as the hydrochloride salt) and stored in glass containers for four hours. Paclitaxel 1.2 mg/mL was also stable when mixed with both ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL and stored in glass containers for four hours. PMID:7913797
Burm, J P; Jhee, S S; Chin, A; Moon, Y S; Jeong, E; Nii, L; Fox, J L; Gill, M A
21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.
...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...oxytetracycline and 10,000 units of polymyxin B sulfate. (b) Sponsor....
Reactions of resin-bound triazenes with dithianylium tetrafluoroborates: efficient synthesis of ?-azo ketene dithioacetals and related hydrazones.
The conversion of dithianylium cations into ?-azo ketene dithioacetals via addition of polymer-bound diazonium precursors is shown. This new procedure allows the synthesis of ?-azo ketene dithioacetals in one step within 2-90 min at rt and yields highly pure compounds that do not have to be purified in most cases. The ?-azo ketene dithioacetals obtained have been shown to be valuable intermediates for the synthesis of hydrazones, ?-halogenated ?-azo ketene dithioacetals, and azo-functionalized dienes. PMID:24517451
Jung, Nicole; Stanek, Bettina; Gräßle, Simone; Nieger, Martin; Bräse, Stefan
Synthesis and antituberculosis activity of derivatives of Stevia rebaudiana glycoside steviolbioside and diterpenoid isosteviol containing hydrazone, hydrazide, and pyridinoyl moieties
Conjugates of the antituberculosis drug isoniazid (isonicotinyl hydrazine) and isomeric hydrazides of nicotinic and ?-picolinic\\u000a acid with glycoside steviolbioside from the Stevia rebaudiana plant and the product of its acid hydrolysis, diterpenoid isosteviol, were synthesized. In addition, isosteviol hydrazide\\u000a and hydrazone derivatives as well as conjugates containing two isosteviol moieties joined by a dihydrazide linker were obtained.\\u000a The parental compounds
V. E. Kataev; I. Yu. Strobykina; O. V. Andreeva; B. F. Garifullin; R. R. Sharipova; V. F. Mironov; R. V. Chestnova
Synthesis and characterization of novel hydrazide–hydrazones and the study of their structure–antituberculosis activity
A series of hydrazide–hydrazones, based on a series of 4-substituted benzoic acid, were synthesized, and their structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv with the help of the BACTEC 460 radiometric system. Compound 3, 4-fluorobenzoic acid [((5-nitro)thiophen-2yl) methylene]hydrazide showed the highest inhibitory activity in this series. The search of pharmacophores was done by means
Koçyi?it-Kaymakç?o?lu Bedia; Oruç Elçin; Unsalan Seda; Kandemirli Fatma; Shvets Nathaly; Rollas Sevim; Anatholy Dimoglo
Preparation of catalytically active, covalent ?-polylysine-enzyme conjugates via UV/vis-quantifiable bis-aryl hydrazone bond formation.
Covalent UV/vis-quantifiable bis-aryl hydrazone bond formation was investigated for the preparation of conjugates between ?-poly-d-lysine (PDL) and either ?-chymotrypsin (?-CT) or horseradish peroxidase (HRP). PDL and the enzymes were first modified via free amino groups with the linking reagents succinimidyl 6-hydrazinonicotinate acetone hydrazone (S-HyNic, at pH 7.6) and succinimidyl 4-formylbenzoate (S-4FB, at pH 7.2), respectively. The modified PDL and enzymes were then conjugated at pH 4.7, whereby polymer chains carrying several enzymes were obtained. Kinetics of the bis-aryl hydrazone bond formation was investigated spectrophotometrically at 354 nm. Retention of the enzymatic activity after conjugate formation was confirmed by using the substrates N-succinimidyl-l-Ala-l-Ala-l-Pro-l-Phe-p-nitroanilide (for ?-CT) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS, for HRP). Thus, not only a mild and efficient preparation and convenient quantification of a conjugate between the polycationic ?-polylysine and enzymes could be shown, but also the complete preservation of the enzymatic activity. PMID:21171644
Grotzky, Andrea; Manaka, Yuichi; Kojima, Taisuke; Walde, Peter
Interference by ascorbic acid in test systems involving peroxidase. II. Redox-coupled indicator systems.
Ascorbic acid hampers some test systems based on use of peroxidase (EC 18.104.22.168) and redox indicators, by producing a lag time in color development. With reversible indicators, no color development occurs during the ascorbic acid lag time. With oxidatively coupled indicator systems, such as 3-methyl-2-benzothiazolinone hydrazone (MBTH) and a suitable coupler such as chromotropic acid (CTA; 4,5-dihydroxynaphthalene-2,7-disulfonic acid), ascorbic acid diminishes the rate of color development, but does not abolish it. The effect of ascorbic acid strongly depends on the reaction pH as well as the nature of the coupler used. The ascorbate-elicited reduction (or lag) in color development was inversely proportional to the concentrations of MBTH and virtually unaffected by changes in CTA coupler concentration. The rate of color development following the lag was directly proportional to the concentration of MBTH but unaffected by the CTA. These observations suggest that peroxidase with H2O2 catalyzes the oxidation and activation of MBTH to an oxidized species (MBTHox). This species is reduced by ascorbic acid and at the same time couples oxidatively with CTA. Thus, the activity during the ascorbate-induced lag time reflects this competition of ascorbic acid and coupler for MBTHox. This study of peroxidase/ascorbate lag time with the redox coupled indicator system has led to the selection of fast couplers that are highly resistant to interference by ascorbic acid. Suitable resistant couplers (e.g., chromotropic acid, Chicago acid, and H acid) appear to be aromatic ring systems with highly activating substituents and directing toward electrophilic aromatic substitution at the ortho and para positions. PMID:7074825
White-Stevens, R H; Stover, L R
A Post Hoc Analysis of d- threo-Methylphenidate Hydrochloride (Focalin) Versus d, l- threo-Methylphenidate Hydrochloride (Ritalin)
Objective:To evaluate clinical measures of the benefit\\/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH).
A new mechanism-based inhibitor of photosynthetic water oxidation: Acetone hydrazone. I. Equilibrium reactions
SciTech Connect
The process of photosynthetic water oxidation has been investigated by using a new type of water oxidation inhibitor, the alkyl hydrazones. Acetone hydrazone (AceH), (CH{sub 3}){sub 2}CNNH{sub 2}, inhibits water oxidation by a mechanism that is analogous to that of NH{sub 2}OH. This involves binding to the water-oxidizing complex (WOC), followed by photoreversible reduction of manganese (loss of the S{sub 1} {yields} S{sub 2} reaction). At higher AceH concentrations the S{sub 1} state is reduced in the dark and Mn is released, albeit to a lesser extent than with NH{sup 2}OH. Following extraction of Mn, AceH is able to donate electrons rapidly to the reaction center tyrosine radical Z{sup +} ({sup 161}Tyr-D{sub 1} protein), more slowly to a reaction center radical C{sup +}, and not at all to the dark-stable tyrosine radical D{sup +} ({sup 160}Tyr-D{sub 2} protein) which must be sequestered in an inaccessible site. Unexpectedly, Cl{sup {minus}} was found not to interfere or compete with AceH for binding to the WOC in the S{sub 1} state, in contrast to the reported rate of binding of N,N-dimethylhydroxylamine (CH{sub 3}){sub 2}NOH. The authors interpret the latter behavior as due to ionic screening of the thylakoid membrane, rather than a specific Cl site involved in water oxidation. AceH appears not to bind to the acceptor side of PSII as evidenced by normal EPR signals both for Q{sub A}{sup {minus}}Fe(II), the primary electron acceptor, and for the oxidized Fe(III) acceptor (Q{sub 400} species), in contrast to that observed with NH{sub 2}OH. AceH can be oxidized in solution by a variety of oxidants including Mn(III) to form a reactive diazo intermediate, (CH{sub 3}){sub 2}CNN, which reacts with carbonyl compounds. Oxidation to this diazo intermediate is postulated to be responsible for inhibition of the WOC.
Tso, J.; Dismukes, G.C. (Princeton Univ., NJ (USA)); Petrouleas, V. (Nuclear Research Center, Athens (Greece))
Efficient Bioconjugation of Protein Capture Agents to Biosensor Surfaces Using Aniline-Catalyzed Hydrazone Ligation
Aniline-catalyzed hydrazone ligation between surface immobilized hydrazines and aldehyde-modified antibodies is shown to be an efficient method for attaching protein capture agents to model oxide-coated biosensor substrates. Silicon photonic microring resonators are used to directly evaluate the efficiency of this surface bioconjugate reaction at various pHs and in the presence or absence of aniline as a nucleophilic catalyst. It is found that aniline significantly increases the net antibody loading for surfaces functionalized over a pH range from 4.5 to 7.4, allowing derivatization of substrates with reduced incubation time and sample consumption. This increase in antibody loading directly results in more sensitive antigen detection when functionalized microrings are employed in a label-free immunoassay. Furthermore, these experiments also reveal an interesting pH dependent non-covalent binding trend that plays an important role in dictating the amount of antibody attached onto the substrate, highlighting the competing contributions of the bioconjugate reaction rate and the dynamic interactions that control opportunities for a solution-phase biomolecule to react with a substrate-bound reagent.
Byeon, Ji-Yeon; Limpoco, F. T.; Bailey, Ryan C.
Z-Group ketone chain transfer agents for RAFT polymer nanoparticle modification via hydrazone conjugation
A ketal-containing trithiocarbonyl compound has been synthesized and characterized as a chain transfer agent (CTA) in Reversible Addition Fragmentation Transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization of acrylate monomers, which proceeds as previously reported to yield macro-CTA polymers and block co-polymers. Post-polymerization ketal cleavage revealed ketone functionality at the polar terminus of an amphiphilic block co-polymer. Hydrazone-formation was facile in both organic solution as well as in aqueous buffer where polymer nanoparticle assemblies were formed, indicating a conjugation/end-functionalization yield of 40–50%. Conjugation was verified with fluorescein, biotin and Gd-DOTA derivatives, and though the trithiocarbonate linkage is hydrolytically labile, we observed stable conjugation for several days at pH 7.4. and 37°C. As expected, streptavidin binding to biotinylated polymer micelles was observed, and size-change based relaxivity increases were observed when Gd-DOTA hydrazide was conjugated to polymer micelles. Cell-uptake of fluorescently labeled polymer micelles was also readily tracked by FACS and fluorescence microscopy. These polymer derivatives demonstrate a range of potential theranostic/biotechnological applications for this conveniently accessible keto-CTA, which include ligand-based nanoparticle targeting and fluorescent/MR nanoparticle contrast agents.
Bandyopadhyay, Saibal; Xia, Xin; Maiseiyeu, Andrei; Mihai, Georgeta; Rajagopalan, Sanjay
Synthesis, characterization and studies on the nonlinear optical parameters of hydrazones
Three hydrazones, 2-(4-methylphenoxy)- N'-[(1E)-(4-nitrophenyl)methylene]acetohydrazide (compound-1), 2-(4-methylphenoxy)- N'-[(1E)-(4-methylphenyl)methylene]acetohydrazide ((compound-2) and N'-{(1E)-[4-(dimethylamino)phenyl]methylene}-2-(4-ethylphenoxy) acetohydrazide(compound-3) were synthesized and their third order nonlinear optical properties were investigated using a single beam z-scan technique with nanosecond laser pulses at 532 nm. Open aperture data obtained from the three compounds indicates two photon absorption at this wavelength. The nonlinear refractive index n2, the nonlinear absorption coefficient ?, the magnitude of the effective third order susceptibility ?(3), the second order hyperpolarizability ?h and the coupling factor ? have been estimated. The values obtained are comparable with the values obtained for 4-methoxy chalcone derivatives and dibenzylidene acetone derivatives. Among the compounds studied, compounds-1 and 3 exhibited the better optical power limiting behaviour at 532 nm. Our studies suggest that compounds-1, 2 and 3 are potential candidates for optical device applications such as optical limiters and optical switches.
Naseema, K.; Sujith, K. V.; Manjunatha, K. B.; Kalluraya, Balakrishna; Umesh, G.; Rao, Vijayalakshmi
Simultaneous UV Spectrophotometric Estimation of Ambroxol Hydrochloride and Levocetirizine Dihydrochloride
A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of ambroxol hydrochloride and levocetirizine dihydrochloride. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths 242 nm and 231 nm, the ? max of ambroxol hydrochloride and levocetirizine dihydrochloride, respectively. Beer's law was obeyed in the concentration range 10–50 ?g/ml and 8–24 ?g/ml for ambroxol hydrochloride and levocetirizine dihydrochloride respectively. Results of the method were validated statistically and by recovery studies.
Prabhu, S. Lakshmana; Shirwaikar, A. A.; Shirwaikar, Annie; Kumar, C. Dinesh; Kumar, G. Aravind
Simultaneous UV Spectrophotometric Estimation of Ambroxol Hydrochloride and Levocetirizine Dihydrochloride.
A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of ambroxol hydrochloride and levocetirizine dihydrochloride. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths 242 nm and 231 nm, the gamma max of ambroxol hydrochloride and levocetirizine dihydrochloride, respectively. Beer's law was obeyed in the concentration range 10-50 mug/ml and 8-24 mug/ml for ambroxol hydrochloride and levocetirizine dihydrochloride respectively. Results of the method were validated statistically and by recovery studies. PMID:20046721
Prabhu, S Lakshmana; Shirwaikar, A A; Shirwaikar, Annie; Kumar, C Dinesh; Kumar, G Aravind
Striking stabilization of Rana catesbeiana ribonuclease 3 by guanidine hydrochloride.
Unfolding by chemical denaturants and the linear extrapolation method are widely used to determine the free energy of proteins. Ribonuclease 3 from bullfrog shows an extraordinary behavior in guanidinium hydrochloride in comparison to its homologues ribonuclease A and onconase with a high transition midpoint of denaturation but an apparently low cooperativity. The analysis of the interdependence of thermal, urea-, and guanidine hydrochloride-induced unfolding revealed that whereas addition of urea resulted in the expected destabilization of all three proteins, guanidine hydrochloride acted diversely: in contrast to ribonuclease A and onconase, both of which were destabilized as expected, low concentrations of guanidine hydrochloride significantly stabilize ribonuclease 3 from bullfrog. This stabilizing effect was endorsed by in silico docking studies. PMID:23395613
Solé, Magali; Brandt, Wolfgang; Arnold, Ulrich
Primary Eye Irritation of Guanidine Hydrochloride in Rabbits.
The primary eye irritation potential of guanidine hydrochloride was determined in male New Zealand White rabbits using a modified Draize method. The compound produced irritation in all animals tested. Signs of irritation were erythemaz and chemosis of the...
L. D. Brown T. P. Kellner D. W. Korte
Isolation and characterization of some potential impurities in ropinirole hydrochloride.
Three impurities in ropinirole hydrochloride drug substance at levels approximately 0.06-0.15% were detected by reverse-phase high performance liquid chromatography (HPLC). These impurities were isolated from the drug substance. These impurities were analyzed using reverse-phase HPLC. Based on the spectral data (IR, NMR and MS), structures of these impurities were characterized as 4-[2-(propylamino) ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride (impurity-A), 5-[2-(diropylamino) ethyl]-1,4-dihydro-3H-benzoxazin-3-one hydrochloride (impurity-B) and 4-[2-(diropylamino) ethyl]-1H-indol-2,3-dione hydrochloride (impurity-C). Synthesis of these impurities is discussed. PMID:17207602
Sahasrabuddhey, B; Nautiyal, R; Acharya, H; Khyade, S; Luthra, P K; Deshpande, P B
21 CFR 520.2345a - Tetracycline hydrochloride capsules.
...sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the...
Arrhythmogenic potential of dopexamine hydrochloride during halothane anaesthesia in dogs.
Dopexamine hydrochloride (Dopacard) is the novel synthetic catecholamine designed for use in the acute management of a low cardiac output status. In addition to dopaminergic receptor stimulation, dopexamine hydrochloride is a potent beta 2 adrenoceptor agonist with negligible direct beta 1 and no alpha adrenergic effect. The objective of this study was to compare the arrhythmogenic effects of dopexamine hydrochloride and dopamine in dogs anaesthetized with halothane (1.2 MAC). The starting dose for dopexamine hydrochloride was 3.5 micrograms.kg-1.min-1 and for dopamine was 5 micrograms.kg-1.min-1. Concentrations of the drugs were increased until four or more premature ventricular contractions within 15 seconds were produced. All dogs developed ventricular tachycardia when dopamine was administered in concentrations ranging between 18-20 micrograms.kg-1.min-1. Unlike dopamine, dopexamine hydrochloride even at concentrations as high as 50 micrograms.kg-1.min-1 did not induce any atrial or ventricular ectopic beats. Lack of beta 1 and alpha adrenergic agonist effects is a likely explanation for low arrhythmogenicity of dopexamine hydrochloride. Both drugs increase cardiac output; dopexamine hydrochloride primarily by a dose-related increase in heart rate and increased afterload. At the maximal concentration dopexamine hydrochloride increased heart rate from 114 to 150 beat.min-1, mean arterial pressure decreased from 81 mmHg to 45 mmHg and SVR decreased from 2418 to 962 dyne.sec-1cm-5. Myocardial contractility increased only moderately, as evaluated by dP/dt, which increased from 1290 to 1696 mmHg.sec-1. Dopamine had a more marked inotropic effect: the dP/dt increased, at the maximal concentration, from 1480 to 2570 mmHg.sec-1.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:7915210
Neustein, S M; Dimich, I; Sampson, I; Sadeghi, A; Mezrow, C; Shiang, H
Identification, isolation and characterization of impurities of clindamycin palmitate hydrochloride
Clindamycin palmitate hydrochloride is a water soluble hydrochloride salt of the ester of clindamycin and palmitic acid. It is inactive in vitro, rapid in vivo hydrolysis converts this compound to the antibacterially active clindamycin. Total 12 impurities at levels ranging from 0.05% to 0.5% were detected by isocratic reverse-phase high performance liquid chromatography (HPLC) using RI detector. The molecular weights
Ch. Bharathi; P. Jayaram; Joseph Sunder Raj; M. Saravana Kumar; V. Bhargavi; V. K. Handa; Ramesh Dandala; A. Naidu
Synthesis, Magnetic, and Spectral Studies of Some Mono? and Binuclear Dioxomolybdenum(VI) Complexes with Chelating Hydrazones Derived from Acid Hydrazides and Furfural or Thiophene?2?aldehyde
This paper deals with the synthesis, magnetic and spectral studies of some mono? and binuclear dioxomolybdenum(VI) complexes with chelating hydrazones derived from salicylic acid\\/benzoic acid\\/isonicotinic acid hydrazide with thiophene?2?aldehyde or furfural. The acid hydrazones synthesized are N?(furfuralidene)?N??salicyloylhydrazine [FSAH, (I)], N?(2?thiophenidene)?N??salicyloylhydrazine [TSAH, (II)], N?(furfuralidene)?N??isonicotinoylydrazine [FINH, (III)], N?(2?thiophenidene)?N??isonicotinoylhydrazine [TINH, (IV)], N?(furfuralidene)?N??benzoylhydrazine [FBZH, (V)] and N?(2?thiophenidene)?N??benzoylhydrazine [TBZH, (VI)]. The metal complexes (1)–(6) were
R. C. Maurya; R. Verma; T. Singh
X-ray, spectroscopic and computational studies of the tautomeric structure of a new hydrazone of 5-nitrosalicylaldehyde with indole-3-acetic hydrazide
A new hydrazone of 5-nitrosalicylaldehyde with indole-3-acetic hydrazide (NSIAH) has been obtained and its structure has been studied by X-ray, FT-IR and CPMAS in the solid as well as 1H, 13C and 15N NMR in the CH3CN-d3 and DMSO-d6 solutions. The hydrazone crystallises in the Pbca space group from the orthorhombic system with a=9.5435(7) Ĺ, b=11.0932(8) Ĺ and c=29.672(2) Ĺ.
Krystian Pyta; Piotr Przybylski; Adam Huczynski; Anna Hoser; Krzysztof Wozniak; Wojciech Schilf; Bohdan Kamienski; Eugeniusz Grech; Bogumil Brzezinski
Stability of ondansetron hydrochloride in portable infusion-pump reservoirs.
The stability of ondansetron hydrochloride 0.24 and 2 mg/mL when delivered by portable infusion pump at near-body temperature over various time periods was investigated. Nine 100-mL drug reservoirs were prepared, three containing ondansetron hydrochloride 2 mg/mL and six containing ondansetron hydrochloride diluted with 0.9% sodium chloride injection to 0.24 mg/mL. Three of the reservoirs containing the diluted solution were refrigerated for up to 30 days at 3 degrees C before being attached to portable infusion pumps and pumped over 24 hours at 30 degrees C. The remaining six reservoirs were attached to pumps immediately after being filled, and the solutions were delivered for up to 24 hours (the diluted solution; three reservoirs) or up to seven days (the concentrated solution; three reservoirs) at 30 degrees C. Samples were taken initially and periodically and analyzed by high-performance liquid chromatography and with a pH meter. Both the diluted and the concentrated solutions of ondansetron hydrochloride retained at least 95% of the initial drug concentration under all the conditions studied. There was no appreciable change in pH. Ondansetron hydrochloride 0.24 mg/mL was stable when stored for up to 30 days at 3 degrees C and infused over 24 hours at 30 degrees C. Ondansetron hydrochloride 2 mg/mL was stable when infused for up to one week at 30 degrees C. PMID:1388331
Stiles, M L; Allen, L V; Fox, J L
Canine olfactory sensitivity to cocaine hydrochloride and methyl benzoate
Methyl benzoate is a consistent product of cocaine hydrochloride exposed to humid air. The detection responses of dogs trained to detect illicit cocaine hydrochloride may be controlled by vapor from cocaine, methyl benzoate, or other constituents of illicit cocaine. The present study addressed the following questions: 1) How capable are dogs of detecting methyl benzoate compared to cocaine hydrochloride, 2) When dogs are trained to detect methyl benzoate, do they respond to cocaine hydrochloride as being the same or different from methyl benzoate. These questions were investigated using random source dogs trained and tested under laboratory conditions. Odor stimuli were generated and delivered by a vapor generation systems, the outputs from which were characterized by thermal desorption GC/MS. ONe group of dogs was trained to discriminate pharmaceutical grade and illicit cocaine hydrochloride from clean air and tested using a two lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine whether they responded to cocaine hydrochloride as the same or different from methyl benzoate.
Waggoner, L. P.; Johnston, James M.; Williams, Marc; Jackson, Jan; Jones, Meredith; Boussom, Teresa; Petrousky, James A.
Synthesis and insecticidal activity of novel hydrazone compounds derived from a naturally occurring lignan podophyllotoxin against Mythimna separata (Walker).
In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, a series of novel hydrazone derivatives of podophyllotoxin, which is a naturally occurring aryltetralin lignan and isolated as the main secondary metabolite from the roots and rhizomes of Podophyllum species, were synthesized and evaluated as insecticidal agents against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in vivo at 1mg/mL. Especially compounds 8i, 8j, 8t, and 8u showed the more potent insecticidal activity with the final mortality rates greater than 60%. PMID:24810569
Wang, Yi; Yu, Xiang; Zhi, Xiaoyan; Xiao, Xiao; Yang, Chun; Xu, Hui
Synthesis and absorption and luminescence spectral properties of 3-formyl and 3-acetyl-7- (diethylamino) coumarin hydrazones
Various substitued coumarins are of interest as organic luminphors, many of which are effective laser dyes for the blue-green region of the spectrum. This paper attempts to extend the range of fluorescent coumarin dyes by synthesizing and investigating substitued hydrazones of 3-formyl- and 3-acetyl-coumarins (III). The absorption and luminescence spectral properties of the coumarins synthesized are discussed. Some lowering of the quantum yield of fluorescence in comparison with known coumarins is explained by the nonradiative degradation of the energy of electron excitation, which competes with the fluorescence.
Komlev, I.V.; Khrolova, O.R.; Mikhailova, T.A.; Tavrizova, M.A.
Reversible photochromic system based on rhodamine B salicylaldehyde hydrazone metal complex.
Photochromic molecules are widely applied in chemistry, physics, biology, and materials science. Although a few photochromic systems have been developed before, their applications are still limited by complicated synthesis, low fatigue resistance, or incomplete light conversion. Rhodamine is a class of dyes with excellent optical properties including long-wavelength absorption, large absorption coefficient, and high photostability in its ring-open form. It is an ideal chromophore for the development of new photochromic systems. However, known photochromic rhodamine derivatives, such as amides, exhibit only millisecond lifetimes in their colored ring-open forms, making their application very limited and difficult. In this work, rhodamine B salicylaldehyde hydrazone metal complex was found to undergo intramolecular ring-open reactions upon UV irradiation, which led to a distinct color and fluorescence change both in solution and in solid matrix. The complex showed good fatigue resistance for the reversible photochromism and long lifetime for the ring-open state. Interestingly, the thermal bleaching rate was tunable by using different metal ions, temperatures, solvents, and chemical substitutions. It was proposed that UV light promoted isomerization of the rhodamine B derivative from enol-form to keto-form, which induced ring-opening of the rhodamine spirolactam in the complex to generate color. The photochromic system was successfully applied for photoprinting and UV strength measurement in the solid state. As compared to other reported photochromic molecules, the system in this study has its advantages of facile synthesis and tunable thermal bleaching rate, and also provides new insights into the development of photochromic materials based on metal complex and spirolactam-containing dyes. PMID:24397593
Li, Kai; Xiang, Yu; Wang, Xiaoyan; Li, Ji; Hu, Rongrong; Tong, Aijun; Tang, Ben Zhong
Ligational, analytical and biological applications on oxalyl bis(3,4-dihydroxybenzylidene) hydrazone
The molecular modeling and parameters have been calculated to confirm the geometry of oxalyl bis(3,4-dihydroxybenzylidene) hydrazone, H 6L. The metal complexes of Cr 3+, VO 2+, ZrO 2+, HfO 2+, UO 22+ and MoO 22+ with H 6L have been prepared and characterized by partial elemental analysis, spectral studies (electronic; IR), thermal analysis and magnetic measurements. The data suggest the formation of polymer complexes with a unit [Cr(H 4L)(H 2O) 3Cl]·H 2O, [VO(H 4L)(H 2O) 2], [Hf(H 4L)(H 2O)]·H 2O [UO 2(H 4L)(H 2O) 2]·2H 2O [MoO 2(H 4L)] and [(ZrO) 2(H 2L)-(C 2H 5OH) 2]. The ligand behaves as a dibasic bidentate in all complexes except ZrO 2+ which acts as a tetrabasic tetradentate with the two ZrO 2+ ions. An octahedral geometry was proposed for the Cr 3+, HfO 2+, MoO 22+and UO 22+ complexes and square pyramid for VO 2+. The Cr 3+ is necessary to degrade the DNA of eukaryotic subject completely; the other complexes have little effect. H 6L was found suitable as a new reagent for the separation and preconcentration of ZrO 2+ ions from different water samples using flotation technique with satisfactory results.
El-Asmy, Ahmed A.; El-Gammal, O. A.; Radwan, H. A.; Ghazy, S. E.
The use of tiletamine hydrochloride and zolazepam hydrochloride for sedation of the mountain brushtial possum, Trichosurus caninus Ogilby (Phalangeridae: Marsupialia).
A combination of tiletamine hydrochloride and zolazepam hydrochloride in a 1:1 ration by weight was used successfully to sedate mountain brushtail possums, Trichosurus caninus, in the field. A standard total dose of 50 to 60 mg provided adequate sedation for the completion of a range of handling procedures. We describe the induction time, dose rate and side-effects associated with the use of tiletamine and zolazepam in T caninus. PMID:8526814
Viggers, K L; Lindenmayer, D B
A Post Hoc Analysis of D-Threo-Methylphenidate Hydrochloride (Focalin) Versus D,l-Threo-Methylphenidate Hydrochloride (Ritalin)
ERIC Educational Resources Information Center
Objective: To evaluate clinical measures of the benefit/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH). Method: Data from a phase III clinical trial was used to compare equimolar doses of d-MPH and d,l-MPH treatment for…
Weiss, Margaret; Wasdell, Michael; Patin, John
In vitro antifungal activity of naftifine hydrochloride against dermatophytes.
The incidence of superficial dermatophytoses is high in developed countries, and there remains a need for effective topical antifungals. In this study, we evaluated the in vitro antifungal activity of naftifine hydrochloride, the active ingredient in naftifine hydrochloride cream and gel 1% and 2%, against dermatophytes. The MICs and minimum fungicidal concentrations (MFCs) of naftifine hydrochloride against 350 clinical strains, including Trichophyton rubrum, T. mentagrophytes, T. tonsurans, Epidermophyton floccosum, and Microsporum canis, were determined using the CLSI methodology. Subsets from this test panel were subsequently tested in a time-kill assay at 0.125×, 0.25×, 0.5×, and 1× the MFC for each isolate. CFU counts were performed over a period of 48 h of incubation. Additionally, in order to determine the potential for resistance development, six strains were subjected to 15 serial passages in concentrations higher than the MIC for each strain. MICs were determined following each passage. The MIC range against the dermatophyte isolates tested was 0.015 to 1.0 ?g/ml, with naftifine hydrochloride being fungicidal against 85% of the Trichophyton species. The time-kill assay showed dose-dependent activity, with the greatest reduction in the numbers of CFU corresponding to the highest drug concentration. There was no increase in MIC for any strains following repeated exposure to naftifine hydrochloride. Naftifine hydrochloride demonstrated potent activity against all dermatophytes tested, and none of the isolates within this test panel demonstrated the potential for the development of resistance. Thus, future clinical studies of naftifine hydrochloride against dermatophytes may be warranted for the treatment of superficial dermatophytoses. PMID:23817365
Ghannoum, M; Isham, N; Verma, A; Plaum, S; Fleischer, A; Hardas, B
Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit
A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs.
de Melo, Thais Regina Ferreira; Chelucci, Rafael Consolin; Pires, Maria Elisa Lopes; Dutra, Luiz Antonio; Barbieri, Karina Pereira; Bosquesi, Priscila Longhin; Trossini, Gustavo Henrique Goulart; Chung, Man Chin; dos Santos, Jean Leandro
Submicron Organic Matter in a Peri-alpine, Ultra-oligotrphic Lake
Combining organic carbon (OC) measurements with the classic MBTH (3-methyl-2-benzothiazolinone hydrochloride) method for carbohydrate determination and a new voltammetric method for the determination of refractory organic matter (ROM) made it possible, for the first time, to quantify the types, sources and fate of submicron organic matter present in an ultra-oligotrophic lake (Lake Brienz, Switzerland). The lake is extremely rich in suspended glacial flour in summer (glacier melting season). Measurements were taken from June 2004 to October 2005 from 1.2 {mu}m filtered samples. OC concentration remained extremely low throughout the year (below 1 mg C L{sup -1}). MBTH carbohydrate concentration was very low in the lake (0.06-0.43 mg C L{sup -1}) and in the two tributary rivers (0.06-0.25 mg C L{sup -1}). Lake carbohydrate concentration only correlated with phytoplanktonic biomass at the onset of the productivity period. The results suggest that differences in MBTH concentration may sometimes reflect differences in the nature of the carbohydrates rather than differences in carbon concentration. Extensive fibril formation was evidenced by transmission electron microscopy (TEM) observations. ROM concentration in the lake was also very low (0.1-0.2 mg C L{sup -1}). Significant variation in ROM riverine input was due to either annual occurrences (snow melting) or irregular episodes (floods). Melting snow was responsible for about 30% of the lake's annual ROM input. One box mass balance calculations showed that about 25% of ROM was lost within the lake. Evidence gleaned from TEM and STXM (scanning transmission X-ray microscopy) observations clearly indicates that this is mainly caused by ROM sedimentation after association with inorganic colloids.
Chanudet,V.; Filella, M.
The iron chelator pyridoxal isonicotinoyl hydrazone (PIH) and its analogues prevent damage to 2-deoxyribose mediated by ferric iron plus ascorbate
Iron chelating agents are essential for treating iron overload in diseases such as ?-thalassemia and are potentially useful for therapy in non-iron overload conditions, including free radical mediated tissue injury. Deferoxamine (DFO), the only drug available for iron chelation therapy, has a number of disadvantages (e.g., lack of intestinal absorption and high cost). The tridentate chelator pyridoxal isonicotinoyl hydrazone (PIH)
Marcelo Hermes-Lima; Prem Ponka; Herbert M. Schulman
Synthesis of o-(Dimethylamino)aryl Ketones, Acridones, Acridinium Salts, and 1H-Indazoles by the Reaction of Hydrazones and Arynes
A novel, efficient route to biologically and pharmaceutically important o-(dimethylamino)aryl ketones, acridones, acridinium salts, and 1H-indazoles has been developed starting from readily available hydrazones of aldehydes and o-(trimethylsilyl)aryl triflates. The reaction proceeds through arynes under mild conditions, tolerates a wide range of functional groups, and provides the final products in good to excellent yields.
Dubrovskiy, Anton V.; Larock, Richard C.
In vivo iontophoretic administration of ropinirole hydrochloride.
This work explores the possibility of achieving therapeutic levels of the anti-Parkinsonian drug, ropinirole hydrochloride (RHCl), by transdermal iontophoretic delivery. An in vivo study was performed in hairless rats during which RH(+) was delivered at one current intensity (0.58 mA identical with 0.12 mA/cm(2)) and at three different drug concentrations (25, 125, and 250 mM). In vivo RH(+) flux and transport number were deduced from the steady-state plasma concentration values. Plasma concentration profiles and RH(+) transport numbers were independent of the drug donor concentration. The average iontophoretic input rate was about 3 micromol/h. Postiontophoresis transepidermal water loss (TEWL) was monitored and biopsies were histologically examined to identify any effects of iontophoresis on the skin. TEWL was elevated only at the anodal sites. TEWL recovery was faster for the "no-drug" control anodal sites, which suggests a combined effect of the drug and current on the skin. In conclusion, (1). the in vivo iontophoretic transport of RH(+) is independent of the drug donor concentration, and (2). iontophoresis can deliver therapeutic amounts of RH(+). PMID:14603489
Luzardo-Alvarez, Asteria; Delgado-Charro, M Begońa; Blanco-Méndez, José
Ticlopidine hydrochloride use and threatened stroke.
Ticlopidine hydrochloride is an antiplatelet agent of proven antithrombotic efficacy that in December 1991 became available for general clinical use in the United States. The relative value of ticlopidine compared with aspirin, also an effective antiplatelet agent, has become a key clinical issue. Whereas ticlopidine is somewhat more effective than aspirin for preventing stroke in certain populations, it is also more expensive and potentially toxic. We recommend its use for patients with threatened stroke who are intolerant of aspirin and for patients who have cerebral ischemic symptoms despite aspirin therapy. Patients surviving major ischemic stroke make up a third group for whom ticlopidine use may be recommended in preference to aspirin. The use of ticlopidine rather than aspirin in patients with other cerebrovascular conditions is not strongly supported by existing data. The risk-benefit-cost equation involving ticlopidine versus other antithrombotic therapies is complex, rendering a wide range of acceptable management practices. If reliable laboratory monitoring for neutropenia during the first 3 months of therapy is not feasible, ticlopidine should not be used.
Rothrock, J F; Hart, R G
78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...
...Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release...has determined that METADATE ER (methylphenidate hydrochloride (HCl)) extended-release...new drug applications (ANDAs) for methylphenidate HCl extended-release tablet,...
40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.
...2013-07-01 2013-07-01 false Phenol, 5-amino-2,4-dicholoro-, hydrochloride...Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride...The chemical substance identified as phenol,...
Inhibition of uptake1 by dopexamine hydrochloride in vitro.
1 Dopexamine hydrochloride, a compound under evaluation for the acute treatment of heart failure, was examined in vitro for its ability to prevent neuronal uptake of noradrenaline. 2 Despite possessing only weak beta 1-adrenoceptor agonist activity in paced guinea-pig left atria, dopexamine hydrochloride was only 23 times less potent than isoprenaline in augmenting responses of field-stimulated atrial preparations. 3 This potent effect was not observed in field-stimulated atria depleted of noradrenaline by reserpine and in the presence of cocaine was greatly reduced (1 microM) or abolished (50 microM). 4 Dopexamine hydrochloride (3 microM) potentiated the inotropic effect of exogenous noradrenaline in paced atria, thereby resembling cocaine (10 microM) and dopamine (30 microM), both of which are known inhibitors of Uptake. 5 The sodium-dependent uptake of [3H]-noradrenaline into rabbit brain synaptosomes was prevented by dopexamine hydrochloride (IC50 26 nM) and cocaine (IC50 108 nM), as well as by two other catecholamines used in the treatment of heart failure, dopamine (IC50 270 nM) and dobutamine (IC50 380 nM). 6 The cardiac stimulant effect of dopexamine hydrochloride reported in dogs and in patients with heart failure, may therefore be due in part to potentiation of endogenous catecholamines.
Mitchell, P. D.; Smith, G. W.; Wells, E.; West, P. A.
Extensive in vitro activity of guanidine hydrochloride polymer analogs against antibiotics-resistant clinically isolated strains
Polyhexamethylene guanidine hydrochloride (PHMG) possesses great potential in the development of covalently bound permanent sterile-surface materials for hospital infection control. This study aimed at evaluating the extensive activity of PHMG and its three novel analogs, including polybutamethylene guanidine hydrochloride, polyoctamethylene guanidine hydrochloride (POMG) and poly(m-xylylene guanidine hydrochloride), against 370 clinical strains, especially 96 isolates of which were antibiotics-resistant. Their in
Zhongxin Zhou; Dafu Wei; Yong Guan; Anna Zheng; Jian-Jiang Zhong
21 CFR 520.1242c - Levamisole hydrochloride and piperazine dihydrochloride.
...2009-04-01 2009-04-01 false Levamisole hydrochloride and piperazine dihydrochloride...FORM NEW ANIMAL DRUGS § 520.1242c Levamisole hydrochloride and piperazine dihydrochloride...contains in each fluid ounce 0.36 gram of levamisole hydrochloride and piperazine...
21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.
...2010-04-01 2010-04-01 false Tetracycline hydrochloride and sodium novobiocin...NEW ANIMAL DRUGS § 520.2345g Tetracycline hydrochloride and sodium novobiocin...contains the equivalent of 60 milligrams of tetracycline hydrochloride and 60 milligrams...
...2009-04-01 2009-04-01 false Tetracycline hydrochloride and sodium novobiocin...NEW ANIMAL DRUGS § 520.2345g Tetracycline hydrochloride and sodium novobiocin...contains the equivalent of 60 milligrams of tetracycline hydrochloride and 60 milligrams...
Measurement of pseudoephedrine hydrochloride dissolution using chloride-ion electrode.
Experiments were performed to determine the suitability of using a chloride-ion electrode for the measurement of pseudoephedrine hydrochloride dissolution from commercially available compressed tablets. Dissolution experiments were carried out in 500 ml of distilled water using the USP paddle method at 100 rpm. Both chloride ion and pseudoephedrine (UV spectrophotometry) were measured at six different sampling times. Percent dissolved versus time values were linearized on a log-normal probability basis. The slopes of individual lines obtained from the chloride and pseudoephedrine measurements were compared using a Student t test and did not differ significantly (t = 0.415, df = 5, p greater than 0.05). In addition to providing an efficient, inexpensive, and simple method for measuring pseudoephedrine hydrochloride dissolution rates, the chloride-ion electrode could be used in the measurement of dissolution rates for a wide variety of drugs available as hydrochloride salts. PMID:7299681
Chen, S T; Thompson, R C; Poust, R I
Polymorphism and a metastable solvate of duloxetine hydrochloride.
Duloxetine hydrochloride (1) is an important antidepressant that acts as a serotonin and noradrenaline reuptake inhibitor that has only recently been characterized by single-crystal X-ray diffraction. This study describes an investigation into polymorphism of duloxetine hydrochloride, discusses the challenges of characterizing new structures, and reports a new metastable solvate (1(acetone)) where acetone is trapped in a duloxetine hydrochloride host lattice. In view of the importance of formulation processing and bioavailability characteristics of the crystalline forms of 1, a comprehensive structural study of 1(acetone) was carried out using single-crystal and powder X-ray diffraction, infrared and Raman spectroscopies, and solid-state NMR spectroscopy. The rapid desolvation from 1(acetone) to the stable unsolvated form was investigated, and the structures of free and solvated forms are discussed in terms of the noncovalent intermolecular interactions. PMID:22050389
Marjo, Christopher E; Bhadbhade, Mohan; Hook, James M; Rich, Anne M
[Preparation and in vitro permeation of tetramethylpyrazine hydrochloride transdermal gel].
The purpose of this study was to prepare tetramethylpyrazine hydrochloride transdermal gel and to study its permeation ability in vitro. The skin permeation ability was evaluated by Valian-Chien permeation cells with isolated rat skin. The concentration of tetramethylpyrazine in samples was determined by HPLC. The optimal formulation was composed with 5% azone, 5% peppermint oil, 8% sodium carboxymethylcellulose and 8% tetramethylpyrazine hydrochloride. The accumulative permeation amount of the gel was (6 731.87 +/- 102.31) microg x cm(-2) in 12 h,and the permeation rate was (535.02 +/- 33.89) microg x cm(-2) x h(-1). The release profile in vitro was in line with zero-order formulation. Tetramethylpyrazine hydrochloride gel prepared in the study would be developed as a novel transdermal preparation. PMID:24079234
Tang, Zhan; Xu, Hong-Yan; Wang, Qiao
Colestipol hydrochloride prophylaxis of diarrhea during pelvic radiotherapy
Thirty-three patients were randomized prior to pelvic radiotherapy to receive the bile acid-sequestering resin colestipol hydrochloride, 5 grams qid, during the entire time of their therapy or diphenoxylate hydrochloride and atropine sulfate 2.5-20 mg per day (control) if they experienced diarrhea. The colestipol patients also took diphenoxylate if they had diarrhea. The patients in the colestipol group often experienced nausea, vomiting, and abdominal cramps and 8 were forced to discontinue the drug. There was no difference in the weekly stool frequency between the colestipol and the control patients but the colestipol patients who took at least 50% of the prescribed dose required fewer diphenoxylate tablets than the controls. The data suggest that colestipol hydrochloride is not of value in preventing radiation-induced diarrhea because of the side effects associated with the drug, but the theory on which the use of bile acid-sequestering agents is based may be correct.
Stryker, J.A.; Chung, C.K.; Layser, J.D.
Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride
Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a ? 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.
Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei
Propranolol hydrochloride release behaviour of crosslinked chitosan membranes.
Chitosan membranes of 20 microns thickness were prepared by a solvent evaporation technique and crosslinked with different concentrations of glutaraldehyde to obtain membranes of various degrees of crosslinking. These membranes were characterized by thermogravimetric (TG) analysis, differential scanning calorimetry (DSC) and tensile strength studies. The effect of crosslinking on the permeability of membranes to propranolol hydrochloride was evaluated by permeation studies conducted in static glass diffusion cells. A decrease in the thermal stability of chitosan membranes due to crosslinking was observed. The tensile strength of the membranes was improved by crosslinking. The introduction of crosslink points within the membrane reduced its permeability to propranolol hydrochloride as evidenced by decreased permeability and diffusion coefficients. Permeability studies revealed the operation of a pore mechanism in the transport of hydrophilic agents such as propranolol hydrochloride through chitosan and crosslinked chitosan membranes. PMID:7764115
Thacharodi, D; Rao, K P
Mucoadhesive bilayer tablets of propranolol hydrochloride.
The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling index, in vitro drug release, ex vivo drug permeation, ex vivo mucoadhesion, and in vivo pharmacodynamics in rabbits. Tablets containing Na-alginate and CP in the ratio of 5:1 (F2) had the maximum percentage of in vitro drug release without disintegration in 12 hours. The swelling index was proportional to Na-alginate content and inversely proportional to CP content. The surface pH of all tablets was found to be satisfactory (7.0 +/- 1.5), close to neutral pH; hence, buccal cavity irritation should not occur with these tablets. The mechanism of drug release was found to be non-Fickian diffusion and followed zero-order kinetics. The formulation F4 was optimized based on good bioadhesive strength (28.9 +/- 0.99 g) and sustained in vitro drug permeation (68.65% +/- 3.69% for 12 hours). The behavior of formulation F4 was examined in human saliva, and both the drug and the buccal tablet were found to be stable. The formulation F4 was applied to rabbit oral mucosa for in vivo studies. The formulation inhibited isoprenaline-induced tachycardia. The studies conducted in rabbits confirmed the sustained release as compared with intravenous administration. PMID:17915827
Patel, Vishnu M; Prajapati, Bhupendra G; Patel, Harsha V; Patel, Karshanbhi M
Stability of procainamide hydrochloride in neutralized 5% dextrose injection.
The stability of procainamide hydrochloride in neutralized 5% dextrose injection was studied. Sixty-four admixtures were prepared by adding either 2 mL (for 0.4% admixtures) or 4 mL (for 0.8% admixtures) of procainamide hydrochloride to 250 mL of 5% dextrose injection in plastic containers. The pH of 32 of these admixtures (16 of each type) was adjusted to 7.5. These 32 admixtures represented the neutralized group, and the remaining 32 represented the control group. The admixtures were stored at either 23-25 degrees C (room temperature) or 5 degrees C (refrigeration) for 24 hours. Procainamide hydrochloride concentrations in each sample were determined by high-performance liquid chromatography immediately after the admixtures were prepared and at various intervals during storage. Procainamide concentrations decreased over time in 5% dextrose injection. The decrease was significantly less for admixtures in neutralized 5% dextrose injection, those stored under refrigeration, and those with an 0.8% concentration of drug. Decreases in procainamide hydrochloride concentrations in the control admixtures might have been caused by procainamide-dextrose complexation. Initial concentrations of procainamide hydrochloride in 5% dextrose injection can be adequately maintained over a 24-hour storage period by neutralizing the 5% dextrose injection or storing the admixture at 5 degrees C. However, because it is impractical to maintain the necessary temperature condition during a 24-hour infusion, neutralization might be the most viable alternative when extended stability of procainamide hydrochloride in 5% dextrose injection is required. PMID:3228104
Raymond, G G; Reed, M T; Teagarden, J R; Story, K; Geberbauer, C W
Stability of ondansetron hydrochloride and 12 medications in plastic syringes.
The stability and compatibility of ondansetron hydrochloride with neostigmine methylsulfate, naloxone hydrochloride, midazolam hydrochloride, fentanyl citrate, alfentanil hydrochloride, atropine sulfate, morphine sulfate, meperidine hydrochloride, propofol, droperidol, metoclopramide monohydrochloride, and glycopyrrolate were studied. Ondansetron 1.33 or 1.0 mg/mL was combined with 0.9% sodium chloride injection and each of the 12 drugs in duplicate in plastic syringes (or glass for propofol). The syringes were stored at 21.8-23.4 or 4 degrees C in the dark, except for those containing propofol, which were stored at ambient temperature. Samples were removed at 0, 4, 8, and 24 hours for analysis by high-performance liquid chromatography and pH measurement; the propofol-containing samples were removed at 0, 1, 2, and 4 hours. Syringes were visually assessed for color and clarity, and particulate content was measured with a particle counter at the end of the study period. All solutions containing ondansetron retained more than 90% of their initial ondansetron concentration. Solutions containing each of the other drugs except droperidol retained more than 90% of their initial concentration of these drugs. The solutions containing droperidol retained more than 90% of their initial droperidol concentration for up to eight hours at ambient temperature but precipitated quickly at 4 degrees C. In combinations of ondansetron 1.33 or 1.0 mg/mL and 10 of 12 drugs, all drugs were stable for 24 hours in plastic syringes at 23 and 4 degrees C; ondansetron hydrochloride 1.0 mg/mL and propofol 1.0 and 5.0 mg/mL in admixtures were stable for 4 hours, and droperidol on its own and combined with ondansetron 1.0 mg/mL was stable for no more than 8 hours at ambient temperature. PMID:9872702
Stewart, J T; Warren, F W; King, D T; Venkateshwaran, T G; Fox, J L
Modified cobalt thiocyanate presumptive color test for ketamine hydrochloride.
A new presumptive color test for ketamine hydrochloride is reported. The test is a modification of the cobalt thiocyanate test currently used for cocaine and involves basifying samples rather than acidifying them. The two-step procedure for liquids and three-step procedure for powdered samples are straightforward, definitive, and utilize reagents commonly used in forensic drug analysis. The test works on ketamine hydrochloride in both powder and liquid form and has a sensitivity of c. 1.25 mg. Performing the test with numerous other controlled substances and related chemicals demonstrates the test to be highly selective. PMID:17209915
Morris, Jeremiah A
Antifungal activity of hydrochloride salts of tylophorinidine and tylophorinine.
The antimicrobial efficacy of two phenanthroindolizidine alkaloids, tylophorinidine hydrochloride (TdnH) and tylophorinine hydrochloride (TnnH), isolated from the plant Tylophora indica (local name, Antamul) was evaluated. These were screened for in vitro antifungal and antibacterial activities. Both compounds exhibited potent antifungal activity displaying minimum inhibitory concentrations (MIC) in the range of 2-4 microg/mL for TdnH and 0.6-2.5 microg/mL for TnnH against Candida species. PMID:23074899
Dhiman, Mini; Parab, Rajashri R; Manju, Sreedharannair L; Desai, Dattatraya C; Mahajan, Girish B
Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories.
A visible spectrophotometric method has been developed for the quantitation of aminacrine hydrochloride in creams, jellies, and suppositories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum was recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbances of the minima at about 389 and 412 nm. Aminacrine and a trace contaminant, 9(10H)-acridone, were independently identified by different thin layer chromatographic systems. PMID:6826500
Bunch, E A
Design and synthesis of a new class of 4-aminoquinolinyl- and 9-anilinoacridinyl schiff base hydrazones as potent antimalarial agents.
A series of novel 4-aminoquinolinyl and 9-anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated in vitro for their antimalarial activity against chloroquine-sensitive strain 3D7 and the chloroquine-resistant K1 strain of Plasmodium falciparum and for cytotoxicity toward Vero cells. Compounds 17, 20, and 21 displayed good activity against the 3D7 strain with IC50 values ranging from 19.69 to 25.38 nm. Moreover, compounds 16, 17, 21, 24, 32, and 33 exhibited excellent activities (21.64-54.26 nm) against K1 strain and several compounds displayed ?-hematin inhibitory activity, suggesting that they act on the heme crystallization process such as CQ. Compounds were also found to be non-toxic with good selectivity index. PMID:24444074
Sharma, Moni; Chauhan, Kuldeep; Srivastava, Rajeev K; Singh, Shiv V; Srivastava, Kumkum; Saxena, Jitendra K; Puri, Sunil K; Chauhan, Prem M S
Synthesis and Structural Characterization of a Nickel(II) Complex with Unsymmetrical NNO-Donor Schiff Base like Hydrazone Ligand
\\u000a Abstract The nickel(II) complex Ni[C5H4N–C(CH3)=N–N=C(O)–C6H5]2 (1), containing the potentially tridentate Schiff base like hydrazone ligand (LH) which is the 1:1 condensation product of benzhydrazide\\u000a and 2-acetylpyridine, was prepared and characterized by IR and UV–Vis spectra, thermal analysis and single crystal X-ray diffraction\\u000a measurements. Structural investigation shows that the molecule prefers a monoclinic lattice, having space group Cc, a = 10.248(6), b = 19.692(11), c = 12.281(7) Ĺ,
Amitabha Datta; Nien-Tsu Chuang; Jui-Hsien Huang
Control and analysis of hydrazine, hydrazides and hydrazones--genotoxic impurities in active pharmaceutical ingredients (APIs) and drug products.
This is the latest of a series of reviews focused on the analysis of genotoxic impurities. This review summarises the analytical approaches reported in the literature relating to hydrazine, hydrazines, hydrazides and hydrazones. It is intended to provide guidance for analysts needing to develop procedures to control such impurities, particularly where this is due to concerns relating to their potential genotoxicity. Of particular note is the wide variety of techniques employed, both chromatographic and spectroscopic, with most involving derivatisation. Such a wide variety of options allow the analyst a real choice in terms of selecting the most appropriate technique specific to their requirements. Several generic methodologies, covering the three main analytical approaches; i.e. HPLC (high performance liquid chromatography), GC (gas chromatography) and IC (ion chromatography), are also described. PMID:21145684
Elder, D P; Snodin, D; Teasdale, A
Stereoselective Alkylations of Chiral Nitro Imine and Nitro Hydrazone Dianions. Synthesis of Enantiomerically Enriched 3-Substituted 1-Nitrocyclohexenes†
Dianions of chiral nitro imines (generated by a combination of LDA and s-BuLi) underwent diastereoselective alkylation with methyl, butyl, isopropyl, allyl and methallyl iodides. In contrast to the behavior of simple metalloenamines, the most selective auxiliary contained no coordinating groups, but did possess a large steric difference between the two substituents. The yield and selectivity of the alkylations were improved by the addition of HMPA or DMPU. The use of (S)-1-naphthylethylamine as the auxiliary afforded the R absolute configuration of the alkylation products. This stereochemical outcome could be rationalized by simple steric approach controlled alkylation in a conformationally fixed, internally coordinated dianion. A SAMP nitro hydrazone gave poorer yields and selectivities.
Denmark, Scott E.; Ares, Jeffrey J.
Anticancer phytochemical analogs 37: synthesis, characterization, molecular docking and cytotoxicity of novel plumbagin hydrazones against breast cancer cells.
We have synthesized, structurally characterized and examined cytotoxicity of novel plumbagin hydrazones against estrogen and progesterone receptor positive (ER+/PR+) MCF-7 and triple negative MDA-MB-231 breast cancer cell lines in order to evaluate the potential of these novel phytochemical analogs. Compounds were docked into the protein cavity of p50-subunit of NF-?B protein revealing better fit and better binding energies than the parent plumbagin compound. This was also reflected in their superior cytotoxicities which were found to be mediated by inhibition of NF-?B expression. These compounds can provide a starting point for the development of novel drug molecules against triple negative breast cancers. PMID:24835626
Dandawate, Prasad; Ahmad, Aamir; Deshpande, Jyoti; Swamy, K Venkateswara; Khan, Ejazuddin M; Khetmalas, Madhukar; Padhye, Subhash; Sarkar, Fazlul
Amides and Hydrazides from Amine and Hydrazine Hydrochlorides.
This safe and efficient procedure for the synthesis of N-substituted amides and hydrazides is a modification of the Schotten-Bausmann procedure in which the amine or hydrazide is replaced by the corresponding hydrochloride salt, and the use of alkali is eliminated. (Author/BB)
Shama, Sami A.; Tran, Thuan L.
Preparation and in vitro evaluation of suppositories of halofantrine hydrochloride
Halofantrine (HF) hydrochloride is commercially available only as oral dosage forms. Limitations of oral dosing of the drug coupled with non-availability of the safe parenteral preparations prompted the need to develop and evaluate suppository HF formulations, which may serve as a practical alternative. The effects of type of suppository base and incorporation of non ionic surfactants on in vitro release
F. A. Oladimeji; S. I. Omoruyi; C. O. Onyeji
In Vitro Release of Propranolol Hydrochloride from Topical Vehicles
Transdermal drug delivery is becoming increasingly important and for this reason it is clear that academia must ensure that current graduates are knowledgeable in all facets of topical drug administration. An in vitro diffusion cell experiment was designed to demonstrate the rate of release of propranolol hydrochloride (PHC) from three different topical vehicles: (I) an oil-in-water cream; (if) a gel;
Eric W. Smith; J. M. Haigh
Polymorphic changes of thiamine hydrochloride during granulation and tableting.
Thiamine hydrochloride was granulated using an instrumented fluidized bed granulator (Hüttlin HKC 05-TJ). Granules consisting of pure thiamine hydrochloride were produced using an aqueous solution of thiamine hydrochloride as the granulating liquid. The effects of process variables such as inlet air temperature, spray rate, and amount of granulating liquid on granule properties are described. Particle size distributions of granules depended mainly on the amount of granulating liquid sprayed into the powder bed. Granules were tableted on a rotary tablet press at four different compression forces. Crushing strengths and disintegration times of all tablets were found to be very low after manufacture, but increased considerably after 4 months of storage at room temperature. Granular materials showed "caking" under the same storage conditions. These changes could be attributed to alterations of the polymorphic form of thiamine hydrochloride. The water-free form, being present directly after granulation, absorbs humidity very fast and is transformed into the monohydrate, which is stable at room temperature. Loss of water takes place during the drying phase of the granulation process and on storage of the substance at temperatures of 50 degrees C and 80 degrees C. During storage at room temperature while exposed to humidity, a transformation into the hemihydrate was observed. This polymorph is transformed during thermal analysis at about 190 degrees C to a water-free form that is stable at higher temperatures. PMID:11548854
Wöstheinrich, K; Schmidt, P C
[Experimental Prototheca mastitis in cattle and therapy with tetramisole hydrochloride].
In one cow all 4 quarters were infected with 2 x 10(8) germs of Prototheca zopfii each. 2 quarters of it were treated over 6 subsequent milking times with 20 ml Tetramisole hydrochloride (4 mg/kg body mass) in each case. Clinical symptoms diminished within 3-24 hours after the first application in comparison with the control quarters distinctly. Macroscopic alterations in the treated quarters could be found for a short time only, whereas they were evident in the control quarters for up to 2 days. The milk cell counts were raised til the 5. day p.i. The number of Prototheca excreted by treated quarters in each ml initial milk was reduced to 38% and in each ml end milk to 67% in comparison with the 2 control quarters. A more potent reduction of Prototheca can be expected after the application of Levamisole hydrochloride. At the future therapy applications after every milking time for at least 3 days with 25-40 ml of the preparations in each quarter are recommended. A total dose per animal and application time of 150 ml preparations (6 g Levamisole hydrochloride = 15 mg/kg body mass) must not be exceeded. Before Levamisole hydrochloride may be used for patients, susceptibility tests are necessary of the strains of Prototheca zopfii present and additional investigations for the reliability of the results hitherto obtained in one experimental Prototheca mastitis only. PMID:8216187
Bergmann, A
21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.
...level of 1 to 2 milligrams of ethylisobutrazine hydrochloride per pound of body weight to effect.1 1 These conditions are NAS/NRC reviewed and deemed effective. Applications for these uses need not include effectiveness data as specified by §...
Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values.
The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0?milligram (mg) per kg body weight and 2.0?mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P < 0.05) and mean corpuscular hemoglobin concentration (MCHC) (P < 0.05). The study might help to evaluate health profiles of sloth bears for appropriate line treatment. PMID:24876990
Veeraselvam, M; Sridhar, R; Perumal, P; Jayathangaraj, M G
Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values
The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0?milligram (mg) per kg body weight and 2.0?mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P < 0.05) and mean corpuscular hemoglobin concentration (MCHC) (P < 0.05). The study might help to evaluate health profiles of sloth bears for appropriate line treatment.
Veeraselvam, M.; Sridhar, R.; Perumal, P.; Jayathangaraj, M. G.
A Facile and Convenient Synthesis of some Novel Hydrazones, Schiff's Base and Pyrazoles Incorporating Thieno[2,3-b]thiophenes
A facile and convenient synthesis of some novel hydrazones, schiff's base and pyrazoles from thieno[2,3-b]thiophene derivatives 1 have been achieved in high yields assisted by microwave and classical methods. The structures of all the title compounds have been elucidated by elemental analysis, IR, MS, 1H-NMR and 13C-NMR. Generally, these findings represent a new class of sulfur and nitrogen moieties that should also be of interest as new materials.
Mabkhot, Yahia Nasser; Barakat, Assem; Al-Majid, Abdullah Mohammed; Al-Othman, Zeid Abdullah; Alamary, Abdullah Saleh
Mono and BiNuclear Metal Complexes of Schiff-Base Hydrazone (ONN) Derived from o-Hydroxyacetophenone and 2Amino4Hydrazino6Methyl Pyrimidine
A tridentate ONN donor Schiff-base hydrazone ligand, H2L, was synthesized by the condensation of 2-amino-4-hydrazino-6-methyl pyrimidine with o-hydroxyacetophenone. The structure of the ligand was elucidated by IR and H NMR spectra which indicated the presence of three different coordinating groups, the oxygen atom of the phenolic OH group, the nitrogen atom of the azomethine, C=N, group and one of the
Saied M. E. Khalil; H. S. Seleem; B. A. El-Shetary; M. Shebl
Hydrazone-based ligands for micro-solid phase extraction-high performance liquid chromatographic determination of biogenic amines in orange juice
Eight hydrazone-based ligands were synthesized, trapped in a silica sol–gel matrix, and were subsequently used in the micro-solid phase extraction (?-SPE) of biogenic amines (BAs). The BAs investigated were tryptamine, phenylethylamine, putrescine, histamine, tyramine and spermidine. Prior to the extraction, dansyl chloride was added to the samples which were heated to 70°C for 10min. The samples were extracted with ?-SPE,
Chanbasha Basheer; Weishan Wong; Ahmad Makahleh; Abdassalam Abdelhafiz Tameem; Abdussalam Salhin; Bahruddin Saad; Hian Kee Lee
Effects of zilpaterol hydrochloride and zilpaterol hydrochloride withdrawal time on beef carcass cutability, composition, and tenderness.
The impact of zilpaterol hydrochloride (ZH) on carcass yield, composition, and tenderness was evaluated using 384 beef steers in a randomized complete block design. Main effects were the addition of 0 or 8.3 mg/kg of ZH for the final 20 d of feeding and each inclusion level was paired with withdrawal periods of 3, 10, 17, or 24 d. The 2 animals with BW closest to the pen average were selected for carcass fabrication to determine carcass yield, composition, and tenderness. The carcasses from animals fed ZH had greater (P = 0.008) individual side weights. Carcass fat determinations were unchanged (P = 0.70) by ZH. Weights of the strip loin (P = 0.01), peeled tenderloin (P = 0.02), and top sirloin butt (P < 0.001) were all improved with ZH. When expressed as a proportion of carcass weight, ZH increased percentage of carcass in the top sirloin butt (P = 0.006), bottom sirloin tri-tip (P = 0.02), top inside round (P = 0.002), bottom round flat (P = 0.001), and flank steak (P = 0.02). A longer withdrawal time (WT) increased (P < 0.001) carcass weights. Shoulder clod weights were greatest (P < 0.001) with 17-d WT from ZH, whereas chuck roll weights were greatest (P = 0.02) at 17 and 24 d of WT. Peeled tenderloins, top sirloin butts, and eye of rounds responded to WT, with increased (P < 0.001) weights seen at 10 d of WT as compared with all other WT. Shear force values were greater at each of the 3 aging times, 7 d (P < 0.001), 14 d (P < 0.001), and 21 d (P = 0.003), in steaks from ZH-fed steers compared with control steers. Protein percentages were greater in ZH steaks (P = 0.03) and ZH ground beef trim (P < 0.001). Percent moisture was increased (P < 0.001) in strip loin steaks at 3 and 10 d WT. Ground beef trim had an increase (P = 0.04) in percent moisture and a decrease (P = 0.01) in percent fat at 10 d WT. Carcass weights and yields were improved with ZH feeding and may continue to improve even up to 10 d after withdrawal of the supplement. Tenderness was slightly reduced with ZH supplementation but was unaffected by WT. Zilpaterol hydrochloride can be a valuable supplement to finishing beef steers to improve carcass lean yields and composition. PMID:19684279
Shook, J N; VanOverbeke, D L; Kinman, L A; Krehbiel, C R; Holland, B P; Streeter, M N; Yates, D A; Hilton, G G
Synthesis and structural characterization of organotin(IV) compounds derived from the self-assembly of hydrazone Schiff base series and various alkyltin salts
Reactions of pyruvic acid hydrazone series [pyruvic acid thiophenecarbonyl hydrazone (L1), pyruvic acid 4-hydroxybenzoylhydrazone (L2), pyruvic acid salicyloylhydrazone (L3), pyruvic acid benzoylhydrazone (L4)], or salicylaldehyde hydrazone Schiff base ligand [salicylaldehyde isonicotinoylhydrazone (L5)] with different alkyltin salts result in six new organotin(IV) compounds, {(n-Bu)2Sn[2-SC4H3CON2C(CH3)CO2](HOC3H7-i)}2 (1), [{(n-Bu)2SnCl(O)(n-Bu)2 Sn(O)[C6H4CON2C(CH3)CO2]Sn(n-Bu)2(HOCH3)}2]? (2), {(o-ClBz)2Sn[4-HOC6H4CON2C(CH3) CO2] (HOC2H5)}2 (3), {(n-C8H17)2Sn[2-HOC6H4CON2C(CH3)CO2](H2O)}2 (4), {(n-Bu)2Sn[C6H5 CON2C(CH3)CO2][HOSn(n-Bu)3]}2 (5), and {[(n-C4H9)SnCl2]?[4-NHC5H4CON2CH (C6H4O-2)]+ (6),
Min Hong; Han-Dong Yin; Shao-Wen Chen; Da-Qi Wang
Evaluation of the efficacy of olapatadine hydrochloride 0.1% ophthalmic solution and azelastine hydrochloride 0.05% ophthalmic solution in the conjunctival allergen challenge model
Background: Olopatadine hydrochloride 0.1% ophthalmic solution and azelastine hydrochloride 0.05% ophthalmic solution are 2 topical antiallergic agents indicated for the treatment of itching of the eye associated with allergic conjunctivitis. Olopatadine has recently received US Food and Drug Administration (FDA) approval for an expanded indication for the treatment of signs and symptoms of allergic conjunctivitis, including itching, tearing, eyelid swelling,
Dennis L. Spangler; George Bensch; Gregg J. Berdy
Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure.
The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M(")(f) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across T(g). The situation is analogous to many non-ionic glass-formers showing the presence of the structural ?-relaxation together with the Johari-Goldstein (JG) ?-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary ?-conductivity relaxation and the secondary ?-conductivity relaxation, respectively. The analogy of the ?-conductivity relaxation in procaine HCl and procainamide HCl with JG ?-relaxation in non-ionic glass-formers goes further by the finding that the ?-conductivity is strongly related to the ?-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain ?-conductivity relaxation time constant, the data show invariance of the ratio between the ?- and the ?-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the ?-conductivity relaxation has fundamental importance and is indispensable as the precursor of the ?-conductivity relaxation, analogous to the relation found between the Johari-Goldstein ?-relaxation and the structural ?-relaxation in non-ionic glass-forming systems. The novel features of the ionic conductivity relaxation are brought out by presenting the measurements in terms of the electric modulus or permittivity. If presented in terms of conductivity, the novel features are lost. This warns against insisting that a log-log plot of conductivity vs. frequency is optimal to reveal and interpret the dynamics of ionic conductors. PMID:22559496
Wojnarowska, Z; Swiety-Pospiech, A; Grzybowska, K; Hawelek, L; Paluch, M; Ngai, K L
X-ray crystallographic, electrochemical and spectroscopic properties of 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate
In contrast to the reaction between di-2-pyridyl ketone with a variety of hydrazines or hydrazides in refluxing acidified alcoholic solution to form unprotonated di-2-pyridyl ketone hydrazones (dpkhydrazones), the reaction between di-2-pyridyl ketone and phenyl hydrazine hydrochloric acid under the same conditions gave unprecedented pyridyl protonated 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate, dpkphh·HCl·3H 2O. Crystals of dpkphh·HCl·3H 2O obtained from an ethanolic solution of dpkphh·HCl·3H 2O that contains a few drops of HCl are in the centric triclinic space group P-1. Structure analysis reveals non-coplanar dpkphh·H + along with a chloride anion and three water molecules. The molecules pack show infinite stacks of anti-parallel dpkphh·H + locked to the chloride anion and water molecules via novel fused hydrogen bonded oxygen-chloride four and six-membered cyclic rings propagating between the stacks. Electrochemical measurements on dpkphh·HCl·3H 2O in non-aqueous solvents show solvent dependence, single and multi-electronic transfers in DMF and in CH 3CN single electronic redox transfers. The reversibility of the second electronic reduction following the first irreversible electronic transfer hints to the stability of electrochemically generated intermediate following the sequential electronic transfers. In contrast to the optical behavior of a variety unprotonated and metal coordinated dpkhydrazones, protonation of one pyridine ring in dpkphh·HCl·3H 2O decreases the electron density on the pyridine ring ceases the intraligand charge transfer electronic transition and renders the protonated systems (dpkphh·HCl·3H 2O plus surrounding solvent molecules) insensitivity to their surroundings although the spectra show strong solvent-solute interactions. 1H NMR measurements on dpkphh·HCl·3H 2O in non-aqueous media reveal sensitivity to solvent and temperature variations that point to strong solvent-solute interactions. The amide and water protons show sensitivity to solvent and temperature variations higher than the aromatic protons consistent with their participation in non-covalent hydrogen bonds.
Bakir, Mohammed; Hassan, Ishmael; Johnson, Toni; Brown, Ordel; Green, Orville; Gyles, Colin; Coley, Michael D.
Preformed microcapsules for loading and sustained release of ciprofloxacin hydrochloride.
A novel pathway for ciprofloxacin hydrochloride delivery system based on spontaneous deposition mechanism was introduced with respect to encapsulation, quantitative drug loading and sustained release. Layer-by-layer assembly of oppositely charged polyelectrolytes onto melamine formaldehyde (MF) colloidal particles, followed by removal of the cores at low pH has yielded hollow microcapsules having a unique property to induce spontaneous deposition of various water-soluble substances. Observations under scanning electron microscopy, atomic force microscopy and transmission electron microscopy provided direct proofs of the spontaneous deposition. The quantitative drug loading and sustained release properties were elucidated. Results show that the loaded drug is proportional to drug feeding concentrations, temperature and salt concentrations, demonstrating tailorable deposition behavior that is crucial for the drug carrier. The deposited ciprofloxacin hydrochloride could be again released in a sustained manner and exhibited a significant antiseptic activity with high biocompatibility. PMID:15866345
Mao, Zhengwei; Ma, Lie; Gao, Changyou; Shen, Jiacong
14-Benzoyl-mesaconine hydro-chloride methanol monosolvate
The title compound, C31H44N3O10 +·Cl?·CH4O, is the methanol solvate of 8-benzoyloxy-,9,11,11a-tetrahydroxy-6,10,13-trimethoxy-3-methoxymethyl-1-methyltetradecahydro-1H-3,6a,12-(epiethane-1,1,2-triyl)-7,9-methanonaphtho[2,3-b]azocin-1-ium chloride, the amine-protonated hydrochloride of 14-benzoylmesaconine hydrochloride. The cation has an aconitine carbon skeleton with four six-membered rings of which three display chair conformations and one a boat conformation, and two five-membered rings with envelope conformations. In the crystal, the components are connected into an infinite chain by inter- and intramolecular O—H?O, N—H?O and O—H?Cl hydrogen bonds.
Mu, Yan; Li, Lin; Wei, Hai-Liu; Kuang, Tong-Chun; Hu, Song-Qing
Extractive spectrophotometric determination of TRODAT-1 hydrochloride in lyophilized kit.
A simple, sensitive, and accurate spectrophotometric method has been developed for the assay of TRODAT-1 hydrochloride in lyophilized kit. The method is based on the formation of ion-pair association complex of TRODAT-1 with bromothymol blue (BTB) in disodium hydrogen phosphate/citric acid buffer of pH 4.0. The colored product was extracted with chloroform, and measured spectrophotometrically at 414 nm. Beer's law was obeyed in the range of 5-25 microg/ml with molar absorptivity of 2.75 x 10(4) l/mol/cm. Optimization of experimental conditions was described for the method. The proposed method has been successfully applied for the analysis of TRODAT-1 hydrochloride in lyophilized kit. No interference with pharmaceutical excipients was observed. PMID:18819514
Li, X M; Chen, Z P; Wang, S P; Tang, J; Liu, C Y; Zou, M F
Disposable screen-printed sensors for determination of duloxetine hydrochloride.
A screen-printed disposable electrode system for the determination of duloxetine hydrochloride (DL) was developed using screen-printing technology. Homemade printing has been characterized and optimized on the basis of effects of the modifier and plasticizers. The fabricated bi-electrode potentiometric strip containing both working and reference electrodes was used as duloxetine hydrochloride sensor. The proposed sensors worked satisfactorily in the concentration range from 1.0 × 10-6-1.0 × 10-2 mol L-1 with detection limit reaching 5.0 × 10-7 mol L-1 and adequate shelf life of 6 months. The method is accurate, precise and economical. The proposed method has been applied successfully for the analysis of the drug in pure and in its dosage forms. In this method, there is no interference from any common pharmaceutical additives and diluents. Results of the analysis were validated statistically by recovery studies. PMID:22264225
Alarfaj, Nawal A; Ammar, Reda A; El-Tohamy, Maha F
Design and development of diltiazem hydrochloride transmucosal drug delivery system.
Diltiazem hydrochloride is an antihypertensive agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery. Diltiazem mucoadhesive buccal patches were prepared using HPMC, chitosan, PVP, PVA and carbopol. The physicochemical interactions between diltiazem and the polymers were investigated by FTIR and DSC, results revealed no interaction between drug and polymers. The patches were evaluated for various physicochemical parameters, in vitro release studies and ex vivo permeation through porcine buccal mucosa. Residual solvent content in patches was determined by gas chromatography and are largely below the tolerated limits. The formulations showed an extended release of the drug upto a period of 12 hours during ex vivo permeation and showed non Fickian drug release. Stability of the optimized formulation was investigated as per ICH guidelines and was found to be stable with respect to drug content and ex vivo permeation. Keywords: diltiazem hydrochloride buccal patches residual solvents mucoadhesion in vitro drug release ex vivo permeation. PMID:23578264
Penjuri, Subhash Chandra Bose; Damineni, Saritha; Ravouru, Nagaraju
Coadministration of colesevelam hydrochloride with atorvastatin lowers LDL cholesterol additively
Colesevelam hydrochloride is a novel, potent, non-absorbed lipid-lowering agent previously shown to reduce low density lipoprotein (LDL) cholesterol. To examine the efficacy and safety of coadministration of colesevelam and atorvastatin, administration of these agents alone or in combination was examined in a double-blind study of 94 hypercholesterolemic men and women (baseline LDL cholesterol ?160 mg\\/dl). After 4 weeks on the
Donald Hunninghake; William Insull Jr; Phillip Toth; David Davidson; Joanne M. Donovan; Steven K. Burke
Potentiometric Flow Injection Analysis of Drotaverine Hydrochloride in Pharmaceutical Preparations
Five poly (vinyl chloride) (PVC) membrane electrodes for the determination of drotaverine hydrochloride (DvCl) were constructed and fully characterized in terms of composition, life span, response time, usable pH range, working concentration range, and temperature. The membranes of these electrodes consist of drotaverinium?silicotungstate (Dv?ST), silicomolybdate (Dv?SM), phosphotungstate (Dv?PT), phosphomolybdate (Dv?PM), or tetraphenylborate (Dv?TPB) ion associations dispersed in PVC matrix with
Hosny Ibrahim; Yousry M. Issa
A validated UV spectrophotometric method for determination of duloxetine hydrochloride.
A simple, sensitive and accurate UV spectrophotometric method was developed for the assay of duloxetine hydrochloride in raw material and capsules. Validation of the method yielded good results concerning range, linearity, precision and accuracy. The absorbance was measured at 290 nm for duloxetine capsule solution. The linearity range was found to be 5-50 microg/mL for the drug. It was found that the excipients in the commercial formulation did not interfere with the methods. PMID:17663186
Kamila, M M; Mondal, N; Ghosh, L K
Nortriptyline hydrochloride skin absorption: Development of a transdermal patch
The influence of propylen glycol (PG), ethanol, and oleic acid (OA) on nortriptyline hydrochloride (NTH) penetration through human epidermis was studied in vitro at two different pH values (5.5 and 7.4). The influence of lactic acid and polysorbate 80 was studied for a pH of 5.5. Permeation studies through Heat Separated Epidermis, as well as the enhancing effect of the
Ana Melero; T. M. Garrigues; P. Almudever; A. Mart?´n Villodre; C. M. Lehr; U. Schäfer
Scalable synthesis of (1-cyclopropyl)cyclopropylamine hydrochloride
Summary 1-Cyclopropylcyclopropanecarboxylic acid (2), which is accessible on a large scale (900 mmol) from 1-bromo-1-cyclopropylcyclopropane (1) in 64% yield (89% on a 12.4 mmol scale), has been subjected to a Curtius degradation employing the Weinstock protocol to furnish the N-Boc-protected (1-cyclopropyl)cyclopropylamine 3 (76%). Deprotection of 3 with hydrogen chloride in diethyl ether gave the (1-cyclopropyl)cyclopropylamine hydrochloride (4·HCl) in 87% yield.
Khlebnikov, Alexander F; Kostikov, Rafael R; Yufit, Dmitrii S
Unfolding and inactivation of cutinases by AOT and guanidine hydrochloride
We present a comparative analysis of the unfolding and inactivation of three cutinases in the presence of guanidine hydrochloride (GdnHCl) and bis(2-ethylhexyl) sodium sulfosuccinate (AOT). Previous investigations have focused on the cutinase from Fusarium solani pisi (FsC). In addition to FsC, the present study includes the cutinase from Humicola insolens (HiC) and a mutant variant of HiC (?HiC) with increased
Tomas Ternström; Allan Svendsen; Mikael Akke; Patrick Adlercreutz
Stability of ondansetron hydrochloride injection in various beverages.
The stability of ondansetron hydrochloride injection in beverages likely to be acceptable to patients was studied. Ondansetron hydrochloride injection (containing ondansetron 2 mg/mL) was added to apple juice, fruit punch, cherry-flavored drink, carbonated soft drinks, and hot tea to provide a nominal ondansetron concentration of 32.8, 64.5, or 95.2 micrograms/mL. Samples were stored at -3 to 28 degrees C (noncarbonated-beverage mixtures except tea), 2 to 28 degrees C (carbonated-beverage mixtures), and 25 degrees C (tea) and assayed for ondansetron concentration by high-performance liquid chromatography at 6, 24, 48, and 72 hours (noncarbonated-beverage mixtures except tea); 6, 24, and 48 hours (carbonated-beverage mixtures); and 1 hour (tea). More than 95% of the initial ondansetron concentration was retained in apple juice, fruit punch, cherry-flavored drink, Sprite, and Diet Coke throughout the periods studied. A precipitate formed immediately after ondansetron was added to hot tea, but the drug was chemically stable for at least one hour in this preparation. Ondansetron hydrochloride injection 32.7, 64.5, and 95.2 micrograms/mL (expressed as free base) was stable in various beverages when stored at -3 to 28 degrees C for up to 72 hours. Ondansetron at these same concentrations precipitated in hot tea preparations but was chemically stable for at least one hour. PMID:8528869
Yamreudeewong, W; Danthi, S N; Hill, R A; Fox, J L
Stability of ondansetron hydrochloride injection in extemporaneously prepared oral solutions.
The stability of ondansetron hydrochloride in extemporaneously prepared oral solutions containing orange juice, cola, or cherry syrup was determined. Solutions were prepared by adding ondansetron hydrochloride to orange juice, cola, or cherry syrup to produce ondansetron concentrations of 0.267 and 0.067 mg/mL in orange juice or cola and 0.533 mg/mL in cherry syrup. The ondansetron concentration in orange juice and cola solutions was assayed at the time of preparation and at 30 minutes and one hour. The cherry syrup solution was stored at both 3-5 and 25-27 degrees C, with the ondansetron concentration being determined at the time of preparation and daily for seven days. All the solutions were prepared in triplicate. Ondansetron concentrations were measured by stability-indicating high-performance liquid chromatography. At each time interval, the mean ondansetron concentration remained > or = 97% of the initial measurement for all solutions. The appearance and color of the solutions did not change. Ondansetron hydrochloride was stable for at least one hour in orange juice or cola and at least seven days in cherry syrup. PMID:8427264
Graham, C L; Dukes, G E; Fox, J L; Kao, C F; Hak, L J
Spectrophotometric estimation of betahistine hydrochloride in tablet formulations
Aim: The study aims to develop simple, sensitive, rapid, accurate and precise spectrophotometric method for estimation of Betahistine hydrochloride in tablet dosage forms. Materials and Methods: For method I and II, in a series of 10 ml volumetric flask, aliquots of standard drug solution (100 ?g/ml) in double distilled water were transferred and diluted with same so as to give several dilutions in concentration range of 15-90 ?g/ml and 10-80 ?g/ml respectively of betahistine hydrochloride. To 5 ml of each dilution taken in a separating funnel, (5 ml of methyl orange for method I and 5 ml of bromo phenol blue for method II) reagent and 5 ml of chloroform was added. Reaction mixture was shaken gently for 5 min and allowed to stand so as to separate aqueous and chloroform layer. Absorbance maxima measured at 421.6 nm and 412 nm for method I and II respectively. Results: The recovery studies were found close to 100 % that indicates accuracy and precision of the proposed methods. The statistical analysis was carried out and results of which were found satisfactory. Standard deviation values were found low that indicated reproducibility of the proposed methods. Conclusion: Based on results the developed methods could be used for routine estimation of betahistine hydrochloride from tablet formulations.
Kumar, Amit; Nanda, Sanju; Chomwal, Rajiv
Release of nortriptyline hydrochloride from oil-water microemulsions.
The release of nortritptyline hydrochloride from oil-in-water (o/w) microemulsions (isopropyl myristate as oil, propylene glycol as cosurfactant, polysorbate 80 as surfactant and phosphate buffer, pH 7.4, as the continuous phase) containing increasing concentrations of polyethylene glycol 400, used to facilitate the diffusion of a drug from the inner oily phase of the microemulsion to the outer aqueous phase of such a dispersion system, was studied by determining the permeability constants of the drug through hydrophilic and lipophilic membranes separating the o/w microemulsions from the receiving aqueous phase (phosphate buffer pH 7.4). The permeability of nortriptyline hydrochloride from microemulsions through the lipophilic membrane increased as the concentration of polyethylene glycol 400 in the disperse system increased. The apparent permeability constant for nortriptyline hydrochloride, from the microemulsion without polyethylene glycol, was 1.36 x 10(-3) cm x h(-1), it increased up to 7.80 x 10(-3) cm x h(-1) in the presence of polyethylene glycol at a concentration of 50% (v/v) of the initial volume of the aqueous phase. PMID:11086887
Moreno, M; Frutos, P; Ballesteros, M P; Lastres, J L; Castro, D
Stereoselective dissolution of propranolol hydrochloride from hydroxypropyl methylcellulose matrices.
Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutical formulation containing a racemic drug and a chiral excipient. The mechanism of such an event may arise from preferential intermolecular interaction between the chiral excipient and one of the enantiomers. To test this hypothesis, the release of the enantiomers of propranolol hydrochloride into water from formulations containing the chiral excipients, hydroxypropyl methylcellulose (HPMC) or beta-cyclodextrin, was investigated by stereospecific HPLC analysis of the dissolved concentrations of each of the enantiomers from the formulations. The release of the enantiomers of propranolol hydrochloride from the formulations containing HPMC, although variable, was found to be stereoselective. However, the release of propranolol hydrochloride enantiomers from the beta-cyclodextrin complex was found to be non-stereoselective. PMID:8290480
Duddu, S P; Vakilynejad, M; Jamali, F; Grant, D J
Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of wild leopards (Panthera pardus fusca) in emergency situations.
In India, leopards (Panthera pardus fusca) inhabit human-dominated landscapes, resulting in encounters that require interventions to prevent harm to people, as well as the leopards. Immobilization is a prerequisite for any such intervention. Such emergency field immobilizations have to be carried out with limited tools, often amidst large uncontrollable crowds. An effective and practicable approach is discussed, based on 55 wild leopard immobilizations undertaken between January 2003 and April 2008. A xylazine hydrochloride (1.4 +/- 0.3 mg/kg)--ketamine hydrochloride (5 +/- 2 mg/kg) mixture was used for immobilization of leopards, based on estimated body weight. When weight could not be estimated, a standard initial dose of 50 mg of xylazine--150 mg of ketamine was used. Supplemental doses (50-75 mg) of only ketamine were used as required. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization. PMID:20597228
Belsare, Aniruddha V; Athreya, Vidya R
Coordination diversity of new mononuclear ONS hydrazone with transition metals: Synthesis, characterization, molecular modeling and antimicrobial studies
The mononuclear hydrazone ligand, H2L, a condensation product of 4-amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one with 2-hydroxy-1-naphthaldehyde and its metal chelates of Cu(II), Ni(II), Co(II), Zn(II), Cd(II), VO(IV) and UO2(VI) ions were synthesized and characterized using elemental analyses, spectral, magnetic and molar conductance studies as well as thermal gravimetric analysis (TGA). The physico-chemical studies support that the ligand acts as mono- or dibasic tridentate ONS donor toward metal ions forming a mononuclear square planar, tetrahedral, square pyramidal and octahedral geometrical arrangements except UO2(VI) complex in which the metal ion is octa-coordinated. The ligand field parameters, Dq, B and ? values, in the case of the cobalt and nickel complexes are calculated. The kinetics of the thermal decomposition for some metal complexes studied and their thermodynamic parameters were reported. Structural parameters of the ligand and its metal chelates have been calculated and correlated with the experimental data. The ligand and its metal chelates were screened for their antimicrobial activity against Staphylococcus aureus and Bacillus subtilis as Gram-positive bacteria, Escherichia coli and Salmonella typhimurium as Gram-negative bacteria and Candida albicans as fungus strain.
Adly, Omima M. I.; Taha, A.
Pharmacokinetics and cardiovascular effects in rabbits of a major hydralazine metabolite, the hydralazine pyruvic-acid hydrazone.
The hydrazone of hydralazine and pyruvic acid (HPH) has been recognized as a quantitatively important metabolite of hydralazine in human plasma. We evaluated the disposition of [14C] HPH after its i.v. administration to normal, anephric and probenecid-pretreated rabbits. Renal clearance of HPH in normal rabbits exceeded the glomerular filtration rate by a factor of 3 to 4 and accounted for 80 to 90% of the total body clearance. Active tubular secretion was established by the effect of probenecid pretreatment to reduce the renal clearance of HPH by 80%. Total body clearance of HPH in anephric rabbits was 10% of that of normal animals, emphasizing the minor importance of metabolic conversion for the overall disposition of HPH. HPH in a maximum dose of 50 mumol/kg i.v. had no hypotensive effect in renal hypertensive rabbits and did not interfere with the subsequent hypotensive response to hydralazine. This HPH dose produced plasma levels at least 50 times in excess of those reported in humans after administration of therapeutic doses of parent hydralazine. HPH is consequently of negligible clinical significance, despite the relatively high plasma concentration of this metabolite which occurs after administration of parent hydralazine. PMID:512915
Talseth, T; Haegele, K D; McNay, J L; Skrdlant, H B; Clementi, W A; Shepherd, A M
Antiplatelet and antithrombotic activities of non-steroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit.
Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1-5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA. PMID:24549233
Chelucci, Rafael Consolin; Dutra, Luiz Antônio; Lopes Pires, Maria Elisa; de Melo, Thais Regina Ferreira; Bosquesi, Priscila Longhin; Chung, Man Chin; Dos Santos, Jean Leandro
The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase II? Inhibition
The antitumor property of iron chelators and aromatic nitrogen mustard derivatives has been well documented. Combination of the two pharmacophores in one molecule in drug designation is worth to be explored. We reported previously the syntheses and preliminary cytotoxicity evaluation of benzaldehyde nitrogen mustard pyridine carboxyl acid hydrazones (BNMPH) as extended study, more tumor cell lines (IC50 for HepG2: 26.1 ± 3.5??M , HCT-116: 57.5 ± 5.3??M, K562: 48.2 ± 4.0??M, and PC-12: 19.4 ± 2.2??M) were used to investigate its cytotoxicity and potential mechanism. In vitro experimental data showed that the BNMPH chelating Fe2+ caused a large number of ROS formations which led to DNA cleavage, and this was further supported by comet assay, implying that ROS might be involved in the cytotoxicity of BNMPH. The ROS induced changes of apoptosis related genes, but the TFR1 and NDRG1 metastatic genes were not obviously regulated, prompting that BNMPH might not be able to deprive Fe2+ of ribonucleotide reductase. The BNMPH induced S phase arrest was different from that of iron chelators (G1) and alkylating agents (G2). BNMPH also exhibited its inhibition of human topoisomerase II?. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation.
Fu, Yun; Zhou, Sufeng; Liu, Youxun; Yang, Yingli; Sun, Xingzhi; Li, Changzheng
New acyclic 1,2,4-triazole-based Schiff base hydrazone: synthesis, characterization, spectrophotometric and computational studies.
A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H(4)L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H(2)L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H(4)L was characterized by using FT-IR, UV-Vis and (1)H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H(4)L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H(4)L were also measured in DMSO-water (1:10) mixture. Furthermore, (1)H chemical shifts of H(4)L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G(*) basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data. PMID:23321219
Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan
Reactivity differences between ?,?-unsaturated carbonyls and hydrazones investigated by experimental and theoretical electron density and electron localizability analyses.
It is still a challenge to predict a compound's reactivity from its ground-state electronic nature although Bader-type topological analyses of the electron density (ED) and electron localizability indicator (ELI) give detailed and useful information on electron concentration and electron-pair localization, respectively. Both ED and ELI can be obtained from theoretical calculations as well as high-resolution X-ray diffraction experiments. Besides ED and ELI descriptors, the delocalization index is used here; it is likewise derived from theoretical calculations as well as from experimental X-ray results, but in the latter case, demonstrated here for the first time. We investigate ?,?-unsaturated carbonyl and hydrazone compounds because resonance exhibited by these compounds in the electronic ground-state determines their reactive behavior. The degree of resonance as well as the reactivity contrast are quantified with the electronic descriptors. Moreover, competitive mesomeric substituent effects are studied using the two biologically important compounds acrolein and acrylamide. The reactivity differences predicted from the analyses are in line with the known reactivity of these compounds in organic synthesis. Hence, the capability of the ED and ELI for rationalizing and predicting different and competing substituent effects with respect to reactivity is demonstrated. PMID:21780784
Grabowsky, Simon; Weber, Manuela; Jayatilaka, Dylan; Chen, Yu-Sheng; Grabowski, Matthias T; Brehme, Rainer; Hesse, Malte; Schirmeister, Tanja; Luger, Peter
Solid surface room temperature phosphorimetry analysis of yohimbine hydrochloride in pharmaceutical formulations
A new method of analysis for yohimbine hydrochloride pharmaceutical formulations is reported. The phosphorescence characteristics of yohimbine hydrochloride were studied at room temperature employing low background paper substrate. The use of phosphorescence enhancers such as sodium iodide, thallium(I) nitrate, and sodium dodecyl sulfate were optimized to obtain limits of detection at the nanogram level. The interference effects of active ingredients
R. Q. Aucélio; A. D. Campiglia
Bioassay of o-Anisidine Hydrochloride for Possible Carcinogenicity. CAS No. 134-29-0.
A bioassay of o-anisidine hydrochloride for possible carcinogenicity was conducted by administering the test chemical in feed to Fischer 344 rats and B6C3F1 mice. Groups of 55 rats and mice of each sex were administered o-anisidine hydrochloride at one of...
Comparative in vivo evaluation of propranolol hydrochloride after oral and transdermal administration in rabbits
The purpose of this study was the in vivo evaluation of orally and transdermally administered propranolol hydrochloride in rabbits. Transdermal patches of propranolol hydrochloride (PPN) were formulated employing ethyl cellulose and polyvinylpyrrolidone as film formers. The pharmacodynamic (PD) and pharmacokinetic (PK) performance of PPN following transdermal administration was compared with that of oral administration. This study was carried out in
P Rama Rao; M. Narender Reddy; Sistla Ramakrishna; Prakash V Diwan
Acute toxicity and toxicokinetics of dipfluzine hydrochloride, a novel calcium channel blocker
Dipfluzine hydrochloride, diphenylpiperazine calcium channel blocker, is a promising candidate to treat ischemic stroke. The purpose of the study is to evaluate the acute toxicity and toxicokinetics of dipfluzine hydrochloride after single intravenous doses in rats. Acute toxicity study was performed in rats at doses of 5, 6, 10, 15, 25, 30, 35, and 40mg\\/kg. Concentrations of dipfluzine in plasma
Huiqing Hu; Yongli Wang; Tingmei Pei; Lei Dong; Yanfang Xu
Effects of sevelamer hydrochloride and calcium acetate on the oral bioavailability of ciprofloxacin
Background: The oral bioavailability of ciprofloxacin is significantly decreased when administered with calcium carbonate. Sevelamer hydrochloride is a phosphate-binding cationic polymer that is devoid of calcium. The authors conducted a 3-way, randomized, crossover study to determine the effects of sevelamer hydrochloride and calcium acetate on the relative oral bioavailability of ciprofloxacin. Methods: Fifteen healthy volunteers were assigned randomly to receive
Michael B Kays; Brian R Overholser; Bruce A Mueller; Sharon M Moe; Kevin M Sowinski
Stability and compatibility of topotecan hydrochloride for injection with common infusion solutions and containers
The stability and compatibility of topotecan hydrochloride with common infusion solutions and containers were studied. During this study, the leaching of diethylhexyl phthalate (DEHP), a major plasticizer of some polyvinyl chloride (PVC) materials was also investigated. A formulation of topotecan hydrochloride was added to 50 ml PVC infusion bags, polyolefin infusion bags and 150 ml glass bottles containing either 5%
Samuel B Craig; Uday H Bhatt; Kamlesh Patel
Synthesis, characterization and crystal structures of Ni(II), Cd(II) complexes with N-(2-propionic acid)-salicyloyl hydrazone and bipy\\/phen
The ligand N-(2-propionic acid)-salicyloyl hydrazone(H3L, 1) and its new transition metal(II) complexes [NiHL(bipy)H2O] (2), [CdHL(bipy)(H2O)2]2·2H2O (3) and [NiHL(phen)H2O]·H2O (4) (HL is a dianion, bipy?=?2,2?-bipyridine and phen?=?1,10-phenanthroline) were synthesized and characterized on the basis of elemental analyses, IR, H NMR, molar conductivity and thermal analysis. Single crystal X-ray diffraction showed that 1 is in keto form and connected by hydrogen bonds
Wang-Ting Wu; Shui-Yang He; Feng Liu; Feng-Ying Chen; Yao-Yu Wang; Qi-Zhen Shi
Oligonuclear Fe complexes (Fe, Fe4, Fe6, Fe9) derived from tritopic pyridine bis-hydrazone ligands-structural, magnetic, and Mössbauer studies.
Tri-topic pyridine bis-hydrazone ligands produce polynuclear complexes with Fe(II) and Fe(III) salts with varying nuclearity and metal ion oxidation states. Mononuclear, tetranuclear, hexanuclear, and nonanuclear examples are discussed using structural, magnetic and Mössbauer data. In one case, although X-ray data suggest a [3 × 3] Fe9 grid (space group P42/n), careful examination of the structure, in conjunction with magnetic and Mössbauer data, indicates an unusual situation where the corner and center sites are present at unit occupancy, whereas side site occupancy is ?0.6. PMID:24762184
Anwar, Muhammad U; Dawe, Louise N; Parsons, Stewart R; Tandon, Santokh S; Thompson, Laurence K; Dey, Subrata K; Mereacre, Valeriu; Reiff, William M; Bunge, Scott D
The effects of Dalmane /flurazepam hydrochloride/ on human EEG characteristics.
NASA Technical Reports Server (NTRS)
Evaluation of the changes in the waking EEGs of six healthy male subjects who received 30 mg daily oral doses of flurazepam hydrochloride for two weeks. A placebo was then substituted for flurazepam for another two weeks. An increase in beta activity with a maximum in fronto-central leads was observed during the test period. A small increase in the mean wavelength of the alpha and theta activities in the central-occipital derivations was also apparent in the subjects during the period.
Frost, J. D., Jr.; Carrie, J. R. G.; Borda, R. P.; Kellaway, P.
Torsionally responsive C3-symmetric azo dyes: azo-hydrazone tautomerism, conformational switching, and application for chemical sensing.
An efficient triple azo coupling reaction between anilines and phloroglucinol furnished a series of C(3)-symmetric molecules 7-9 supporting multiple conjugation pathways that converge at the molecular core. A combination of (1)H/(13)C NMR spectroscopy, X-ray crystallography, and density functional theory computational studies provided a coherent picture of the [n,pi]-conjugated molecular core, which is best described as the tris(hydrazone) [rather than tris(azo)] tautomer stabilized by resonance-assisted hydrogen bonding. For a homologous series of compounds, an increase in the torsional angles between the planar molecular core and the peripheral aryl groups results in a systematic blue shift in the low-energy electronic transitions (7, 523 nm; 8, 505 nm; 9, 445 nm in CHCl(3)) that qualitatively correlates with the shrinkage of effective conjugation through structural distortion. Similar spectral shifts could also be induced by amine substrates that interact with the intramolecular hydrogen-bonding network to trigger bond-twisting motions. Specifically, a brief exposure of a thin film of 7 to vapor samples of butyl-, hexyl-, diethyl-, and diisopropylamine resulted in a rapid and reversible color change from pink to dark-orange. Under similar conditions, however, triethylamine did not elicit any detectable color change, despite the fact that it has a significantly higher vapor pressure than n-hexylamine. These findings implicate that the hydrogen-bonding donor ability is a key requirement for the binding-induced conformational switching, which allows for direct naked-eye detection of volatile amines under ambient conditions. PMID:20698548
Lee, Ho Yong; Song, Xinli; Park, Hyunsoo; Baik, Mu-Hyun; Lee, Dongwhan
Torsionally Responsive C[subscript 3]-Symmetric Azo Dyes: Azo?Hydrazone Tautomerism, Conformational Switching, and Application for Chemical Sensing
An efficient triple azo coupling reaction between anilines and phloroglucinol furnished a series of C{sub 3}-symmetric molecules 7-9 supporting multiple conjugation pathways that converge at the molecular core. A combination of {sup 1}H/{sup 13}C NMR spectroscopy, X-ray crystallography, and density functional theory computational studies provided a coherent picture of the [n,{pi}]-conjugated molecular core, which is best described as the tris(hydrazone) [rather than tris(azo)] tautomer stabilized by resonance-assisted hydrogen bonding. For a homologous series of compounds, an increase in the torsional angles between the planar molecular core and the peripheral aryl groups results in a systematic blue shift in the low-energy electronic transitions (7, 523 nm; 8, 505 nm; 9, 445 nm in CHCl{sub 3}) that qualitatively correlates with the shrinkage of effective conjugation through structural distortion. Similar spectral shifts could also be induced by amine substrates that interact with the intramolecular hydrogen-bonding network to trigger bond-twisting motions. Specifically, a brief exposure of a thin film of 7 to vapor samples of butyl-, hexyl-, diethyl-, and diisopropylamine resulted in a rapid and reversible color change from pink to dark-orange. Under similar conditions, however, triethylamine did not elicit any detectable color change, despite the fact that it has a significantly higher vapor pressure than n-hexylamine. These findings implicate that the hydrogen-bonding donor ability is a key requirement for the binding-induced conformational switching, which allows for direct naked-eye detection of volatile amines under ambient conditions.
Lee, Ho Yong; Song, Xinli; Park, Hyunsoo; Baik, Mu-Hyun; Lee, Dongwhan (Indiana)
Synthesis and characterization of a new mebendazole salt: mebendazole hydrochloride.
Mebendazole hydrochloride [(5-benzoyl-1H-benzimidazole-2-yl)-carbamic acid methyl ester hydrochloride, MBZ.HCl], a new stable salt of mebendazole (MBZ), has been synthesized and characterized. It can easily be obtained from recrystallization of forms A, B, or C of MBZ in diverse solvents with the addition of hydrochloric acid solution. Crystallographic data reveals that the particular conformation adopted by the carbamic group contributes to the stability of the network. The crystal packing is stabilized by the presence of three N-H...Cl intermolecular interactions that form chains along the b axis. The XRD analyses of the three crystalline habits found in the crystallization process (square-based pyramids, pseudohexagonal plates, and prismatic) show equivalent diffraction patterns. The vibrational behavior is consistent with crystal structure. The most important functional groups show shifts to lower or higher frequencies in relation to the MBZ polymorphs. The thermal study on MBZ.HCl indicates that the compound is stable up to 160 degrees C approximately. Decomposition occurs in four steps. In the first step the HCl group is eliminated, and after that the remaining MBZ polymorph A decomposes in three steps, as happens with polymorphs B and C. ( PMID:17854049
Brusau, E V; Camí, G E; Narda, G E; Cuffini, S; Ayala, A P; Ellena, J
Identification, isolation and characterization of impurities of clindamycin palmitate hydrochloride.
Clindamycin palmitate hydrochloride is a water soluble hydrochloride salt of the ester of clindamycin and palmitic acid. It is inactive in vitro, rapid in vivo hydrolysis converts this compound to the antibacterially active clindamycin. Total 12 impurities at levels ranging from 0.05% to 0.5% were detected by isocratic reverse-phase high performance liquid chromatography (HPLC) using RI detector. The molecular weights of impurities were determined by LC-MS analysis. Two impurities were starting materials and the remaining impurities were isolated from crude samples/enriched mother liquors using reverse-phase preparative HPLC. Based on the spectral data the structures of these impurities were characterized as, clindamycin palmitate sulphoxides alpha-/beta-isomers (impurity I); clindamycin laurate (impurity II); lincomycin palmitate (impurity III); clindamycin myristate (impurity IV); epiclindamycin palmitate (impurity V); clindamycin palmitate 3-isomer (impurity VI); clindamycin pentadecanoate (impurity VII); clindamycin B-palmitate (impurity VIII); clindamycin heptadecanoate (impurity IX) and clindamycin stearate (impurity X). Structural elucidation of all impurities by spectral data ((1)H NMR, (13)C NMR, MS and IR) and formation of these impurities have been discussed in detail. PMID:18947955
Bharathi, Ch; Jayaram, P; Sunder Raj, Joseph; Saravana Kumar, M; Bhargavi, V; Handa, V K; Dandala, Ramesh; Naidu, A
Fabrication and development of pectin microsphere of metformin hydrochloride.
Purpose. The objective of the proposed work is to evaluate the efficacy of Pectins to qualify them as polymers for designing an oral microsphere for the delivery of selected oral antidiabetic drug-like metformin hydrochloride. Methods. Different Microspheres formulations were prepared by the water in oil (w\\o) emulsion solvent evaporation technique and subsequently evaluated for its different physical parameters as well as its in vitro and in vivo drug release study. Results. The formulations F2 (98.42) and F3 (98.03) showed a constant and high release in the dissolution profile, so among these two formulations, F2 was taken for development study, due to the better result shown over in other evaluation parameters. From the HPLC determinations after in vivo study, it had been found that the test samples and the standard sample had not shown any significant fluctuation in relation to their retention time. Conclusion. From in vitro and in??vivo results, it may be concluded that drug-loaded pectin microspheres in 1?:?1 ratio are a suitable delivery system for metformin hydrochloride and may be used for effective management of NIDDM. From this experiment, it could be concluded that as a natural polymer, pectin has potentiality in novel drug delivery system. PMID:22900209
Banerjee, Pritam; Deb, Jyotirmoy; Roy, Amitava; Ghosh, Amitava; Chakraborty, Prithviraj
Application of direct crystallization for racemic compound propranolol hydrochloride.
The application of direct crystallization integrating with chromatography to the resolution of a racemic compound propranolol hydrochloride was studied and the crystallization progression was clearly illustrated in terms of the diagram of solubility and metastable zone widths with different enantiomeric compositions. The solubility and metastable zone widths of propranolol hydrochloride in the mixture of methanol and isopropanol were determined using an in situ Lasentec Focused Beam Reflectance Measurement (FBRM) probe. The direct crystallizations were carried out in an automatic lab reactor (Mettler Toledo LabMax) system. The optical purity of final product crystals was examined using differential scanning calorimetry (DSC), HPLC and PXRD. The crystal size distribution and morphology were analyzed using Malvern Mastersizer and Jeol SEM. It was found that optically pure crystal product could be obtained within certain safe supersaturation limit and there was no evidence of polymorph or solvate/hydrate transformation during the crystallization process. There was no selectivity of crystal growth or nucleation between the pure enantiomer and its racemate when the solution reaches the temperature lower than saturation temperature of the racemate. Hence, the critical supersaturation control of a solution was essential to obtain pure enantiomers from a partially resolved racemate. PMID:17549769
Wang, Xiujuan; Lu, Jie; Ching, Chi Bun
Transepithelial transport of biperiden hydrochloride in Caco-2 cell monolayers.
The aim of this research has been to determine the biperiden hydrochloride permeability in Caco-2 model, in order to classify it based on the Biopharmaceutics Classification System (BCS). The World Health Organization (WHO) as well as many other authors have provisionally assigned the drug as BCS class I (high solubility-high permeability) or III (high solubility-low permeability), based on different methods. We determined biperiden BCS class by comparing its permeability to 5 pre-defined compounds: atenolol and ranitidine hydrochloride (low permeability group) and metoprolol tartrate, sodium naproxen and theophylline (high permeability group). Since biperiden permeability was higher than those obtained for high permeability drugs, we classified it as a BCS class I compound. On the other hand, as no differences were obtained for permeability values when apical to basolateral and basolateral to apical fluxes were studied, this drug cannot act as a substrate of efflux transporters. As a consequence of our results, we suggest that the widely used antiparkinsonian drug, biperiden, should be candidate for a waiver of in vivo bioequivalence studies. PMID:22554863
Abalos, Ivana S; Rodríguez, Yanina I; Lozano, Verónica; Cereseto, Marina; Mussini, Maria V; Spinetto, Marta E; Chiale, Carlos; Pesce, Guido
Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies.
Recently we described some (thiazol-2-yl)hydrazones as antiprotozoal, antifungal and anti-MAO agents as well as Gcn5 HAT inhibitors. Among these last compounds, CPTH2 and CPTH6 showed HAT inhibition in cells and broad anticancer properties. With the aim to identify HAT inhibitors more potent than the two prototypes, we synthesized several new (thiazol-2-yl)hydrazones including some related thiazolidines and pyrimidin-4(3H)-ones, and we tested the whole library existing in our lab against human p300 and PCAF HAT enzymes. Some compounds (1x, 1c', 1d', 1i' and 2m) were more efficient than CPTH2 and CPTH6 in inhibiting the p300 HAT enzyme. When tested in human leukemia U937 and colon carcinoma HCT116 cells (100 ?M, 30 h), 1x, 1i' and 2m gave higher (U937 cells) or similar (HCT116 cells) apoptosis than CPTH6, and were more potent than CPTH6 in inducing cytodifferentiation (U937 cells). PMID:24835815
Carradori, Simone; Rotili, Dante; De Monte, Celeste; Lenoci, Alessia; D'Ascenzio, Melissa; Rodriguez, Veronica; Filetici, Patrizia; Miceli, Marco; Nebbioso, Angela; Altucci, Lucia; Secci, Daniela; Mai, Antonello
Investigation on the toxic interaction of chrysoidine hydrochloride-CTMAB combined contamination with calf thymus DNA
The toxic interaction of the azo dye-chrysoidine hydrochloride combined with cetyltrimethyl ammonium bromide (CTMAB) in living tissue was studied in vitro. The absorption spectrum, resonance light scattering (RLS), circular dichroism (CD) and transmission electron microscopy (TEM) results showed that the toxicity of chrysoidine hydrochloride itself to calf thymus DNA (ct-DNA) is weak, while the chrysoidine hydrochloride-CTMAB combined pollution showed obvious toxic interaction with ct-DNA. The chrysoidine hydrochloride-CTMAB combined contamination can interact with ct-DNA to form an ion-associated complex through electrostatic and hydrophobic forces. The conformation of DNA was changed in the interaction process to show toxic. The experimental results showed that the combination of chrysoidine hydrochloride-CTMAB has higher toxicity to ct-DNA than either chrysoidine hydrochloride or CTMAB individually, and the combined pollution showed a strong toxic co-effect at a dose of 3.0 × 10 -4 mol L -1 chrysoidine hydrochloride and 1.6 × 10 -5 mol L -1 CTMAB.
Chi, Zhenxing; Liu, Rutao; Pan, Xingren; Teng, Yue; Qin, Hao; Zhu, Jianhua; Hao, Xiaopeng
Developmental rates of immatures of three Chrysomya species (Diptera: Calliphoridae) under the effect of methylphenidate hydrochloride, phenobarbital, and methylphenidate hydrochloride associated with phenobarbital.
Entomotoxicology is focused on obtaining data on necrophagous entomofauna, for criminal investigations purposes. This study aimed to evaluate the effect of different concentrations of methylphenidate hydrochloride, phenobarbital, and their association on the developmental rate, larval and pupal survivorship, and the interval of emergence of adults of Chrysomya albiceps (Wiedemann), Chrysomya megacephala (Fabricius), and Chrysomya putoria (Wiedemann) (Diptera: Calliphoridae). Considering the therapeutic dose (TD) of methylphenidate hydrochloride (0.29 mg/Kg), the concentrations tested were 10× TD, 50× TD, and 100× TD. For phenobarbital, the concentrations used were 1× TD (=150 mg/Kg), 3.3× TD, and 6.7× TD. For the association of the drugs, the combinations used were 10× TD-methylphenidate hydrochloride plus 1× TD-phenobarbital, 50× TD-methylphenidate hydrochloride plus 3.3× TD-phenobarbital, and 100× TD-methylphenidate hydrochloride plus 6.7× TD-phenobarbital. The control group, without addition of drug, was maintained under the same conditions of temperature (25?±?1 °C), humidity (70?±?10%), and photoperiod (12 h). Specimens of each group were weighed every 12 h until pupariation. The developmental rate of the three Chrysomya species immatures was monitored. For C. albiceps the developmental time was delayed in 24 h for methylphenidate hydrochloride group and in 12 h for the phenobarbital and the drugs association groups. The effect was observed only at specific ages for C. megacephala, without altering the developmental time. For C. putoria, the developmental time was delayed in 12 h for methylphenidate hydrochloride group and in 24 h for the phenobarbital and the drugs association groups. The emergence interval was similar among all experimental groups, but larval and pupal viabilities were affected in different ways. PMID:24633905
Rezende, Fábio; Alonso, Marcela A; Souza, Carina M; Thyssen, Patrícia J; Linhares, Arício X
Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of Indian fox (Vulpes bengalensis) in field situations.
Reports on doses of anesthetic agents for safe and effective immobilization of most wild species occurring in India are very limited. Further, the anesthetic agents available in India for field immobilizations are limited to xylazine hydrochloride and ketamine hydrochloride. A safe and effective dosage of xylazine-ketamine for Indian fox (Vulpes bengalensis) is reported, based on 37 wild Indian fox immobilizations between April 2006 and May 2007. Foxes captured for a radiotelemetry and health monitoring study were immobilized with a mixture of xylazine (2.27 +/- 0.44 mg/kg) and ketamine (13.39 +/- 2.26 mg/kg). Induction and recovery was smooth and uneventful in all foxes. The duration of anesthesia was sufficient for the fitting of radiotransmitters, morphometric measurements, and blood sampling. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization. The results suggest that field immobilization of Indian foxes with 2 mg/kg xylazine and 13 mg/kg ketamine is effective and safe. PMID:24063107
Belsare, Aniruddha V; Vanak, Abi Tamim
Multivariate Chemometric Assisted Analysis of Metformin Hydrochloride, Gliclazide and Pioglitazone Hydrochloride in Bulk Drug and Dosage Forms
Purpose: In this work a numerical method, based on the use of spectrophotometric data coupled to partial least squares (PLS) regression and net analyte preprocessing combined with classical least square (NAP/CLS) multivariate calibration, is reported for the simultaneous determination of metformin hydrochloride (MET), gliclazide (GLZ) and pioglitazone hydrochloride (PIO) in synthetic samples and combined commercial tablets. Methods: Spectra of MET, GLZ and PIO were recorded at concentrations within their linear ranges (5-25 µg/ml, 0.5-8 µg/ml and 0.5-3 µg/ml respectively) and were used to compute a total of 25 synthetic mixtures involving 15 calibration and 10 validation sets between wavelength range of 200 and 400 nm in 0.1N HCl. The suitability of the models was decided on the basis of root mean square error (RMSE) values of calibration and validation data. Results: The analytical performances of these chemometric methods were characterized by relative prediction errors and recovery studies (%) and were compared with each other. These two methods were successfully applied to pharmaceutical formulation, tablet, with no interference with excipients as indicated by the recovery study results. Mean recoveries of the commercial formulation set together with the figures of merit (calibration sensitivity, selectivity, limit of detection, limit of quantification etc.) were estimated. Conclusion: The proposed methods are simple, rapid and can be easily used as an alternative analysis tool in the quality control of drugs and formulation.
Bhaskar, Radhika; Bhaskar, Rahul; Sagar, Mahendra K; Saini, Vipin
Liquid crystalline pharmacogel based enhanced transdermal delivery of propranolol hydrochloride.
A novel pharmacogel was developed for the enhanced transdermal delivery of propranolol hydrochloride (PH). The synthesized prodrugs, propranolol palmitate hydrochloride (PPH) and propranolol stearate hydrochloride (PSH) self-assembled to form gel simply upon mixing alcoholic solution of prodrug with an aqueous solution in a specified ratio. By varying the ratio of prodrug, alcohol and water, three-component phase diagram was constructed which revealed isotropic-gel-vesicular dispersion regions, respectively concomitant to increasing the ratio of water. The gel phase is termed 'Pharmacogel' and exhibits birefringence under plane-polarized light corroborating the presence of lamellar liquid crystals. The pharmacogel by virtue of high chemical potential gradient and improved physicochemical properties showed the enhanced in-vitro skin permeation flux of 51.5+/-3.7 and 42.5+/-3.1 microg/cm(2)/h from PPH and PSH gel, respectively, as compared to 1.9+/-0.1 microg/cm(2)/h for control; and decrease in lag time (1.8 and 2.8 h for PPH and PSH gel, respectively) compared to control (7.6 h) was observed. The admixing of egg lecithin (EL) in increasing ratio concomitantly decreased the flux values to 31.7+/-2.1 microg/cm(2)/h (at a mole ratio of 50:50 PPH:EL) and increased the lag time. In the gel containing 50% EL, the addition of span 40 and cholesterol slightly reduced the permeation while sodium deoxycholate and Tween-80 improved it. The plasma drug levels following transdermal application of control were low (C(max)=23 ng/ml) while in PPH gel, it increased with time reaching C(max) of 94 ng/ml at 8 h post-application of PPH gel (C(max) of 75 ng/ml at 12 h post application of PL5 gel) and maintained for longer times. The AUC(0-32 h) for PPH gel was much higher (1968 ng h/ml) than control (AUC(0-18 h) was 239 ng h/ml), while EL mixed gel also showed better absorption (AUC(0-32 h) was 1707 ng h/ml). The gel formulations also caused less irritation than control, while mixed gel showed least irritation. This novel self-assembled pharmacogel providing high transdermal permeation with many variables to regulate the delivery is therefore having a great potential in percutaneous delivery. PMID:12175739
Namdeo, Alok; Jain, N
Double emulsion templated monodisperse phospholipid liposomes incorporating Doxorubicin hydrochloride
We present a novel approach for fabricating monodisperse phospholipid liposomes incorporating water soluble anticancer drug Doxorubicin hydrochloride using controlled w/o/w double emulsions as templates. Glass-capillary microfluidics is used to generate monodisperse w/o/w double emulsion templates and double emulsion droplet size is from 20 to 100 um according to different flow rates. We show that the high uniformity in size and shape of the templates are maintained in the final phospholipid liposomes after a solvent removal step by Nikon eclipse microscopy. The lipid bilayers encapsulating anticancer drug inside is retained after the emulsion drops are converted to vesicles. The liposomes vesicles are promising water soluble anticancer drug delivery vehicles.
Hai, Mingtan; Weitz, David
Spectroscopic and Electrical Conductivity Studies of Some Semicarbazide Hydrochloride Complexes
The infrared and electronic absorption spectra of semicarbazide hydrochloride and its complexes with anthracene, tetracyanoquinodimethane TCNQ, Na-fluorescein and cupferron were recorded in the regions 200-4000cm-1 and 200-400nm. The new bands that appeared in the complex spectra were assigned. The effect of the complex formation on the frequency and intensity of the active vibrational bands was also studied. The internal energy changes of the complexes were calculated in a new line of calculation to give a clear insight about the stability of the investigated complexes. The electrical conductivity of the complexes was measured in the temperature range 25-130°C. The activation energy E was calculated and discussed on the basis of the spectroscopic information.
Fadly, M.; El-Manakhly, H.
Identification and Characterization of Potential Impurities in Raloxifene Hydrochloride
During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxyphenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy
Reddy, Reguri Buchi; Goud, Thirumani Venkateshwar; Nagamani, Nagabushanam; Kumar, Nutakki Pavan; Alagudurai, Anandan; Murugan, Raman; Parthasarathy, Kannabiran; Karthikeyan, Vinayagam; Balaji, Perumal
Studies on the interaction of palmatine hydrochloride with bovine hemoglobin.
The interaction between bovine hemoglobin (BHb) and palmatine hydrochloride (PMT) was investigated at different temperatures using multispectroscopy, as well as the effect of common metal ions (Ca(2+) , Mg(2+) , Zn(2+) , Cu(2+) , Fe(2+) , Fe(3+) , Co(2+) , Ni(2+) ) on the BHb-PMT system. Results showed that the quenching mechanism of PMT on BHb was a static process. The electrostatic force played an important role in the conjugation reaction between BHb and PMT. The order of magnitude of the binding constants (Ka ) was 10(4) , and the number of binding sites (n) in the binary system was?~?1. The binding distance (r) was?~?2.44?nm and the primary binding for PMT was located at ?-37 tryptophan in the hydrophobic cavity of BHb. In addition, the Hill's coefficients were?~?1. Synchronous and circular dichroism spectra revealed that the microenvironment and the conformation of BHb were changed during the binding reaction. PMID:23696111
Liu, Baosheng; Yan, Xiaona; Cao, Shina; Chong, Baohong; Lü, Yunkai
Pharmaceutical development of an intravenous dosage form of diacetylmorphine hydrochloride.
A solid dosage form for multiple use was developed for parenteral administration of diacetylmorphine in a clinical trial on co-prescription of heroin to heroin addicts. A 300-mg/mL diacetylmorphine hydrochloride solution was lyophilised as 10-mL aliquots in 30-mL glass vials, to be reconstituted to 150 mg/mL with water for injection before use. Addition of bulking agents for improvement of the cake structure of the lyophilised product appeared unnecessary. Stability studies indicated good stability of the lyophilised product under prescribed storage conditions (25 degrees C, 60% relative humidity) and under more extreme conditions (40 degrees C, 75% relative humidity). The reconstituted product was found to be stable for six days at room temperature. Suitability of the product for multiple use was supported by the fact that the reconstituted product was found to be antimicrobially active. PMID:15663060
Klous, Marjolein G; Nuijen, Bastiaan; van den Brink, Wim; Van Ree, Jan M; Beijnen, Jos H
Effect of L-leucinamide hydrochloride on experimental inflammation.
L-leucinamide hydrochloride, an amino acid derivative, was found to share the ability of phenylbutazone in attenuating the phlogistic response induced by intraplantar injection of formaldehyde and nystatin in the unanesthetized rat. In the granuloma pouch induced by the injection of air and croton oil, chronic administration of the drug for 7 days resulted in significant reduction in the volume of exudate and the weight of granulation tissue. While the mechanism of anti-inflammatory action has not been elucidated, it seems that the pituitary-adrenal system is not involved since there was no change in the weight of the adrenals. Of interest is the finding that leucinamide, unlike phenylbutazone, failed to produce gastric ulcers in the effective anti-inflammatory doses. PMID:3438573
Madan, B R; Al-Motrefi, A
Coated hydralazine hydrochloride beads for sustained release after oral administration.
Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10?h in simulated intestinal fluid. PMID:23057650
Mughal, M Akhlaq; Saripella, Kalyan K; Kouba, Chahinaz; Iqbal, Zafar; Neau, Steven H
Residual solvent analysis in hydrochloride salts of active pharmaceutical ingredients.
GMP conditions commands to control adequately the quality of APIs by checking the levels of residual solvents. Organic solvents such as acetone, ethyl acetate, isopropyl alcohol, methanol, tetrahydrofuran and toluene frequently used in pharmaceutical industry for the manufacturing of Active Pharmaceutical ingredients (APIs). A selective Gas Chromatographic (GC) method has been developed and validated as per ICH guidelines for residual solvent analysis in 10 different hydro chloride salts of APIs. Residual solvents in APIs were monitored using gas chromatography (GC) with Flame Ionisation detector (FID). The separation was carried out on BP 624 column (30 mx0.53 mm i.d.x0.25 m coating thickness), using GC 17 A shimadzu, with nitrogen as carrier gas in the split mode by direct injection method. The method described is simple, sensitive, rugged, reliable and reproducible for the quantitation of acetone, ethyl acetate, isopropyl alcohol, methanol, tetrahydrofuran and toluene at residual level from hydrochloride chloride salts of APIs. PMID:19783521
Puranik, S B; Pawar, Varun R; Lalitha, N; Pai, P N Sanjay; Rao, G K
Conductivity scaling and thermoelectric properties of polyaniline hydrochloride
We report on the thermoelectric properties of the polyaniline hydrochloride as a function of the temperature. In order to stress the influences of both the synthesis and the samples preparation on the thermoelectric efficiency, we have systematically measured the electrical conductivity, the thermopower, and the thermal conductivity. We show that several parameters such as the polymerization temperature and the pressure used to compress powders are crucial in order to optimize the thermoelectric performance. The microscopic origins of the transport coefficients are also discussed. In particular, the overall dataset of the measured electrical conductivity is found to scale onto a master curve involving a unique microscopic length, which coincides with the total bond length of the repeating unit of the polymeric chain. We believe that the drawn conclusions can hold for most of the conducting polymers and are thus potentially generic.
Limelette, P.; Schmaltz, B.; Brault, D.; Gouineau, M.; Autret-Lambert, C.; Roger, S.; Grimal, V.; Tran Van, F.
Amantadine hydrochloride treatment in heredodegenerative ataxias: a double blind study.
OBJECTIVE: A group of 27 patients with Friedreich's ataxia and another group of 30 patients with olivopontocerebellar atrophies were each randomly divided into two subgroups, one receiving placebo and the other amantadine hydrochloride (AH; 200 mg daily) for three to four months. METHODS: The effect of double blind treatment was evaluated by simple visual and auditory reaction time (RT) and movement time (MT) for both right and left hands. RESULTS: The subgroup with olivopontocerebellar atrophies receiving AH showed significant improvement on seven out of eight variables studied by analysis of covariance. In patients with Friedreich's ataxia, improvement was definitely less. Treatment remained contraindicated for those with cardiomyopathies or drug intolerance. CONCLUSION: The rationale of AH use in heredodegenerative ataxias can be explained by its replacement effect (dopamine release) and by direct involvement of N-methyl-D-aspartate (NMDA) in glutamate mediated neurotoxicity in cerebellar granular cells; memantine, an AH analogue, is a potent blocker of NMDA receptors.
Botez, M I; Botez-Marquard, T; Elie, R; Pedraza, O L; Goyette, K; Lalonde, R
Berberine hydrochloride prevents postsurgery intestinal adhesion and inflammation in rats.
Intestinal adhesion, characterized by connection of the loops of the intestine with other abdominal organs by fibrous tissue bands, remains an inevitable event of abdominal operations and can cause a number of complications. Berberine hydrochloride (berberine), a natural plant alkaloid derived from Chinese herbal medicine, is characterized by diverse pharmacological effects, such as anticancer and lower elevated blood glucose. This study is designed to investigate the effects of berberine on adhesion and inflammation after abdominal surgeries and the underlying molecular mechanisms. Adhesion severity grades and collagen deposition were assessed 14 days after surgery. We evaluated the levels of intercellular adhesion molecule-1 (ICAM-1) and inflammatory cytokines interleukin-1? (IL-1?), IL-6, transforming growth factor ? (TGF-?), tumor necrosis factor-? (TNF-?), and examined transforming growth factor-activated kinase 1 (TAK1)/c-Jun N-terminal kinase (JNK) and TAK1/nuclear factor ?B (NF-?B) signaling. The surgery group experienced the most severe adhesions, and berberine strikingly reduced the density and severity of adhesion. Results showed significant lower expression of IL-1?, IL-6, TGF-?, TNF-?, and ICAM-1, in berberine groups compared with the operation group. Activities of phosphorylated JNK and phosphorylated NF-?B were inhibited in the berberine groups compared with the surgery group. Our novel findings identified berberine hydrochloride as a promising strategy to prevent adhesion by downregulating ICAM-1 and reduce inflammation by inhibiting the TAK1/JNK and TAK1/NF-?B signaling after abdominal surgery, which brought out a good therapeutic approach for the development of clinical application for postoperative abdominal adhesion and inflammation. PMID:24676878
Zhang, Yong; Li, Xiaoguang; Zhang, Qingwei; Li, Jiamin; Ju, Jiaming; Du, Ning; Liu, Xin; Chen, Xiaohui; Cheng, Feiran; Yang, Lei; Xu, Chaoqian; Bilal, Muhammad U; Wei, Yunwei; Lu, Yanjie; Yang, Baofeng
Formulation and evaluation of verapamil hydrochloride loaded solid lipid microparticles.
The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after processing showed that verapamil did not undergo any chemical modification within the micro-particles. The in-vitro release of verapamil from the microparticles was very low and an initial burst effect of 17% of the dose was observed. The slow release may help to avoid a high frequency of administration. The prepared solid lipid microparticles appear to have interesting perspectives as delivery systems for the oral administration of verapamil hydrochloride with improved half-life, improved bioavailability, and minimized local and systemic gastrointestinal disturbances of the drug. PMID:21391431
Pilaniya, U; Pilaniya, K; Chandrawanshi, H K; Gupta, N; Rajput, M S
21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.
...hydrocortisone spray contains 300 milligrams of oxytetracycline hydrochloride and 100 milligrams of hydrocortisone with an inert freon propellant such that a 1-second spray treatment will deliver approximately 2.5 milligrams of oxytetracycline...
Doxapram Hydrochloride Aggravates Adrenaline-Induced Arrhythmias Accompanied by Bidirectional Ventricular Tachycardia
Objectives. Doxapram hydrochloride is a respiratory stimulant that has an inhibitory effect on myocardial IK1 potassium channels and is thought to increase membrane instability and excitability in myocardial cells. We examined the arrhythmogenic effects of doxapram hydrochloride in a rat model of halothane adrenaline-induced arrhythmia. Methods. Thirteen female Wistar rats (12–14 weeks old) were used in the study. Animals were anesthetized with inhalation of halothane to permit observation of the effects of doxapram hydrochloride on halothane adrenaline-induced arrhythmia. Time-dependent changes in ECG repolarization characteristics (QT, QTc, JTp, JT, and Tp-e intervals) were studied. Results. Doxapram hydrochloride itself did not induce arrhythmia but did induce bidirectional ventricular tachycardia after addition of adrenaline. Conclusion. Drug-induced impairment of intracellular Ca2+ regulation caused BVT in the absence of genetic abnormalities in proteins in the sarcoplasmic reticulum.
Oikawa, Shota; Nomura, Hiroko; Nishio, Miki; Nagata, Rina; Hata, Tadayoshi
Fabrication of Triple-Layer Matrix Tablets of Venlafaxine Hydrochloride Using Xanthan Gum
The objective of present investigation was to develop venlafaxine hydrochloride-layered tablets for obtaining sustained drug\\u000a release. The tablets containing venlafaxine hydrochloride 150 mg were prepared by wet granulation technique using xanthan\\u000a gum in the middle layer and barrier layers. The granules and tablets were characterized. The in vitro drug dissolution study was conducted in distilled water. The tablets containing two lower
Mukesh C. Gohel; Shital H. Bariya
Hollow Fibers as an Oral Sustained-Release Delivery System Using Propranolol Hydrochloride
Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and\\/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochloride as a model drug. The U.S.P. basket dissolution method was used to evaluate the in vitro
Munir A. Hussain; Robert C. DiLuccio; Eli Shefter; Arthur R. Hurwitz
Human pharmacokinetics of the muscle relaxant, eperisone hydrochloride by liquid chromatography–electrospray tandem mass spectrometry
Eperisone hydrochloride (4?-ethyl-2-methyl-3-piperidinopropiophenone hydrochloride) is a muscle relaxant agent, widely used\\u000a in the treatment of patients with muscular contractures, low back pain or spasticity. Because of its mechanism of action (inhibition\\u000a of gamma-efferent firing and local vasodilatation activity), side effects on central nervous system are rarely observed. A\\u000a sensitive liquid chromatography–electrospray ionization-mass spectrometry method for determination of eperisone in human
Barbara Melilli; Cateno Piazza; Daniela Cristina Vitale; Maria Rosa Marano; Andrea Pecori; Paolo Mattana; Valentina Li Volsi; Carmelo Iuculano; Francesco Cardě; Filippo Drago
Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy
Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for approval from the Food and Drug Administration.
Epstein, J.B.; Stevenson-Moore, P.
Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes
Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.
Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit
Voltammetric assay of anti-vertigo drug betahistine hydrochloride in sodium lauryl sulphate
Assay and electrochemical behaviour of betahistine hydrochloride in Britton–Robinsons (BR) buffer of pH range 2.5–12.0 at a glassy carbon electrode have been investigated. Addition of anionic surfactant (sodium lauryl sulphate) to the betahistine hydrochloride solution containing electrolyte enhanced the reduction current signal while neutral surfactant (Tween-20) and cationic surfactant cetyl trimethylammonium bromide (CTAB) showed an opposite effect. Voltammograms of betahistine
Rajeev Jain; Rajeev Kumar Yadav; Jahangir Ahmad Rather
Loperamide hydrochloride (4-(p-chlorophenyl)-4- -hydroxy-N,N-dimethyl-diphenyl-1-piperidine butyrami- de hydrochloride), is an opiate agonist widely used as an effective drug for the control and symptomatic relief of acute non-specific diarrhea (1). More recently, it has also been reported that loperamide could have some interest as an antihyperalgesic agent reducing pain without any central nervous system side effects (2). Loperamide is orally administered and
Effects of olopatadine hydrochloride, a histamine h(1) receptor antagonist, on histamine-induced skin responses.
Effects of olopatadine hydrochloride, a histamine H(1) receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate. Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration. Olopatadine was more effective than fexofenadine and bepotastine. None of the drugs studied impaired performance of word processing tasks. These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration. PMID:20886023
Hashimoto, Takashi; Ishii, Norito; Hamada, Takahiro; Dainichi, Teruki; Karashima, Tadashi; Nakama, Takekuni; Yasumoto, Shinichiro
Effects of Olopatadine Hydrochloride, a Histamine H1 Receptor Antagonist, on Histamine-Induced Skin Responses
Effects of olopatadine hydrochloride, a histamine H1 receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate. Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration. Olopatadine was more effective than fexofenadine and bepotastine. None of the drugs studied impaired performance of word processing tasks. These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration.
Effect of tetracycline hydrochloride treatment on the critical thermal maximum of common shiners
The transfer of fish from field to laboratory facilities or their propagation in closed or restricted systems frequently results in bacterial infection and ultimately large-scale mortality. In attemps to alleviate this problem, we have added tetracycline hydrochloride to the water prophylactically (pretreating tanks before wild fish were added) and therapeutically (treating tanks after bacterial outbreaks were detected.) In the present study, we examined the effect of tetracyline hydrochloride on the critical thermal maximum (CTM) of the common shiner (Notropis cornutus).
Not Available
Preparation and Evaluation of W\\/O\\/W Multiple Emulsion Containing Naltrexone Hydrochloride: A Pilot Study
SUMMARY. W\\/O\\/W multiple emulsions containing naltrexone (NTX) hydrochloride were prepared by a two-step emulsification method at 20 şC. Characterization of the developed system was evaluated and the release kinetics of the drug was determined. The tissue response to the injection of the multiple emulsion in mice was observed by histological analysis. The entrapment efficiency of NTX hydrochloride in W\\/O\\/W multiple
Bérgson F. OLIVEIRA; Ana E. R. FERREIRA; Silvia L. FIALHO; Armando SILVA-CUNHA
Treatment of hyperphosphatemia with sevelamer hydrochloride in hemodialysis patients: A comparison with calcium acetate
Treatment of hyperphosphatemia with sevelamer hydrochloride in hemodialysis patients: A comparison with calcium acetate.BackgroundSevelamer hydrochloride is a recently approved calcium- and aluminium-free phosphate binder. A randomized study comparing sevelamer and calcium acetate was performed to assess the control of hyperphosphatemia in hemodialysis patients.MethodsAdministration of phosphate binders was discontinued during a two-week washout period. The patients were then randomized to receive
José G Hervás; Dolores Prados; Sebastián Cerezo
Acid loading during treatment with sevelamer hydrochloride: Mechanisms and clinical implications
Acid loading during treatment with sevelamer hydrochloride: Mechanisms and clinical implications. Short-term and long-term studies indicate that patients treated with sevelamer hydrochloride have lower serum bicarbonate levels than patients treated with calcium-containing phosphate binders. This observation has previously been attributed to withdrawal of a source of base with discontinuation of calcium carbonate or calcium acetate. However, understanding of the chemistry
BARTON BREZINA; Wajeh Y. Qunibi; Charles R. Nolan
Stability-indicating HPLC Method for Simultaneous Determination of Montelukast and Fexofenadine Hydrochloride
A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v), pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 ?g/ml and 24-120 ?g/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations.
Pankhaniya, Mona; Patel, Parula; Shah, J. S.
Polymeric matrix membrane sensors for stability-indicating potentiometric determination of oxybutynin hydrochloride and flavoxate hydrochloride urogenital system drugs.
Four polyvinyl chloride (PVC) matrix membrane electrodes responsive to 2 drugs affecting the urogenital system--oxybutynin hydrochloride (OX) and flavoxate hydrochloride (FX)--were developed, described, and characterized. A precipitation-based technique with tungstophosphate (TP) and ammonium reineckate (R) anions as electroactive materials in a PVC matrix with an OX cation was used for electrode 1 and 2 fabrication, respectively. Electrode 3 and 4 fabrication was based on use of the precipitation technique of FX cation with tetrakis (4-chlorophenyl) borate and R anions as electroactive materials. Fast and stable Nernstian responses in the range 1 x 10(-2)-1 x 10(-6) M for the 2 drugs over the pH range 5-8 revealed the performance characteristics of these electrodes, which were evaluated according to International Union of Pure and Applied Chemistry recommendations. The method was applied to FX and OX in their pharmaceutical formulations and in human plasma samples. The 4 proposed sensors were found to be specific for the drugs in the presence of up to 60% of their degradation products. Validation of the method according to the quality assurance standards showed suitability of the proposed electrodes for use in the quality control assessment of these drugs. The recoveries for determination of the drugs by the 4 proposed selective electrodes were 99.5 +/- 0.5, 100.0 +/- 0.4, 99.9 +/- 0.4, and 100.1 +/- 0.4% for sensors 1-4, respectively. Statistical comparison between the results obtained by this method and the official method of the drugs was done, and no significant difference found. PMID:19202792
Heba, Mohamed; Ramadan, Nesrin; El-Laithy, Moustafa
Comparative effects of ractopamine hydrochloride and zilpaterol hydrochloride on growth performance, carcass traits, and longissimus tenderness of finishing steers.
Ractopamine hydrochloride (RAC) and zilpaterol hydrochloride (ZH) are beta-adrenergic agonists that improve growth performance and affect carcass characteristics. The objective of this study was to evaluate the comparative effects of RAC and ZH when fed to beef steers during the last 33 d of the finishing period. Three hundred crossbred beef steers (516 +/- 8 kg) were grouped by BW, BCS, and breed type and randomly assigned to 1 of 3 treatments (10 steers per pen; 10 pens per treatment). Treatments were control (no beta-agonists added), RAC (200 mg of ractopaminexhdx(-1)d(-1), for 33 d), or ZH (75 mg of zilpaterolxanimalx(-1)d(-1), for 30 d, removed 3 d for required withdrawal period). Steers were slaughtered, carcass characteristics were evaluated, and cut-out yields were determined. Both RAC and ZH increased final BW, ADG, feed efficiency (G:F), and HCW compared with controls (P < 0.05). Compared with RAC, ZH decreased ADG, ADFI, and final BW, but increased HCW and dressing percentage (P < 0.05). Carcass yield was not affected by RAC in this experiment, whereas ZH decreased adjusted fat thickness and KPH, increased ribeye area, improved yield grade, and increased cut-out yields, when compared with controls (P < 0.05). Marbling, lean maturity, and skeletal maturity were not different between treatments (P > 0.05). Steaks from RAC steers had greater (P < 0.05) Warner-Bratzler shear force (WBSF) values than steaks from control steers at 3 and 7 d of aging, but did not differ from controls after 14 d of aging. Steaks from ZH steers had greater WBSF values (P < 0.05) than steaks from controls and RAC steaks throughout the 21-d postmortem aging period. Although both beta-adrenergic agonists were effective at improving feedlot performance, RAC showed no negative effect on WBSF after 14 d, whereas WBSF values for ZH steaks were significantly greater than controls after 21 d. PMID:20042550
Scramlin, S M; Platter, W J; Gomez, R A; Choat, W T; McKeith, F K; Killefer, J
Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride.
The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3?HCOOC2H5, -CH2?HCOOH and -CH2?HCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed. PMID:23680512
Ba?kan, M Halim; Ayd?n, Murat
Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride
The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3?HCOOC2H5, -CH2?HCOOH and -CH2?HCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed.
Ba?kan, M. Halim; Ayd?n, Murat
Weakly-bridged dimeric diorganotin(IV) compounds derived from pyruvic acid hydrazone Schiff base ligands: Synthesis, characterization and crystal structures
We report the synthesis of four diorganotin(IV) compounds of Schiff base pyruvic acid hydrazone derivatives formulated as [R2SnLY]2, where L1 is 2-SC4H3CON2C(CH3)CO2 with Y = CH3CH2CH2CH2OH, R = n-Bu (1); L2 is C6H5CON2C(CH3)CO2 with Y = CH3CH2OH, R = p-F-Bz (2); L3 is 2-HOC6H4CON2C(CH3)CO2 with YH2O, R = p-CN-Bz (3); and L4 is 4-NO2–C6H4CON2C(CH3)CO2 with YCH3CH2OH, R = Bz (4). The structures of all compounds have been established by a combination of
Min Hong; Han-Dong Yin; Ji-Chun Cui
Synthesis and characterization of di- and tri-organotin(IV) complexes with Schiff base ligand pyruvic acid 3-hydroxy-2-naphthoyl hydrazone
A series of organotin(IV) complexes with Schiff base ligand pyruvic acid 3-hydroxy-2-naphthoyl hydrazone [R2SnLY]2, L=3-HO–C10H6-2-CONHNC(CH3)COOH, R=n-C4H9, Y=CH3OH (1), R=n-C4H9, Y=N (2), R=PhCH2 (3), R=Ph, Y=CH3OH (4), R=Me, (5) and [R3SnLY], L=3-HO–C10H6-2-CONHNC(CH3)COOH, R=n-C4H9, Y=H2O, (6), R=Ph (7), R=Me (8) have been synthesized. These complexes have been characterized by elemental analysis, IR, 1H and 119Sn NMR spectra. The crystal and molecular structure
Han Dong Yin; Shao Wen Chen
The improved ammonia gas sensors constructed by l-glutamic acid hydrochloride on surface acoustic wave devices
The gas sensing properties of l-glutamic acid hydrochloride deposited onto 128° YX-LiNbO3 surface acoustic wave (SAW) delay line are monitored in this study. The sensitivity, response time, reversibility, repeatability, selectivity, and long-term stability of l-glutamic acid hydrochloride are also investigated. The SAW gas sensors based on l-glutamic acid hydrochloride exhibit good sensitivity and reversibility towards ammonia gas, and the results
Chi-Yen Shen; Chun-Pu Huang; Hsu-Chi Chuo
Polymer conjugates of doxorubicin bound through an amide and hydrazone bond: Impact of the carrier structure onto synergistic action in the treatment of solid tumours.
In this study, we describe the synthesis, physico-chemical characterisation and results of the in vitro and in vivo evaluation of the biological behaviour of N-(2-hydroxypropyl)methacrylamide-based (HPMA) copolymer conjugates bearing doxorubicin (DOX) partly bound via a pH-sensitive hydrazone and partly via enzymatically degradable amide bonds, each contributing to a different anti-tumour mechanism of action of the polymer-doxorubicin conjugate. The following two types of HPMA copolymer drug carriers designed for passive tumour targeting were synthesised and compared: the linear non-degradable copolymer and the biodegradable high-molecular-weight (HMW) diblock copolymer. The HMW diblock copolymer carrier containing a degradable disulphide bond between the polymer blocks showed a rapid degradation in a buffer containing glutathione within the first few hours of incubation. In contrast to the conjugate with the amide bond-bound DOX requiring the presence of lysosomal enzymes to release DOX, the polymer-drug conjugate with the DOX bound via a hydrazone bond released DOX by pH-sensitive hydrolysis, which was significantly faster in a buffer of pH 5.0 (intracellular pH) than pH 7.4, mimicking the conditions in the bloodstream. The significant and comparable in vivo anti-tumour activity of the diblock HMW conjugate and an equimolar mixture of the conjugates differing in the DOX attachment method along with the development of cancer resistance during treatment with these conjugates demonstrated the high potential of these compounds in the development of new nanomedicines suitable for the treatment of solid tumours. PMID:24632485
Etrych, Tomáš; Subr, Vladimír; Laga, Richard; Ríhová, Blanka; Ulbrich, Karel
Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate.
The aim of this project was to study the effect of stainless steel solid microneedles and microneedle rollers on percutaneous penetration of verapamil hydrochloride and amlodipine besylate. Verapamil, 2-(3,4-dimethooxyphenyl)-5-[2-(3,4 dimethoxyphenyl)ethyl-methyl-amino]-2-propan-2-yl-pentanenitrile is a calcium channel blocker agent that regulates high blood pressure by decreasing myocardial contractilty, heart rate and impulse conduction. Amlodipine, (R, S)-2-[(2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4-dihydropyridine, is a calcium channel blocker that is used for the management of hypertension and ischemic heart disease. Passive penetration of verapamil and amlodipine across the skin is low. In vitro studies were performed with microneedle-treated porcine ear skin using vertical static Franz diffusion cells (PermeGear, Hellertown, PA, USA). The receiver chamber contained 5ml of PBS (pH7.4) and was constantly maintained at 37°C temperature with a water circulation jacket. The diffusion area of the skin was 1.77cm(2). The donor compartment was loaded with 1ml of the solution containing 2.5mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2h for 12h and analyzed by liquid chromatography-mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75?g/cm(2)/h to 49.96?g/cm(2)/h across microneedle-roller treated porcine skin. Percutaneous flux of amlodipine besylate following the use of stainless steel microneedles was 22.39?g/cm(2)/h. Passive flux for the drug was 1.57?g/cm(2)/h. This enhancement of amlodipine flux was statistically significant. Transdermal flux of amlodipine with microneedle roller was 1.05?g/cm(2)/h in comparison with passive diffusion flux of 0.19?g/cm(2)/h. The difference in flux values was also statistically significant. Stainless steel solid microneedles and microneedle rollers increased percutaneous penetration of verapamil hydrochloride and amlodipine besylate. It may be feasible to develop transdermal microneedle patches for these drugs. PMID:24176676
Kaur, Monika; Ita, Kevin B; Popova, Inna E; Parikh, Sanjai J; Bair, Daniel A
Stability-indicating HPTLC determination of ambroxol hydrochloride in bulk drug and pharmaceutical dosage form.
A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for the analysis of ambroxol hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed HPTLC aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of methanol-triethylamine (4:6 v/v). The system was found to give a compact spot for ambroxol hydrochloride (R(f) value of 0.53 +/- 0.02). Densitometric analysis of ambroxol hydrochloride was carried out in the absorbance mode at 254 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r(2) = 0.9966 +/- 0.0013 with respect to peak area in the concentration range 100-1000 ng/spot. The mean value +/- standard deviation of slope and intercept were 164.85 +/- 0.72 and 1168.3 +/- 8.26 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantitation were 10 and 30 ng/spot, respectively. Ambroxol hydrochloride was subjected to oxidation and thermal degradation. The drug undergoes degradation under oxidation and heat conditions. This indicates that the drug is susceptible to oxidation and heat. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of said drug. Stability indicating of new chemical entities is an important part for the drug development of ambroxol hydrochloride and for its estimation in plasma and other biological fluids; the novel Statistical analysis proves that the method is repeatable and selective for the analysis of ambroxol hydrochloride as bulk drug and in pharmaceutical formulations. The proposed developed HPTLC method can be applied for identification and quantitative determination of ambroxol hydrochloride in bulk drug and dosage forms. This work is to determine the purity of the drug available from the various sources by detecting the related impurities. PMID:20056035
Jain, P S
Compatibility and stability of ondansetron hydrochloride with morphine sulfate and with hydromorphone hydrochloride in 0.9% sodium chloride injection at 4, 22, and 32 degrees C.
The physical compatibility and chemical stability of ondansetron hydrochloride 0.1 and 1 mg/mL with morphine sulfate 1 mg/mL and with hydromorphone hydrochloride 0.5 mg/mL in 0.9% sodium chloride injection were studied. Test solutions of the drugs in 0.9% sodium chloride injection were prepared in triplicate and stored at 4, 22, and 32 degrees C. Samples were removed immediately and at various time points over 31 days and stored at -70 degrees C until analyzed. Physical compatibility was assessed visually and by measuring turbidity with a color-correcting turbidimeter and particle content with a light-obscuration particle sizer and counter. Chemical stability was determined by measuring the concentration of each drug in duplicate with stability-indicating high-performance liquid chromatography. There were no visual or subvisual changes in turbidity or particle content in any of the test solutions at any of the time points. There was little or no loss of any of the drugs. When admixed in 0.9% sodium chloride injection, ondansetron hydrochloride 0.1 and 1 mg/mL plus morphine sulfate 1 mg/mL or hydromorphone hydrochloride 0.5 mg/mL were compatible and stable for at least 7 days at 32 degrees C and for at least 31 days at 4 and 22 degrees C. PMID:7527184
Trissel, L A; Xu, Q; Martinez, J F; Fox, J L
A Double-Blind, Placebo-Controlled Trial of Dexmethylphenidate Hydrochloride and D,l-Threo-Methylphenidate Hydrochloride in Children with Attention-Deficit-Hyperactivity Disorder
Objective: To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin[TM]) for the treatment of attention-deficit/hyperactivity disorder (ADHD) and to test an a priori hypothesis that d-MPH would have a longer duration of action than d,l-threo-methylphenidate (d,l-MPH). Method: This was a randomized, double-blind study…
Wigal, Sharon; Swanson, James M.; Feifel, David; Sangal, R. Bart; Elia, Josephine; Casat, Charles D.; Zeldis, Jerome B.; Conners, C. Keith
Canine periodontal disease control using a clindamycin hydrochloride gel.
Stabilizing or reducing periodontal pocket depth can have a positive influence on the retention of teeth in dogs. A topical 2% clindamycin hydrochloride gel (CHgel) was evaluated for the treatment of periodontal disease in dogs. The CHgel formulation provides for the sustained erosion of the matrix, but also flows into the periodontal pocket as a viscous liquid, and then rapidly forms a gel that has mucoadhesive properties and also may function as a physical barrier to the introduction of bacteria. A professional teeth cleaning procedure including scaling and root planing was done in dogs with one group receiving CHgel following treatment. Periodontal health was determined before and after the procedure including measurement of periodontal pocket depth, gingival index, gingival bleeding sites, and number of suppurating sites. There was a statistically significant decrease in periodontal pocket depth (19%), gingival index (16%), and the number of bleeding sites (64%) at 90-days in dogs receiving CHgel. Additionally, the number of suppurating sites was lower (93%) at 90-days for the group receiving CHgel. The addition of CHgel effectively controlled the bacterial burden (e.g, Fusobacterium nucleatum) at both day 14 and 90. Gingival cells in culture were shown to rapidly incorporate clindamycin and attain saturation in approximately 20-minutes. In summary, a professional teeth cleaning procedure including root planning and the addition of CHgel improves the gingival index and reduces periodontal pocket depth. PMID:22416621
Johnston, Thomas P; Mondal, Pravakar; Pal, Dhananjay; MacGee, Scott; Stromberg, Arnold J; Alur, Hemant
Novel chewable sustained-release tablet containing verapamil hydrochloride.
The aim of this research is to produce a compactable self-sealing chewable tablet of verapamil hydrochloride. Tablets were prepared by compressing beads coated with multiple layers including drug, hydroxypropyl methylcellulose, polyethylene oxide, ethylcellulose, lactose, and sodium starch glycolate. Dissolution studies were carried out according to the USP XXII paddle method for 14 h. A new tablet formulation was evaluated in three different forms: 1) whole tablet, 2) crushed tablet using a commercial tablet crusher, and 3) tablet chewed in the mouth and then expelled into dissolution fluid. Sustained release from the new formulation was maintained and was similar in all three different treatments, and similar to drug release from intact commercially available Isoptin SR, but crushing or chewing destroyed the sustained release property of Isoptin SR (as expected). This new formulation can be administered either by swallowing the whole tablet or by first crushing or chewing the tablet. Controlled release properties of this new formulation do not change by chewing or crushing the tablet first. Such a tablet could be valuable for all patients including those who have difficulty swallowing, such as pediatrics and geriatrics. PMID:15202577
El-Gazayerly, Omaima N; Rakkanka, Vipaporn; Ayres, James W
Preliminary Toxicological Report of Metformin Hydrochloride Loaded Polymeric Nanoparticles
Nanosized materials have tremendous application in every field of human activity, with a lot of economic benefit increasing nanoparticle research and use. There are number of nanosized products already available commercially and many others are in queue. Therefore, there is a pressing need for careful consideration of benefits and side effects of the use of nanoparticles in medicine. This research work aims at providing a balanced update of this exciting potentially toxicological effect of manufactured Metformin hydrochloride loaded polymeric nanoparticles. To assess the toxicities systematically on the functions of various tissues and organs in rats, the rats were fed with the manufactured polymeric nanoparticles for a period of 30 days repeated oral administration. Variation in the protein, carbohydrate and fat metabolic profile of the rat exposed to nanoparticles were studied by hematobiochemical and pathology profiles. The haemolytic potential of these nanoparticles were determined by means of an in vitro haemolysis assay. All formulations showed haemolytic effect less than 5%. The study revealed that Metformin loaded PMMA and PLGA polymeric nanoparticle did not produce any toxicity.
Lekshmi, Unnikrishnan Meenakshi Dhana; Reddy, Pully Neelakanta
Properties of melarsamine hydrochloride (Cymelarsan) in aqueous solution.
The antitrypanosomal drug melarsamine hydrochloride (MelCy) (trade name, Cymelarsan) is a melamino-phenylarsine made by conjugation of one equivalent of melarsen oxide and two equivalents of cysteamine. Immediately after it was dissolved in water, the compound was found to exist as an equilibrium mixture containing MelCy (43%), MelCy which had lost one cysteamine moiety (MelCy -1; 24%), melarsen oxide (33%), and free cysteamine. Small amounts (< 1%) of the oxidation products derived from the last two components were also formed (cystamine and sodium melarsen). On incubation at room temperature, the MelCy content decreased steadily, with an associated increase in the melarsen oxide and sodium melarsen contents. After 5 days in solution at room temperature, 27% of the arsenical agent was MelCy, 14% was MelCy -1, 42% was melarsen oxide, and 17% was sodium melarsen. Since H2O2 production was detectable in MelCy or cysteamine solutions and the addition of small amounts of exogenous H2O2 readily converted the trivalent melarsen oxide to the pentavalent sodium melarsen, it is hypothesized that the nonenzymatic conversion of cysteamine to cystamine produced H2O2, which then oxidized melarsen oxide to sodium melarsen. Similar time course experiments showed that melarsonyl potassium and melarsoprol were more stable in solution.
Berger, B J; Fairlamb, A H
Kinetics of degradation of imidapril hydrochloride in finished dosage formulations.
This study investigates the impact of relative air humidity and temperature on the stability of imidapril hydrochloride (IMD) tablets. For this purpose the forced degradation test was used and the following environmental conditions were employed: RH = 76.4% and the temperature range of 313 - 333 K. For the determination of IMD content in the analyzed samples a reversed-phase high performance liquid chromatography (RP-HPLC) technique was used. Three series of tablets were prepared: whole-blistered tablets, whole-bare tablets and halved-bare tablets, in order to analyze the influence of different in-home storage habits on IMD tablets' quality. In the course of the study, the degradation of IMD was observed in each series of tablets. The kinetic mechanisms and the thermodynamic parameters of these reactions were established. It was evidenced that halved IMD tablets stored without immediate packaging retain their quality only for 12 days while tablets stored according to label recommendations are stable for 513 days. PMID:23923397
Stanisz, Beata; Regulska, Katarzyna
Simple and sensitive spectrophotometric methods for determination of amantadine hydrochloride
Three simple and sensitive spectrophotometric methods (A-C) for determination of amantadine hydro-chloride have been developed and validated. The first method (A) is based on the oxidation of the drug by ammonium molybdate. The second method (B) was based on the charge-transfer complexation reaction between the amantadine base as an electron donor and iodine as a ?-acceptor. The third method (C) is based on the reaction of N-alkylvinylamine formed from the interaction of the free amino group in amantadine molecule and acetalde-hyde with chloranil to give colored vinylamino-substituted benzoquinone. The colored products of these reactions were measured at their corresponding maximum absorption peaks. Different variables affecting the reactions were carefully studied and optimized. Under the optimum conditions, linear relationships with good correlation coefficients 0.9993-0.9998 were found between the reading and the corresponding concentration of the drug in the range 2-90 µg·ml-1. The limits of detection ranged from 0.16 to 1.91 µg·ml-1. The precision of the methods was satisfactory: the values of relative standard deviation did not exceed 1.63%. The proposed methods were successfully applied to the analysis of amantadine HCl in its capsules with good accuracy and precision; the label claim percentages ranged from 99.8 to 100.5 ± (0.52-1.22) %. The results obtained by the proposed spectrophotometric methods were comparable with those obtained by the official method.
Darwish, I. A.; Khedr, A. S.; Askal, H. F.; Mahmoud, R. M.
Characteristics of amorphous complex formed between indomethacin and lidocaine hydrochloride.
Indomethacin (IM) easily forms an amorphous complex with lidocaine (LC) by heat treatment. To know the mechanism involved in the formation of this complex, we studied temperature-dependent phase changes in mixtures of IM and lidocaine hydrochloride (LH), in which the cationic form of LC forms a salt with Cl(-), in various molar ratios by using DSC and NMR. Although heating of the mixture of IM and LC (IM+LC), formed a eutectic mixture, that of IM and LH (IM+LH) did not, and IM in the IM+LH mixture was dissolved into fused LH. Cooling of the fused IM+LH showed the glass transition in all of the samples containing various amounts of IM, suggesting that fused IM+LH took a homogenous amorphous state (IM/LH) below its glass transition temperature, in contrast to the fused IM+LC, which formed the rubber state and/or glass state depending on the molar content of IM. The results of the NMR study showed that IM in IM/LH caused the electronic structure of LH to change in such a way as to become similar to that of LC, but this effect was limited. Hence, mode of interaction of LH with IM is different from that of LC with IM. PMID:23352941
Shimada, Yohsuke; Goto, Satoru; Uchiro, Hiromi; Hirota, Keiji; Terada, Hiroshi
Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride.
A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 microg ml(-1) respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml(-1) for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method. PMID:12396035
Amin, A S; Dessouki, H A
Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride
A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 ?g ml -1, respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml -1 for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method.
Amin, A. S.; Dessouki, H. A.
Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study.
The Biopharmaceutics Classification System (BCS) represents the framework for predicting the intestinal drug absorption based on its solubility and intestinal permeability. Recent research has lead to the use of in vitro tests to waive additional in vivo bioequivalence studies for some pharmaceutical products (i.e., biowaiver). The current regulations permit waivers for BCS Class I (highly soluble/highly permeable) drug substances, which represent up to 25% of the drugs. Efforts in both the science and regulatory bodies are being made to extend biowaivers to certain Class II and III products, which would represent more than 50% of all drugs coming to the market. The aim of this study was to investigate the influence of experimental conditions on metformin hydrochloride (CAS 1115-70-4) release from two immediate-release tablet formulations with proven bioequivalence and justify the biowaiver request for dissolution profile similarity in three pH media. The results obtained indicate that differences in drug dissolution observed in vitro were not reflected in vivo. Such data support the existing idea that BCS Class III drugs are eligible biowaiver candidates, even if a very rapid dissolution criterion is not fulfilled. PMID:21117498
Homsek, Irena; Parojci?, Jelena; Dacevi?, Mirjana; Petrovi?, Ljiljana; Jovanovi?, Dusan
Spectrophotometric estimation of tamsulosin hydrochloride by acid-dye method
A new spectrophotometric method for the estimation of tamsulosin hydrochloride in pharmaceutical dosage forms has been developed and validated. The method is based on reaction between drug and bromophenol blue and complex was measured at 421 nm. The slope, intercept and correlation coefficient was found to be 0.054, -0.020 and 0.999, respectively. Method was validated in terms of specificity, linearity, range, precision and accuracy. The developed method can be used to determine drug in both tablet and capsule formulations. Reaction was optimized using three parameters i.e., concentration of the dye, pH of the buffer, volume of the buffer and shaking time. Maximum stability of the chromophore was achieved by using pH 2 and 2 ml volume of buffer. Shaking time kept was 2 min and concentration of the dye used was 2 ml of 0.05% w/v solution. Method was validated in terms of linearity, precision, range, accuracy, LOD and LOQ and stochiometry of the method was also established using Mole ratio and Job's method of continuous variation. The dye benzonoid form (blue color) of dye ionized into quinonoid form (purple color) in presence of buffer and reacts with protonated form of drug in 1:1 ratio and forms an ion-pair complex (yellow color).
Shrivastava, Alankar; Saxena, Prachi; Gupta, Vipin B.
Flow injection chemiluminescence determination of naphazoline hydrochloride in pharmaceuticals.
A simple and sensitive flow injection chemiluminescence (FI-CL) method was developed for the determination of naphazoline hydrochloride (NPZ). The method is based on the enhancing effect of NPZ on the weak CL signal from the reaction of KIO4 with H2 O2 . Experimental parameters that affected the CL signal, including the pH of the KIO4 solution, concentrations of KIO4 , H2 O2 and disodium-EDTA and flow rate were optimized. Under the optimum conditions, the increment of CL intensity was linearly proportional to the concentration of NPZ in the range 5.0 × 10(-6) to 70 × 10(-6) mol/L. The detection limit was 1.0 × 10(-6) mol/L and the relative standard deviation for 50 × 10(-6) mol/L NPZ solution was 2.8% (n = 11). In addition, a high throughput of 120 samples/h was achieved. The utility of this method was demonstrated by determining NPZ in pharmaceuticals. PMID:23463582
Iranifam, Mortaza; Sorouraddin, Mohammad H
Physical characteristics and chemical degradation of amorphous quinapril hydrochloride.
This study was designed to investigate the relationships between the solid-state chemical instability and physical characteristics of a model drug, quinapril hydrochloride (QHCl), in the amorphous state. Amorphous QHCl samples were prepared by rapid evaporation from dichloromethane solution and by grinding and subsequent heating of the crystalline form. Physical characteristics, including the glass transition temperature and molecular mobility, were determined using differential scanning calorimetry, thermogravimetric analysis, powder x-ray diffractometry, polarizing microscopy, scanning electron microscopy, and infrared spectroscopy. The amorphous form of QHCl, produced by both methods, has a T(g) of 91 degrees C. Isothermal degradation studies showed that cyclization of QHCl occurred at the same rate for amorphous samples prepared by the two methods. The activation energy was determined to be 30 to 35 kcal/mol. The rate of the reaction was shown to be affected by sample weight, dilution through mixing with another solid, and by altering the pressure above the sample. The temperature dependence for chemical reactivity below T(g) correlated very closely with the temperature dependence of molecular mobility. Above T(g), however, the reaction was considerably slower than predicted from molecular mobility. From an analysis of all data, it appears that agglomeration and sintering of particles caused by softening of the solid, particularly above T(g), and a resulting reduction of the particle surface/volume ratio play a major role in affecting the reaction rate by decreasing the rate of removal of the gaseous HCl product. PMID:10664545
Guo, Y; Byrn, S R; Zografi, G
Potential beneficial role of sevelamer hydrochloride in diabetic retinopathy.
Patients with chronic kidney disease (CKD) experience co-morbid illnesses, including cardiovascular disease and retinopathy. Sevelamer hydrochloride (Renagel®); a non-calcium phosphate binder reduces coronary artery and aortic calcification as compared to calcium containing phosphate binders and additionally effects inflammatory biomarkers such as C-reactive protein (CRP), and lowers LDL cholesterol in patients with CKD. Since retinopathy is proven to be associated with increased coronary calcification, shared pathophysiological processes may contribute to both microvascular and macrovascular disease. We here suggest three different mechanisms of possible sevelamer's influence on the retinopathy: (1) by direct effect on the microvasculature through lowering CRP and LDL, involved in endothelial dysfunction and atherogenesis, (2) indirectly by attenuation of vascular calcification of aorta and carotid internal artery, it reduces ischaemia and improves circulation in the opthalmic artery and hence postponing retinopathy, (3) through hypertension by reducing atherosclerosis and calcification of carotid arteries, sevelamer decreases stiffness and intima-media wall thickness, therefore lowering blood pressure, which is well known to increase progression of diabetic retinopathy. So far no studies have yet been published on the direct influence of sevelamer on the retinopathy which we believe has good theoretical background. With its combined macrovascular and microvascular effect, sevelamer could potentially postpone and/or decrease retinopathy in diabetic patients with hypertension, and that are on hemodialysis or even predialysis patients. PMID:23357670
Draca, Natasa; Lazic, Ratimir; Simic, Petra; Dumic-Cule, Ivo; Luetic, Ana Tikvica; Gabric, Nikica
Ranitidine Hydrochloride-loaded Ethyl Cellulose and Eudragit RS 100 Buoyant Microspheres: Effect of pH Modifiers
A floating type of dosage form of ranitidine hydrochloride in the form of microspheres capable of floating on simulated gastric fluid was prepared by solvent evaporation technique. Microspheres prepared with ethyl cellulose, Eudragit® RS100 alone or in combination were evaluated for percent yield, drug entrapment, percent buoyancy and drug release and the results demonstrated satisfactory performance. Microspheres exhibited ranitidine hydrochloride release influenced by changing ranitidine hydrochloride-polymer and ranitidine hydrochloride-polymer-polymer ratio. Incorporation of a pH modifier has been the usual strategy employed to enhance the dissolution rate of weakly basic drug from floating microspheres. Further citric acid, fumaric acid, tartaric acid were employed as pH modifiers. Microspheres prepared with ethyl cellulose, Eudragit® RS100 and their combination that showed highest release were utilized to study the effect of pH modifiers on ranitidine hydrochloride release from microspheres which is mainly affected due to modulation of microenvironmental pH. In vitro release of ranitidine hydrochloride from microspheres into simulated gastric fluid at 37° showed no significant burst effect. However the amount of release increased with time and significantly enhanced by pH modifiers. 15% w/w concentration of fumaric acid provide significant drug release from ranitidine hydrochloride microspheres prepared with ranitidine hydrochloride:ethyl cellulose (1:3), ranitidine hydrochloride:Eudragit® RS100 (1:2) and ranitidine hydrochloride:ethyl cellulose:Eudragit® RS100 (1:2:1) whereas citric acid, tartaric acid showed significant cumulative release at 20% w/w. In all this study suggest that ethyl celluose, Eudragit® RS100 alone or in combination with added pH modifiers can be useful in floating microspheres which can be proved beneficial to enhance the bioavailability of ranitidine hydrochloride.
Kotagale, N. R.; Parkhe, A. P.; Jumde, A. B.; Khandelwal, H. M.; Umekar, M. J.
Synthesis of thiophene-2-carbaldehyde-(7-methyl-1,3-benzothiazol-2-yl)hydrazone and its application as an ionophore in the construction of a novel thulium(III) selective membrane sensor
In this work we describe the construction, performance, and applications of a novel thulium(III). The sensor is based on thiophene-2-carbaldehyde-(7-methyl-1,3-benzothiazol-2-yl)hydrazone (TCMH), which acts as an excellent carrier, when used in plasticized poly (vinyl chloride) PVC matrix. The influences of different parameters like the membrane composition and pH of the sample solution on the potentiometric response of the sensor were also
Mohammad Reza Ganjali; Solmaz Rasoolipour; Morteza Rezapour; Parviz Norouzi; Mehdi Adib
The pre- and post-natal toxicity of penequine hydrochloride in mice.
Penequine hydrochloride, a novel anticholinergic agent, was developed as an effective treatment for organophosphorus intoxication (e.g., soman poisoning). The current study was performed to assess the potential pre- and post-natal toxicity of penequine hydrochloride in mice. Approximately 120 timed-pregnant mice were assigned to four dose groups (n=30 per group). Dams were exposed orally to 0, 2.5, 12.5, 62.5 mg/L penequine hydrochloride in drinking water from gestation day 6 to lactation day 21. The F1 generation mice, which were not exposed directly to penequine hydrochloride as pups or as adults, were bred to produce F2 generation fetuses for the fertility test of the F1 population. Various pre- and post-natal measurements, including neurobehavioral tests, were performed with the F0 and F1 mice. Among the significant findings were decreases in water consumption, viability, organ weights and delay of physical landmarks in 62.5 mg/L groups. With the exception of treatment-unrelated abnormality in surface righting reflex in the F1 generation, penequine hydrochloride did not produce any adverse effects at doses up to and including 12.5 mg/L (equal to 2.5 mg/kg/day in mice) that were at least 75 times of human therapeutic dosage. PMID:16777373
Zhang, Zibo; Zhang, Qinglin; Huang, Chunqian; Jin, Hongtao; Wang, Zhiqiao; Wang, Aiping
Formulation and Evaluation of S-(-)-Amlodipine Besylate and Nebivolol Hydrochloride Tablets
The objective of the present study was to develop a tablet formulation of S-(-)-amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-)- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity. The study was also carried out to design a suitable dissolution medium for S-(-) - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(-) - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(-) - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.
Shaikh, S.A; Shaikh, S.S; Shahi, S.R.; Shookur, M.A.; Reddy, L.K; Padalkar, A.N; Thube, Mahesh
Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories: interlaboratory study.
A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by 8 laboratories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbance of the minima at about 389 and 412 nm. Each collaborator received 4 creams (0.2%), 1 jel (0.2%), 1 molded suppository (6 mg/3.198 g), and 2 gelatin-encapsulated suppository samples (12 mg/6.661 g and 14 mg/6.863 g). The cream samples included blind duplicates prepared to contain 0.212% aminacrine hydrochloride, 15% sulfanilamide, and 2% allantoin. Mean recovery for the authentic cream was 104.7% with a coefficient of variation (CV) of 9.22%. The commercial products contained these respective amounts (CVs): creams, 100.0% (2.48%) and 101.5% (2.16%); jel, 118.0% (9.58%); molded suppository, 102.7% (1.88%); and gelatin encapsulated suppositories, 93.1% (1.0%) and 94.3% (1.60%). Standard aminacrine hydrochloride provided for the study was 99.6% pure by nonaqueous titration. Thin layer chromatographic identification of aminacrine hydrochloride was also tested collaboratively. The method was not adopted by AOAC. PMID:3610970
Development and in vitro evaluation of chitosan-based transdermal drug delivery systems for the controlled delivery of propranolol hydrochloride
Membrane permeation-controlled transdermal drug delivery systems were prepared using the natural polymer, chitosan. An adhesive sealing technique was used to construct the devices. Propranolol hydrochloride was selected as the model drug for the present study. Chitosan membranes with different permeability to propranolol hydrochloride obtained by controlled cross-linking with glutaraldehyde were used to regulate the drug release in the devices. Chitosan
D. Thacharodi; K. Panduranga Rao
Raman spectroscopic investigation of cocaine hydrochloride on human nail in a forensic context.
This study describes the application of Raman spectroscopy to the detection of drugs of abuse and noncontrolled substances used in the adulteration of drugs of abuse on human nail. Contamination of the nail may result from handling or abusing these substances. Raman spectra of pure cocaine hydrochloride, a seized street sample of cocaine hydrochloride (77%), and paracetamol could be acquired from drug crystals on the surface of the nail. An added difficulty in the analytical procedure is afforded by the presence of a nail varnish coating the nail fragment. By using confocal Raman spectroscopy, spectra of the drugs under nail varnish could be acquired. Spectra of the drugs could be readily obtained nondestructively within three minutes with little or no sample preparation. Raman spectra could be acquired from drug particles with an average size of 5-20 microm. Acquisition of Raman point maps of crystals from both pure and street samples of cocaine hydrochloride under nail varnish is also reported. PMID:18172621
Ali, Esam M A; Edwards, Howell G M; Hargreaves, Michael D; Scowen, Ian J
[Pyridoxine Hydrochloride Reference Standard (Control 871) of National Institute of Hygienic Sciences].
The raw material of pyridoxine hydrochloride was examined for the preparation of "Pyridoxine Hydrochloride Reference Standard". Analytical data for the sample were as follows: loss on drying is 0.01%; pH 2.94; melting point 205.2 degrees C (decomposition); IR spectrum same as the Pyridoxine Hydrochloride Reference Standard (Control 801); TLC indicates no impurities; nitrogen is 6.77% (Theoretical value 6.81%); and assay 99.5% by non-aqueous titration, 99.8% by UV spectroscopy, and 100.2% by measuring chloride ion. Based on the above results, this raw material was authorized to be Reference Standard of National Institute of Hygienic Sciences. PMID:2636926
Okada, S; Hiroshige, R; Tanaka, M; Murai, M; Tokunaga, H; Kimura, T
RP - HPLC method for the estimation of Tamsulosin Hydrochloride in Tablet Dosage Form.
A rapid and sensitive reverse phase RP-HPLC method is proposed for the estimation of tamsulosin hydrochloride in tablets. Tamsulosin hydrochloride was chromatographed on a reverse phase C18 column with a mobile phase consisting of acetonitrile and water in the ratio of 50:50 v/v. The mobile phase was pumped at a flow rate of 1.5 ml/min. The eluents were monitored at 214 nm. The retention time of the drug was 1.7 min. With this method, linearity was observed between area under curve and concentration of tamsulosin hydrochloride in the injected solution, in the range of 5 to 100 ?g/ml. The method was found to be applicable for analysis of the drug in tablets. The results were validated statistically. PMID:21969754
Kumari, Richa; Dash, P P; Lal, V K; Mishra, A; Murthy, P N
Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection
Photoacoustic imaging (PAI) was employed to detect small animal brain activation after the administration of cocaine hydrochloride. Sprague Dawley rats were injected with different concentrations (2.5, 3.0, and 5.0 mg per kg body) of cocaine hydrochloride in saline solution through tail veins. The brain functional response to the injection was monitored by photoacoustic tomography (PAT) system with horizontal scanning of cerebral cortex of rat brain. Photoacoustic microscopy (PAM) was also used for coronal view images. The modified PAT system used multiple ultrasonic detectors to reduce the scanning time and maintain a good signal-to-noise ratio (SNR). The measured photoacoustic signal changes confirmed that cocaine hydrochloride injection excited high blood volume in brain. This result shows PAI can be used to monitor drug abuse-induced brain activation.
Jo, Janggun; Yang, Xinmai
Interactions between drug substances and excipients. 1. Fluorescence and HPLC studies of triazolophthalazine derivatives from hydralazine hydrochloride and starch.
The strength of hydralazine hydrochloride (I) 10 mg tablets, containing starch as an excipient, decreases significantly with time. An investigation to determine the basis for the drop in strength showed that starch exposed to the drug exhibited fluorescence at 414 nm. As model compounds IIIa and V, which contain a triazolophthalazinyl moiety, also fluoresce at about 414 nm, it is proposed that the emission is due to a triazolophthalazine derivative (IIIc) resulting from hydralazine hydrochloride and starch. Degradation of IIIc generates s-triazolo[3,4-a]phthalazine (IIIb), and a small amount of IIIb is detected in aged tablets. IIIc in aged tablets can be converted to IIIb by acid-catalyzed hydrolysis. The quantity of IIIb determined by HPLC amounts to most of the "missing" hydralazine hydrochloride. The reaction between hydralazine hydrochloride and starch is believed to cause the unexpected drop in the strength of hydralazine hydrochloride tablets. PMID:8699338
Lessen, T; Zhao, D C
Nortriptyline hydrochloride skin absorption: development of a transdermal patch.
The influence of propylen glycol (PG), ethanol, and oleic acid (OA) on nortriptyline hydrochloride (NTH) penetration through human epidermis was studied in vitro at two different pH values (5.5 and 7.4). The influence of lactic acid and polysorbate 80 was studied for a pH of 5.5. Permeation studies through Heat Separated Epidermis, as well as the enhancing effect of the different vehicles, showed a pH dependency. A pH value of 5.5 in the donor solution decreases significantly the permeability coefficient (Kp) with respect to a pH value of 7.4 (0.011+/-0.004 x 10(-6) versus 0.36+/-0.04 x 10(-6)cm/s). The vehicles showed an increasing enhancement effect in the order: polysorbate 80>ethanol/PG/OA>PG>ethanol>ethanol/lactic acid>lactic acid at pH 5.5 while they reduced the permeation of NTH at pH 7.4. Considering the results obtained at pH 5.5, the maximum enhancement ratios were found for polysorbate 80 and the combination ethanol/PG/OA (10.72 and 3.90). Both vehicles were selected for designing a NTH transdermal delivery system (NTH-TDS) using (hydroxypropyl)methyl-cellulose as polymer. The NTH-TDS based on the combination of ethanol/PG/OA showed an enhancement ratio with respect to control of 2.09 and the addition of polysorbate 80 to the matrix, of 5.82. PMID:18191555
Melero, Ana; Garrigues, T M; Almudever, P; Villodre, A Marti N; Lehr, C M; Schäfer, U
Effect of Chemical Enhancers in Transdermal Permeation of Alfuzosin Hydrochloride
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q24) of 702.28 ± 6.97??g/cm2 and 702.74 ± 7.49??g/cm2, respectively. A flux rate of 31.08 ± 0.21??g/cm2/hr by Transcutol 20% and 30.38 ± 0.18??g/cm2/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05?hr. The lowest skin content of 342.33 ± 5.30??g/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.
Prasanthi, D.; Lakshmi, P. K.
Impurity profiling of methamphetamine hydrochloride drugs seized in the Philippines.
Methamphetamine hydrochloride is one of the most widely used illicit drugs in the Philippines. In this study, we describe the application of cluster analysis of trace impurities in the profiling of the seized methamphetamine drug samples. Thirty milligrams of a homogenized drug sample were dissolved in 1 mL of pH 10.5 buffer solution and extracted with ethyl acetate containing three internal standards. The trace impurities were identified using gas chromatography-mass spectrometry (GC-MS) and quantified by gas chromatography with a flame ionization detector (GC-FID). Following previously reported methodologies, 30 impurity peaks were selected from the GC-FID chromatograms. The peak areas and retention times were referenced to the internal standards. The peak areas of the selected peaks were then grouped for cluster analysis. In order to check for consistency of clustering, two further cluster analyses were performed using 40 and 50 impurity peaks. Changes in clustering were observed in going from 30 to 40 impurity peaks, while analyses using 40 and 50 impurity peaks gave similar results. Thus, for the seized drug samples used in this study, cluster analysis using at least 40 impurity peaks showed better consistency of clustering as compared to analysis using 30 peaks only. Ten of the impurity peaks were identified, of which four were identified for the first time in methamphetamine drug samples. These are p-bromotoluene, N-benzyl amphetamine, N-ethyl amphetamine, and N-ethyl methamphetamine. The presence of phenyl-2-propanone (P2P), N,N-dimethyl amphetamine, and N-formyl amphetamine is indicative that these casework samples were synthesized using the Leuckart method. PMID:15240018
Dayrit, Fabian M; Dumlao, Morphy C
Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride.
Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. The aim of this study was to design lercanidipine hydrochloride-loaded nanostructured lipid carriers to investigate whether the bioavailability of the same can be improved by oral delivery. Lercanidipine hydrochloride nanostructured lipid carriers were prepared by the method of solvent evaporation at a high temperature and solidification by freeze drying. The nanostructured lipid carriers were evaluated for particle size analysis, zeta potential, entrapment efficiency, in vitro drug diffusion, ex vivo permeation studies and pharmacodynamic study. The resultant nanostructured lipid carriers had a mean size of 214.97 nm and a zeta potential of -31.6 ± 1.5 mV. More than 70% lercanidipine hydrochloride was entrapped in the NLCs. The SEM studies indicated the formation of type 2 nanostructured lipid carriers. The in vitro release studies demonstrated 19.36% release in acidic buffer pH 1.2 indicating that the drug entrapped in the nanostructured lipid carriers remains entrapped at acidic pH. The ex vivo studies indicated that the drug release was enhanced from 10% to 60.54% at blood pH in 24h. The in vivo pharmacodynamic study showed that NLCs released lercanidipine hydrochloride in a controlled manner for a prolonged period of time as compared to plain drug. These results clearly indicate that nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension. PMID:24445002
Ranpise, Nisharani S; Korabu, Swati S; Ghodake, Vinod N
A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations
Background: Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. Materials and Method: In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Harmonization (ICH) guidelines. The method employed thin layer chromatography aluminum sheets precoated with silica gel as the stationary phase and the mobile phase consisted of chloroform:methanol:ammonia (97:3:0.2), which gave compact bands of yohimbine hydrochloride. Results: Linear regression data for the calibration curves of standard yohimbine hydrochloride showed a good linear relationship over a concentration range of 80–1000 ng/spot with respect to the area and correlation coefficient (R2) was 0.9965. The method was evaluated regarding accuracy, precision, selectivity, and robustness. Limits of detection and quantitation were recorded as 5 and 40 ng/spot, respectively. The proposed method efficiently separated yohimbine hydrochloride from other components even in complex mixture containing powdered plants. The amount of yohimbine hydrochloride ranged from 2.3 to 5.2 mg/tablet or capsule in preparations containing the pure alkaloid, while it varied from zero (0) to 1.5–1.8 mg/capsule in dietary supplements containing powdered yohimbe bark. Conclusion: We concluded that this method employing high performance thin layer chromatography (HPTLC) in quantitative determination of yohimbine hydrochloride in pharmaceutical preparations is efficient, simple, accurate, and validated.
Badr, Jihan M.
The compatibility and stability of octreotide acetate in the presence of diamorphine hydrochloride in polypropylene syringes.
Varying concentrations of octreotide acetate (Sandostatin) and diamorphine hydrochloride were prepared and stored in polypropylene syringes at 37 degrees C in the dark. The solutions were analysed for octreotide acetate content using a validated HPLC method at regular intervals over a 48-h period. The results indicate that octreotide acetate remains stable in the presence of diamorphine hydrochloride at 37 degrees C for 24 h. In addition, the solutions prepared maintained their clarity, with no signs of precipitation upon visual examination under normal light conditions. PMID:10858828
Fielding, H; Kyaterekera, N; Skellern, G G; Tettey, J N; McDade, J R; Msuya, Z; Watson, D G; Urie, J
Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance.
Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm×4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). The identification of these impurities should be useful for quality control in the manufacture of barnidipine. PMID:24451253
Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya
High performance thin layer chromatographic method for simultaneous estimation of Ibuprofen and pseudoephedrine hydrochloride.
High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F(254) plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v) as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively. PMID:20046759
Chitlange, S S; Sakarkar, D M; Wankhede, S B; Wadodkar, S G
Copper-catalyzed synthesis of primary arylamines via cascade reactions of aryl halides with amidine hydrochlorides.
We have developed an efficient method for the synthesis of primary arylamines from aryl halides using amidine hydrochlorides as the ammonia surrogates. The protocol uses 10 mol % CuI as the catalyst, 20 mol % L-proline as the ligand, Cs2CO3 as the base, and DMF as the solvent and proceeds the sequential coupling of aryl halides with amidine hydrochlorides and hydrolysis of intermediates to give the target products. This is a convenient, inexpensive, and practical approach to primary arylamines. PMID:18662031
Gao, Xiaoting; Fu, Hua; Qiao, Renzhong; Jiang, Yuyang; Zhao, Yufen
HPLC method for estimation of metformin hydrochloride in formulated microspheres and tablet dosage form.
A simple, accurate, economical and reproducible HPLC method has been developed for quantitative estimation of metformin hydrochloride from tablet dosage form and formulated microspheres. The developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile:phosphate buffer (65:35) pH adjusted to 5.75 with o-phosphoric acid as mobile phase and glipizide as internal standard. The linearity was observed in concentration range of 0-25 mug/ml for metformin hydrochloride. Results of analysis were validated statistically and by recovery studies. PMID:20490303
Kar, Mousumi; Choudhury, P K
[Bioequivalence of a new tablet formulation of sotalol hydrochloride in comparison to a standard preparations].
Bioequivalence of a New Sotalol Hydrochloride Tablet Formulation Compared with a Standard Preparation An investigation on the bioavailability of a new tablet with 80 mg sotalol hydrochloride (Rentibloc mite, CAS 959-24-0) was performed in a two-way cross-over study with 16 persons. The relative bioavailability with respect to a reference preparation for AUC0-infinity was 101.9% and for Cmax 104.5%. A positive decision for bioequivalence derived from the usual confidence intervals for both parameters. The difference in tmax showed no clinical relevance. The new formulation is bioequivalent to the reference. PMID:8024627
Herrmann, R; Kleinbloesem, C H
LC determination of octreotide acetate in compound formulations of Sandostatin ® and diamorphine hydrochloride
The determination of octreotide acetate in compound formulations of Sandostatin® and diamorphine hydrochloride by RP–LC is described. Octreotide acetate, diamorphine hydrochloride and their respective degradants, [des-Thr-ol8]-octreotide and 6-O-acetylmorphine, were baseline resolved using a Lichrospher-60 RP-select B column with a mobile phase composition of acetonitrile\\/phosphate buffer (pH 7.4, 20 mM) (35:65 v\\/v) with UV detection at 210 nm. The method is
N Kyaterekera; J. N. A Tettey; G. G Skellern; D. G Watson; J Urie; J. R McDade; H Fielding
Synthesis, structural features, absorption spectra, redox behaviour and luminescence properties of ruthenium(ii) rack-type dinuclear complexes with ditopic, hydrazone-based ligands.
The isomeric bis(tridentate) hydrazone ligand strands 1 a-c react with [Ru(terpy)Cl3] (terpy=2,2':6',2''-terpyridine) to give dinuclear rack-type compounds 2 a-c, which were characterised by several techniques, including X-ray crystallography and NMR methods. The absorption spectra, redox behaviour and luminescence properties (both in fluid solution at room temperature and in rigid matrix at 77 K) of the ligand strands 1 a-c and of the metal complexes 2 a-c have been studied. Compounds 1 a-c exhibit absorption spectra dominated by intense pi-pi* bands, which, in the case of 1 b and 1 c, extend within the visible region, while the absorption spectra of the rack-type complexes 2 a-c show intense bands both the in the UV region, due to spin-allowed ligand-centred (LC) transitions, and in the visible, due to spin-allowed metal-to-ligand charge-transfer (MLCT) transitions. The energy position of these bands strongly depends on the ligand strand: in the case of 2 a, the lowest energy MLCT band is around 470 nm, while in 2 b and 2 c, it lies beyond 600 nm. Ligands 1 a-c undergo oxidation processes that involve orbitals based mainly on the CH3--N--N== fragments. The complexes 2 a-c undergo reversible metal-centred oxidation, while reductions involve the hydrazone-based ligands: in 2 b and 2 c, the bridging ligand is reduced twice and in 2 a once before reduction of the peripheral terpy ligands takes place. Ligands 1 a-c exhibit luminescence from the lowest-lying 1pi-pi* level. Only for complex 2 a does emission occur; this may be attributed to a 3MLCT state involving the bridging ligand. Taken together, the results clearly indicate that the structural variations introduced translate into interesting differences in the spectroscopic, luminescence and redox properties of the ligand strands as well as of the rack-type metal complexes. PMID:15844135
Stadler, Adrian-Mihail; Puntoriero, Fausto; Campagna, Sebastiano; Kyritsakas, Nathalie; Welter, Richard; Lehn, Jean-Marie
Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.
Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate. Dexmethylphenidate has been found to be effective and well tolerated in clinical trials, involving a total of 684 children with ADHD and in 15 healthy adult volunteers. Dexmethylphenidate is a schedule II drug. PMID:12455205
Tautomeric effect of hydrazone Schiff bases in tetranuclear Cu(II) complexes: magnetism and catalytic activity towards mild hydrocarboxylation of alkanes.
Three new tetranuclear copper(II) complexes [Cu(HL(1))]4·4EtOH (1·4EtOH), [Cu(HL(2))]4 (2) and [Cu(H2L(3))]4(NO3)4·2H2O (3·2H2O) have been synthesized using three different hydrazone Schiff base ligands derived from the condensation of the aromatic acid hydrazides 2-hydroxybenzo-, 2-aminobenzo- or benzo-hydrazide, with 2,3-dihydroxybenzaldehyde. Complexes 1 and 3 have been characterized by single crystal X-ray diffraction analysis. The coordinating behaviour of the ligand depends on the nature of the ortho substituent present in the hydrazide moiety. The ligands bearing a strong electron donating group (by resonance) in the ortho position undergo complexation via enolization and deprotonation, whereas the absence of such an effect leads to complexation via the keto form, and two different types of tetranuclear Cu(II) clusters, viz. open-cubane and cubane, are obtained. Variable temperature magnetic susceptibility measurements of complexes 1 and 3 have been carried out to examine the nature of magnetic interaction between the Cu(II) centres. All the three complexes (1-3) act as good catalyst precursors towards mild hydrocarboxylation of linear and cyclic alkanes into carboxylic acids in water-acetonitrile medium. PMID:24068161
Sutradhar, Manas; Kirillova, Marina V; Guedes da Silva, M Fátima C; Liu, Cai-Ming; Pombeiro, Armando J L
Reactivity Differences between [alpha, beta]-Unsaturated Carbonyls and Hydrazones Investigated by Experimental and Theoretical Electron Density and Electron Localizability Analyses
It is still a challenge to predict a compound's reactivity from its ground-state electronic nature although Bader-type topological analyses of the electron density (ED) and electron localizability indicator (ELI) give detailed and useful information on electron concentration and electron-pair localization, respectively. Both ED and ELI can be obtained from theoretical calculations as well as high-resolution X-ray diffraction experiments. Besides ED and ELI descriptors, the delocalization index is used here; it is likewise derived from theoretical calculations as well as from experimental X-ray results, but in the latter case, demonstrated here for the first time. We investigate {alpha},{beta}-unsaturated carbonyl and hydrazone compounds because resonance exhibited by these compounds in the electronic ground-state determines their reactive behavior. The degree of resonance as well as the reactivity contrast are quantified with the electronic descriptors. Moreover, competitive mesomeric substituent effects are studied using the two biologically important compounds acrolein and acrylamide. The reactivity differences predicted from the analyses are in line with the known reactivity of these compounds in organic synthesis. Hence, the capability of the ED and ELI for rationalizing and predicting different and competing substituent effects with respect to reactivity is demonstrated.
Grabowsky, Simon; Weber, Manuela; Jayatilaka, Dylan; Chen, Yu-Sheng; Grabowski, Matthias T.; Brehme, Rainer; Hesse, Malte; Schirmeister, Tanja; Luger, Peter (UWA); (Wurzburg); (UC); (Berlin)
[Synthesis and antituberculosis activity of the derivatives of glycoside steviolbioside from the plant Stevia rebaudiana and diterpenoid isosteviol containing hydrazone, hydrazide and pyridinoyl moieties].
Conjugates of antitubercular drug Isoniazid (hydrazide of isonicotinic acid), nicotinic and alpha-picolinic acid hydrazides and glycoside steviolbioside from the plant Stevia rebaudiana as well as the product of its acid hydrolysis, diterpenoid isosteviol, were synthesized. Besides, isosteviol hydrazide and hydrazone derivatives as well as conjugates containing two isosteviol moieties connected by dihydrazide linker were also obtained. Both initial compounds and their synthetic derivatives inhibit the growth of Mycobacterium tuberculosis (H37Rv in vitro). The minimum concentration at which the growth of M. tuberculosis was inhibited by 100% (MIC) for stevioside and steviolbioside equals 7.5 and 3.8 microg/mL, respectively. MIC values for conjugates of the hydrazides of pyridine carbonic acids and steviolbioside as well as isosteviol are in the ranges 5-10 and 10-20 microg/mL, respectively. Maximum inhibitory effect against M. tuberculosis showed the conjugates of isosteviol and adipic acid dihydrazide (MIC values ranged from 1.7 to 3.1 microg/mL). Antitubercular activity of the compounds studied is higher than the activity of antitubercular drug Pyrizanamide (MIC = 12.5-20 microg/mL) but lower than the activity of antitubercular drug Isoniazid (MIC = 0.02-0.04 microg/mL). PMID:22096997
Kataev, V E; Strobykina, I Iu; Andreeva, O V; Garifullin, B F; Sharipova, R R; Mironov, V F; Chestnova, R V
Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma.
The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro-PTA) or ammonium reineckate (Dro-R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors, which were evaluated according to IUPAC recommendations, reveal a fast, stable and linear response for drotaverine over the concentration range 10(-5) to 10(-2) M with cationic slopes of 49.55 and 51.36 mV per concentration decade. The direct potentiometric determination of drotaverine hydrochloride using the proposed sensors gave average recoveries of 99.95+/-0.71 and 100.04+/-0.60 for Dro-PTA and Dro-R, respectively. The sensors are used for determination of drotaverine hydrochloride in tablets, in its mixture with caffeine and paracetamol and in plasma. Validation of the method shows suitability of the proposed sensors for use in the quality control assessment of drotaverine hydrochloride. The developed method was found to be simple, accurate and precise when compared with a reported HPLC method. PMID:16469468
El-Saharty, Y S; Metwaly, F H; Refaat, M; El-Khateeb, S Z
Compressibility of floating pellets with verapamil hydrochloride coated with dispersion Kollicoat SR 30 D
The purpose of this study was to work out a method of compression of floating pellets with verapamil hydrochloride (VH) in a dose of 40mg. It was assumed that this form should reside in the stomach floating for several hours and gradually release the drug in a controlled way. Compression of pellets into tablets, being a modern technological process, is
Wies?aw Sawicki; Rafa? ?unio
Formulation, Evaluation and Optimization of Fast dissolving tablet containing Tizanidine Hydrochloride
Tizanidine HCl is a centrally acting ?-2 adrenergic agonist muscle relaxant. It is slightly bitter in taste. In the present study an attempt has been made to prepare bitter- less fast dissolving tablet of Tizanidine Hydrochloride using Eudragit E 100 as a taste masking agent. Mass extrusion was the technique used for preparing taste masked granules. The tablet was prepared
P. S. Zade; P. S. Kawtikwar; D. M. Sakarkar
The detection properties of ammonia SAW gas sensors based on L-glutamic acid hydrochloride
This study has investigated an improved surface acoustic wave (SAW) ammonia gas sensor based on L-glutamic acid hydrochloride. It presents an excellent reversibility, sensitivity, and repeatability to ammonia. The frequency shift versus ammonia concentration above 40°C was a monotonic function, and the limit of detection of the sensor at 50°C was 80 ppb.
Chi-Yen Shen; Chun-Pu Huang; Wang-Tsung Huang
Olopatadine Hydrochloride Improves Dermatitis Score and Inhibits Scratch Behavior in NC\\/Nga Mice
Background: Control of itch is an important issue in the treatment of atopic dermatitis (AD). Itch is mediated by a variety of pruritogens, including histamine, and promoted by neurite outgrowth in the epidermis of AD patients, probably due to the release of nerve growth factor. Objectives: We investigated the effects of orally administered olopatadine hydrochloride (olopatadine) on itching, itching mediators,
Hiroyuki Murota; Mostafa Abd El-latif; Tadafumi Tamura; Toru Amano; Ichiro Katayama
Design and evaluation of sustained release bilayer tablets of propranolol hydrochloride
The objective of the present research was to develop a bi- layer tablet of propranolol hydrochloride using superdi- sintegrant sodium starch glycolate for the fast release layer and water immiscible polymers such as ethylcellulose, Eudragit RLPO and Eudragit RSPO for the sustaining la- yer. In vitro dissolution studies were carried out in a USP 24 apparatus I. The formulations gave
Effects of Plastic and Acrylate Polymers on the Release Profile of Ambroxol Hydrochloride Controlled Release Pellets
The effects of Ammonio Methacrylate copolymer dispersion (Eudragit ® NE 30 D) and Polyvinyl Acetate dispersion (Kollicoat ® SR 30 D) are compared on the in vitro release of Ambroxol Hydrochloride from coated pellets in the current study. The nuclei pellets were manufactured by Extrusion-Spheronization with the drug, microcrystalline cellulose, lactose, maize starch, and hydroxypropyl methylcellulose followed by fluid bed
Ishtiaq Ahmed; Monzurul Amin Roni; Golam Kibria; Muhammad Rashedul Islam; Habibur Rahman
The aim of the present study is to perform stability study of Ambroxol Hydrochloride sustained release pellets stored in different storage conditions. The drug loaded beads were prepared by Extrusion-Spheronization technology then coated with ammonio methacrylate copolymer Type A (Eudragit RL 30 D) and ammonio methacrylate copolymer Type B (Eudragit RS 30 D) at a ratio of 2:3 (8% polymer
Increase in Serum Magnesium Level in Haemodialysis Patients Receiving Sevelamer Hydrochloride
Background: Clinical studies have shown that sevelamer hydrochloride improves lipid profiles and attenuates the progression of the cardiovascular calcifications in haemodialysis patients. It is known that both of these properties are associated with increased magnesium levels. The effect of sevelamer on serum magnesium level is not well documented. The aim of this study was to determine the effects of sevelamer
Efstathios Mitsopoulos; Ioannis Griveas; Stavros Zanos; Konstantinos Anagnostopoulos; Anastasia Giannakou; Aikaterini Pavlitou; Georgios Sakellariou
Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: propranolol hydrochloride.
One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes. PMID:16960826
Mishra, Dinesh; Garg, Minakshi; Dubey, Vaibhav; Jain, Subheet; Jain, N K
A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).
This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…
Villegas, Orlando; And Others
Stability Indicating RP-HPLC Estimation of Nebivolol Hydrochloride in Pharmaceutical Formulations.
A simple, specific, accurate and stability indicating reversed phase liquid chromatographic method was developed for the determination of nebivolol hydrochloride in tablet dosage forms. A phenomenex Gemini C-18, 5 ?m column having 250×4.6 mm i.d., with mobile phase containing methanol: acetonitrile: 0.02 M potassium dihydrogen phosphate (60:30:10, v/v/v; pH 4.0) was used. The retention time of nebivolol hydrochloride was 2.6 min. The linearity for nebivolol hydrochloride was in the range of 0.2-10 ?g/ml. The recovery was found to be in the range of 98.68-100.86%. The detection limit and quantification limit were found to be 0.06 ?g/ml and 0.2 ?g/ml, respectively. Nebivolol stock solutions were subjected to acid, alkali and neutral hydrolysis, chemical oxidation and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. The proposed method was validated and successfully applied to the estimation of nebivolol hydrochloride in tablet formulations. PMID:21394254
Shah, D A; Bhatt, K K; Mehta, R S; Baldania, S L; Gandhi, T R
Effect of extended withdrawal of zilpaterol hydrochloride on performance and carcass traits in finishing beef steers
The objective was to evaluate the ef- fects of an extended withdrawal period after feeding the ?-adrenergic agonist zilpaterol hydrochloride (ZH) for 20 d at the end of the feeding period. Three hundred eighty-four crossbred beef steers were blocked by BW and randomly allocated into 64 pens (6 steers\\/pen). Pens were assigned to treatments in a 2 × 4 factorial
B. P. Holland; C. R. Krehbiel; G. G. Hilton; M. N. Streeter; D. L. VanOverbeke; J. N. Shook; D. L. Step; L. O. Burciaga-Robles; D. R. Stein; D. A. Yates; J. P. Hutcheson; W. T. Nichols; J. L. Montgomery
Synthesis, antimicrobial potential and toxicological activities of Ni(II) complex of mefloquine hydrochloride
Transition metal complex of Ni(II) with mefloquine hydrochloride (antimalaria drug) was synthesized using a template method. Chemical analysis including conductivity measurements and spectroscopic studies were used to propose the geometry and mode of binding of the ligand to metal ion. From analytical data, the stoichiometry of the complex has been found to be 1:1. Infrared spectral data also suggest that
Joshua A. Obaleye; Johnson F. Adediji; Ebenezer T. Olayinka; Matthew A. Adebayo
Simultaneous HPLC Determination of Butenafine Hydrochloride and Betamethasone in a Cream Formulation
A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250×4.6 mm, 5 ?) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 ± 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 ?g/ml and 5-15 ?g/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation.
Ankam, R.; Mukkanti, K.; Durgaprasad, S.; Khan, M.
77 FR 41411 - Determination That TOPOTECAN INJECTION (Topotecan Hydrochloride) 1 Milligram (Base)/1 Milliliter...
...Hydrochloride) 1 Milligram (Base)/1 Milliliter, 3 Milligram (Base)/3 Milliliter, 4 Milligram (Base)/4 Milliliter, Was...1 milligram (mg) (base)/1 milliliter (mL), 3 mg (base)/3 mL, 4 mg (base)/4 mL, was not...
40 CFR 721.6196 - Hydrochloride salt of a fatty polyalkkylene polyamine (generic).
(1) The chemical substance identified generically as Hydrochloride salt of a fatty polyalkkylene polyamine (PMN P-99-0618) is subject to reporting under this section for the significant new use described in paragraph (a)(2) of this section. (2) The significant new uses...
Reactions of Urea with Semicarbazide and Semicarbazide Hydrochloride Reaktionen von Harnstoff MIT Semicarbazid und Semicarbazidhydrochlorid.
The reactions of urea with semicarbazide and semicarbazide hydrochloride for differnet molar ratios from 1.1 to 1.2 in fusion and aqueous solutions were investigated. Preliminary tests have shown that by using pure components in the same conditions, biure...
W. Engel
Response surface analysis of solution-mediated polymorphic transformation of buspirone hydrochloride
Buspirone hydrochloride has several polymorphs including Form 1 and Form 2. The solution-mediated transformation of Form 2 to Form 1 has been studied in this research. The interconversion of two polymorphs can occur in the salt formation step which is the last step for producing this drug. In addition, the effect of co-solvent and rate of addition of acid to
M. Sheikhzadeh; S. Murad; S. Rohani
Early stages of chemically induced liver carcinogenesis by oral administration of the antihistaminic methapyrilene hydrochloride
The antihistaminic drug methapyrilene hydrochloride, which induces liver tumors in rats, was administrated orally to female Wistar rats. The animals were killed after 21, 38, 77, 119, 181, and 196 days. The activities of adenosine-5-triphosphatase (ATPase) and ?-glutamyltranspeptidase (?-GT) in the liver were investigated histochemically. At 21 days, a homogeneous decrease of ATPase activity as well as a slight increase
G. Fischer; M. Altmannsberger; A. Schauer; N. Katz
Formulation and Evaluation of Propranolol Hydrochloride-Loaded Carbopol-934P/Ethyl Cellulose Mucoadhesive Microspheres
The purpose of this research was to formulate and systemically evaluate in-vitro and in-vivo performances of mucoadhesive propranolol hydrochloride microspheres for its potential use in the treatment of hypertension, myocardial infraction and cardiac arrhythmias. Propranolol hydrochloride mucoadhesive microspheres, containing carbopol-934P as mucoadhesive polymer and ethyl cellulose as carrier polymer, were prepared by an emulsion-solvent evaporation technique. Results of preliminary trials indicated that the quantity of emulsifying agent, time for stirring, drug-to-polymers ratio, and speed of rotation affected various characteristics of microspheres. Microspheres were discrete, spherical, free-flowing and showed a good percentage of drug entrapment efficiency. An in-vitro mucoadhesive test showed that propranolol hydrochloride mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could be retained in the gastrointestinal tract for an extended period of time. A 32 full factorial design was employed to study the effect of independent variables, drug-to-polymer-to-polymer ratio (propranolol hydrochloride-ethyl cellulose-carbopol-934P) (X1), and stirring speed (X2) on dependent variables, i.e. percentage of mucoadhesion, drug entrapment efficiency, particle size and t80. The best batch exhibited a high drug entrapment efficiency of 54 %; 82% mucoadhesion after 1 h and particle size of 110 ?m. A sustained pattern of drug release was obtained for more than 12 h. The drug-to-polymer-to-polymer ratio had a more significant effect on the dependent variables. The morphological characteristics of the mucoadhesive microspheres were studied under a scanning electron microscope. In-vivo evaluation studies on propranolol hydrochloride mucoadhesive microspheres and propranolol hydrochloride powder were performed on normal healthy rabbits. The results showed a sustained anti-hypertensive effect over a longer period of time in case of mucoadhesive microspheres, compared to the powder. In conclusion, the prolonged gastrointestinal residence time and slow release of propranolol hydrochloride resulting from the mucoadhesive microspheres, could contribute to the provision of a sustained anti-hypertensive effect.
Patel, Jayvadan; Patel, Darshna; Raval, Jignyasha
Preparation and the in vitro evaluation of nanoemulsion system for the transdermal delivery of granisetron hydrochloride.
The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4+/-1.5 to 82.4+/-0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1 : 1) and 10% NMP showed that the skin permeation rate was the highest (85.39+/-2.90 microg/cm(2)/h) and enhancement of drug permeability was 4.1-fold for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8+/-2.86 microg/cm(2)) with the shortest lag time (0.11+/-0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms. PMID:20686252
Zheng, Wen-wu; Zhao, Ling; Wei, Yu-meng; Ye, Yun; Xiao, Shun-han
Optimization of mesoporous carbons for efficient adsorption of berberine hydrochloride from aqueous solutions.
Sixteen mesoporous carbon adsorbents were synthesized by varying the ratio of soft to hard templates in order to optimize the pore textural properties of these adsorbents. The mesoporous carbon adsorbents have a high BET specific surface area (1590.3-2193.5m(2)/g), large pore volume (1.72-2.56cm(3)/g), and uniform pore size distribution with a median pore diameter ranging from 3.51nm to 4.52nm. It was observed that pore textural properties of the carbon adsorbents critically depend on the molar ratio of carbon sources to templates, and the hard template plays a more important role than the soft template in manipulating the pore textures. Adsorption isotherms of berberine hydrochloride at 303K were measured to evaluate the adsorption efficacy of these adsorbents. The adsorption of berberine hydrochloride from aqueous solutions on the sixteen mesoporous carbon adsorbents synthesized in this work is very efficient, and the adsorption equilibrium capacities on all samples are more than double the adsorption capacities of berberine hydrochloride of the benchmark adsorbents (polymer resins and spherical activated carbons) at similar conditions. It was observed from the adsorption experiments that the equilibrium adsorption amounts of berberine hydrochloride are strongly correlated with the BET specific surface area and pore volume of the adsorbents. The adsorbent with the highest BET of 2193.5m(2)/g displayed the largest adsorption capacity of 574mg/g at an equilibrium concentration of 0.10mg/mL of berberine hydrochloride in an aqueous solution. PMID:24767505
Li, Yin; Fu, Jie; Deng, Shuguang; Lu, Xiuyang
Clinical effects of the new phosphorus binder, bixalomer in hemodialysis patients switched from sevelamer hydrochloride.
It has been reported that sevelamer hydrochloride, which is often used as a polymer phosphorus (P) binder for managing serum P concentration in dialysis patients, causes gastrointestinal adverse effects such as constipation, etc. The reason for this is thought to be that sevelamer hydrochloride has high water absorption, causing it to absorb water and swell in the gastrointestinal tract. In June 2012, the new polymer P binder bixalomer was launched in Japan. Since bixalomer has low swelling due to water absorption, it can be expected to alleviate adverse effects in the gastrointestinal system. In our study, for 21 cases of maintenance hemodialysis patients undergoing treatment with sevelamer hydrochloride at our hospital, the P binder was switched from sevelamer hydrochloride to the same dosage of bixalomer, and the concentrations of serum P, corrected calcium (Ca) and whole parathyroid hormone (PTH) before and one month after the switch were compared. In addition, gastrointestinal symptoms (acid reflux, abdominal pain, indigestion, diarrhea and constipation) were evaluated before and after the switch using a questionnaire based on the Japanese version of the Gastrointestinal Symptom Rating Scale (GSRS). By switching to bixalomer, serum P concentration was significantly reduced (P?=?0.024), but there were no significant changes observed for serum corrected Ca and whole PTH. Furthermore, there were no significant changes observed for all five of the evaluation items of the GSRS, before and after the switch. These results suggest that although bixalomer can more potently reduce the serum P concentration than sevelamer hydrochloride, there were no significant differences in the effects of both P binders on the gastrointestinal symptoms. PMID:24975889
Gen, Shikou; Sasaki, Takaya; Saito, Kanako; Nobe, Kanako; Nodaira, Yuka; Ikeda, Naofumi
Is planarity of pyridin-2-yl- and pyrazin-2-yl-formamide thiosemicarbazones related to their tuberculostatic activity? X-ray structures of two pyrazine-2-carboxamide-N?-carbonothioyl-hydrazones
Crystal structures of two title compounds and several their relatives known earlier reveal conservative and characteristic features, which may be related to their tuberculostatic activity. The molecules are predominantly planar due to conjugation through five successive bonds in the zwitterionic fragment S --C(sp 2)-N-NH +-C(sp 2)-NH 2 and intramolecular hydrogen bonds, which prevent rotation of the adjacent pyrazine (or pyridine) ring. It has been suggested that in spatial sense such planar molecules resemble acridines intercalating with nucleic acids and that similar process may be responsible for tuberculostatic activity of the title pyrazine-2-carboxamide- N'-carbonothioyl-hydrazones.
Olczak, Andrzej; G?ówka, Marek L.; Go?ka, Jolanta; Szczesio, Ma?gorzata; Bojarska, Joanna; Koz?owska, Krystyna; Foks, Henryk; Orlewska, Czes?awa
Synthesis, characterization and structure of the first rhenium compound of di-2-pyridyl ketone thiophene-2-carboxylic acid hydrazone (dpktah), fac-[Re(CO) 3( N, N-? 2-dpktah)Cl
fac-[Re(CO)3(?2-N,N -dpktah)Cl], isolated from the reaction between [Re(CO)5Cl] and di-2-pyridyl ketone thiophene-2-carboxylic acid hydrazone (dpktah) in refluxing toluene, exhibits rich physico-chemical properties. The formulation of fac-[Re(CO)3(?2-N,N -dpktah)Cl] was established from the results of its elemental analysis and spectroscopic measurements, and confirmed using X-ray crystallography. The 1H NMR spectrum of fac-[Re(CO)3(?2-N,N-dpktah)Cl] revealed the coordination of dpktah and exchange of the amide
Mohammed Bakir; Colin Gyles
Release of tetracycline hydrochloride from electrospun poly(ethylene-co-vinylacetate), poly(lactic acid), and a blend
Electrospun fiber mats are explored as drug delivery vehicles using tetracycline hydrochloride as a model drug. The mats were made either from poly(lactic acid) (PLA), poly(ethylene-co-vinyl acetate) (PEVA), or from a 50:50 blend of the two. The fibers were electrospun from chloroform solutions containing a small amount of methanol to solubilize the drug. The release of the tetracycline hydrochloride from
El-Refaie Kenawy; Gary L. Bowlin; Kevin Mansfield; John Layman; David G. Simpson; Elliot H. Sanders; Gary E. Wnek
Bivalent transition metal complexes of o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone: Spectroscopic, antibacterial, antifungal activity and thermogravimetric studies
Schiff base complexes of Cu(II), Ni(II) and Zn(II) with the o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone (H 2o-HAHNH) containing N and O donor sites have been synthesized. Both ligand and its metal complexes were characterized by different physicochemical methods, elemental analysis, molar conductivity ( 1H NMR, 13C NMR, IR, UV-visible, ESR, MS spectra) and also thermal analysis (TG and DTG) techniques. The discussion of the outcome data of the prepared complexes indicates that the ligand behave as a bidentate and/or tridentate ligand. The electronic spectra of the complexes as well as their magnetic moments suggest octahedral geometries for all isolated complexes. The room temperature solid state ESR spectrum of the Cu(II) complex shows d x2- y2 as a ground state, suggesting tetragonally distorted octahedral geometry around Cu(II) centre. The molar conductance measurements proved that the complexes are non-electrolytes. The kinetic thermodynamic parameters such as: E#, ? H#, ? G#, ? S# are calculated from the DTG curves, for the [Ni(H O-HAHNH) 2] and [Zn(H 2 O-HAHNH)(OAc) 2]·H 2O complexes using the Coats-Redfern equation. Also, the antimicrobial properties of all compounds were studied using a wide spectrum of bacterial and fungal strains. The [Cu(H o-HAHNH)(OAc)(H 2O) 2] complex was the most active against all strains, including Aspergillus sp., Stemphylium sp. and Trichoderma sp. Fungi; E. coli and Clostridium sp. Bacteria.
Zaky, R. R.; Ibrahim, K. M.; Gabr, I. M.
Synthesis, characterization of some transition metal(II) complexes of acetone p-amino acetophenone salicyloyl hydrazone and their anti microbial activity.
Complexes of the type [M(apash)Cl] and [M(Hapash)(H2O)SO4], where M = Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); Hapash = acetone p-amino acetophenone salicyloyl hydrazone have been synthesized and characterized by elemental analyses, molar conductance, magnetic moments, electronic, ESR and IR spectra, thermal studies (TGA & DTA) and X-ray diffraction studies. The ligand coordinates through two >C=N and a deprotonated enolate group in all the chloro complexes, whereas through two >C=N- and a >C=O group in all the sulfato complexes. The electronic spectra suggest a square planar geometry for Co(II), Ni(II) and Cu(II) chloride complexes and an octahedral geometry for the sulfate complexes. ESR data show an isotropic symmetry for [Cu(apash)Cl] and [Cu(Hapash)(H2O)SO4] in solid state. However, ESR spectra of both Cu(II) complexes indicate the presence of unpaired electron in d x2-y2. The X-ray diffraction parameters for [Co(apash)Cl] and [Cu(Hapash)(H2O)SO4] complexes correspond to a tetragonal and an orthorhombic crystal lattices, respectively. Thermal studies of [Co(apash)Cl] complex shows a multi-step decomposition pattern. Most of the complexes show better antifungal activity than the standard miconazole against a number of pathogenic fungi. The antibacterial activity of these complexes has been evaluated against E. coli and Clostridium sp. which shows a moderate activity. PMID:18305909
Singh, Vinod P; Katiyar, Anshu; Singh, Shweta
Cytotoxic iron chelators: characterization of the structure, solution chemistry and redox activity of ligands and iron complexes of the di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) analogues.
Di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) and a range of its analogues comprise a series of monobasic acids that are capable of binding iron (Fe) as tridentate ( N, N, O) ligands. Recently, we have shown that these chelators are highly cytotoxic, but show selective activity against cancer cells. Particularly interesting was the fact that cytotoxicity of theHPKIH analogues is maintained even after complexation with Fe. To understand the potent anti-tumor activity of these compounds, we have fully characterized their chemical properties. This included examination of the solution chemistry and X-ray crystal structures of both the ligands and Fe complexes from this class and the ability of these complexes to mediate redox reactions. Potentiometric titrations demonstrated that all chelators are present predominantly in their charge-neutral form at physiological pH (7.4), allowing access across biological membranes. Keto-enol tautomerism of the ligands was identified, with the tautomers exhibiting distinctly different protonation constants. Interestingly, the chelators form low-spin (diamagnetic) divalent Fe complexes in solution. The chelators form distorted octahedral complexes with Fe(II), with two tridentate ligands arranged in a meridional fashion. Electrochemistry of the Fe complexes in both aqueous and non-aqueous solutions revealed that the complexes are oxidized to their ferric form at relatively high potentials, but this oxidation is coupled to a rapid reaction with water to form a hydrated (carbinolamine) derivative, leading to irreversible electrochemistry. The Fe complexes of theHPKIH analogues caused marked DNA degradation in the presence of hydrogen peroxide. This observation confirms that Fe complexes from theHPKIH series mediate Fenton chemistry and do not repel DNA. Collectively, studies on the solution chemistry and structure of theseHPKIH analogues indicate that they can bind cellular Fe and enhance its redox activity, resulting in oxidative damage to vital biomolecules. PMID:14564555
Bernhardt, Paul V; Caldwell, Lorraine M; Chaston, Timothy B; Chin, Piao; Richardson, Des R
Synthesis and quantitative structure-activity relationship (QSAR) study of novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives as nematicidal agents.
In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by (1)H NMR, (13)C NMR, HRMS, ESI-MS, and mp. Their nematicidal activity was evaluated against that of the pine wood nematode, Bursaphelenchus xylophilus in vivo. Among all of the derivatives, especially V-12 and V-39 displayed the best promising nematicidal activity with LC50 values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R(1) and R(2) together as the electron-withdrawing substituents, R(3) as the methyl group, and R(4) as the phenyl with the electron-donating substituents could be taken into account for further preparation of these kinds of compounds as nematicidal agents. Six selected descriptors are a WHIM descriptor (E1m), two GETAWAY descriptors (R1m+ and R3m+), a Burden eigenvalues descriptor (BEHm8), and two edge-adjacency index descriptors (EEig05x and EEig13d). Quantitative structure-activity relationship (QSAR) studies demonstrated that the structural factors, such as molecular mass (a negative correlation with the bioactivity) and molecular polarity (a positive correlation with bioactivity), are likely to govern the nematicidal activities of these compounds. For this model, the correlation coefficient (R(2)(training set)), the leave-one-out cross-validation correlation coefficient (Q(2)(LOO)), and the 7-fold cross-validation correlation coefficient (Q(2)7-fold) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Q(2)ext) and the root-mean-square error for the test set (RMSE(test set)) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents. PMID:23738496
Che, Zhiping; Zhang, Shaoyong; Shao, Yonghua; Fan, Lingling; Xu, Hui; Yu, Xiang; Zhi, Xiaoyan; Yao, Xiaojun; Zhang, Rui
Influence of limonene on the bioavailability of nicardipine hydrochloride from membrane-moderated transdermal therapeutic systems in human volunteers.
The aim of the present study was to develop a membrane-moderated transdermal therapeutic system (TTS) of nicardipine hydrochloride using 2%w/w hydroxy propyl cellulose (HPC) gel as a reservoir system containing 4%w/w of limonene as a penetration enhancer. The permeability flux of nicardipine hydrochloride through ethylene vinyl acetate (EVA) copolymer membrane was found to increase with an increase in vinyl acetate (VA) content in the copolymer. The effect of various pressure-sensitive adhesives (MA-31, MA-38 or TACKWHITE A 4MED) on the permeability of nicardipine hydrochloride through EVA membrane 2825 (28% w/w VA) or membrane/skin composite was also studied. The results showed that nicardipine hydrochloride permeability through EVA 2825 membrane coated with TACKWHITE 4A MED/skin composite was higher than that coated with MA-31or MA-38. Thus a new TTS for nicardipine hydrochloride was formulated using EVA 2825 membrane coated with a pressure-sensitive adhesive TACKWHITE 4A MED and 2%w/w HPC gel as reservoir containing 4%w/w of limonene as a penetration enhancer. The bioavailability studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady state plasma concentration of the drug with minimal fluctuations for 20 h with improved bioavailability in comparison with the immediate release capsule dosage form. PMID:12429488
Krishnaiah, Y S R; Satyanarayana, V; Bhaskar, P
High-performance thin-layer chromatographic separation of ranitidine hydrochloride and two related compounds.
Ranitidine hydrochloride and its two related compounds, used in the USP TLC purity testing of the drug, were separated on a high-performance thin-layer chromatography (HPTLC) RP-18 WF254S precoated plate using methanol-3% NH4OH (4:1, v/v) as the mobile phase. The main advantage of the proposed HPTLC system over the USP TLC system for testing the purity of ranitidine is a better and more efficient separation of these three compounds in a shorter time and with less consumption of solvents. The system is promising from the point of view of the development of a new method for the TLC purity testing of ranitidine hydrochloride. A video system was used for imaging thin-layer chromatograms. Direct UV densitometric quantitation of the three compounds and a model for the calculation of analytical performance parameters is presented in the second part of the paper. PMID:9792529
Simonovska, B; Prosek, M; Vovk, I; Jelen-Zmitek, A
Study on the Interaction of ?-Cyclodextrin and Berberine Hydrochloride and Its Analytical Application
The fluorescence enhancement of berberine hydrochloride (BBH) as a result of complex with ?-cyclodextrin (?-CD) is investigated. The mechanism of the inclusion was studied and discussed by spectrofluoremetry and infrared spectrograms. The results showed that a 1?1 (?-CD: BBH) complex was formed with an apparent association constant of 4.23×102 L/mol. Based on the enhancement of the fluorescent intensity of berberine hydrochloride, a new spectrofluorimetric method for the determination of BBH in the presence of ?-CD was developed. The linear range was 1.00?4.00 µg/mL with the detection limit of 5.54 ng/mL. The proposed method was successfully applied to the determination of BBH in tablets.
Jia, Baoxiu; Li, Yuqin; Wang, Decai; Duan, Rui
Simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation by liquid chromatography.
A rapid and accurate liquid chromatographic method is described for the simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation. Chromatographic separation of the two drugs was achieved on a Diamonsil C(18) column (200 mm x 4.6 mm, 5 microm). The mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% ammonium acetate (39:11:50 (v/v), pH 5.5) was delivered at a flow rate of 1.0 ml/min. Detection was performed at 220 nm. Linearity, accuracy and precision were found to be acceptable over the concentration range of 201.2-2012.0 microg/ml for roxithromycin and 42.7-427.0 microg/ml for ambroxol hydrochloride, respectively. Separation was complete in less than 10 min. The proposed method can be used for the quality control of formulation products. PMID:15336374
Qi, Meiling; Wang, Peng; Cong, Ruihua; Yang, Jianjun
Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental dermatophytosis in guinea pigs.
Butenafine hydrochloride, N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride (butenafine), is a novel antifungal agent of the class of benzylamine derivatives. Butenafine was investigated for its activity against guinea pig dermatophytosis caused by Trichophyton mentagrophytes or Microsporum canis in comparison with those of naftifine, tolnaftate, clotrimazole, and bifonazole. Topical butenafine showed excellent efficacy against dermatophytosis when it was applied once daily, and the effect was superior to those of all four reference drugs. When applied once at 24 or 48 h before infection, the drug exhibited excellent prophylactic efficacy against experimental T. mentagrophytes infection. The concentrations of butenafine in animal skin at 24 and 48 h after application of 0.2 ml of a 1% solution were several hundred times higher than those required to kill T. mentagrophytes and M. canis. The good efficacy of butenafine against dermatophytosis may be attributable to its fungicidal activity and long retention in the skin after topical application.
Arika, T; Yokoo, M; Hase, T; Maeda, T; Amemiya, K; Yamaguchi, H
Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.
Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride. PMID:23732802
Hathout, Rania M; Nasr, Maha
Spectrophotometric Determination of Cefetamet Pivoxil Hydrochloride and Pitavastatin Calcium in Tablet Dosage form
Two simple, rapid, specific and accurate analytical methods for the estimation of cefetamet pivoxil hydrochloride and pitavastatin calcium in bulk drug and in their tablet formulations are described. These methods are based on difference spectrophotometry, wherein the measurement is done at maximum 221 nm and minimum 275 nm for cefetamet whereas at maximum 240 nm and minimum 259 nm for pitavastatin. The Beer's law was obeyed in the concentration range of 1-35 ?g/ml and 1-25 ?g/ml and the molar absorptivities were 1.3×104 lit mol?1 cm?1 and 2.4×104 lit mol?1 cm?1 for cefetamet pivoxil hydrochloride and pitavastatin calcium, respectively. The proposed methods were validated and successfully applied to the estimation of drugs in tablet formulations.
Vadia, N. H.; Patel, Vandana; Bhalara, H. N.
Quantitative Estimation of Itopride Hydrochloride and Rabeprazole Sodium from Capsule Formulation
Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C18 column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies.
Pillai, S.; Singhvi, I.
Spectrofluorimetric method for determination of duloxetine hydrochloride in bulk and pharmaceutical dosage forms.
A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 mug/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 mug/ml and 0.010 mug/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%. PMID:20046780
Prabu, S L; Shahnawaz, S; Kumar, C Dinesh; Shirwaikar, A
Pharmacokinetics of high-dose oral thiamine hydrochloride in healthy subjects
Background High dose oral thiamine may have a role in treating diabetes, heart failure, and hypermetabolic states. The purpose of this study was to determine the pharmacokinetic profile of oral thiamine hydrochloride at 100 mg, 500 mg and 1500 mg doses in healthy subjects. Methods This was a randomized, double-blind, single-dose, 4-way crossover study. Pharmacokinetic measures were calculated. Results The AUC0-10 hr and Cmax values increased nonlinearly between100 mg and 1500 mg. The slope of the AUC0-10 hr vs dose, as well as the Cmax vs dose, plots are steepest at the lowest thiamine doses. Conclusion Our study demonstrates that high blood levels of thiamine can be achieved rapidly with oral thiamine hydrochloride. Thiamine is absorbed by both an active and nonsaturable passive process. Trial Registration ClinicalTrials.gov: NCT00981877
Preparation and Characterisation of Mucoadhesive Nasal Gel of Venlafaxine Hydrochloride for Treatment of Anxiety Disorders
The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug.
Basu, Shyamoshree; Maity, S.
Management of attention-deficit hyperactivity disorder in adults: focus on methylphenidate hydrochloride
Attention-deficit hyperactivity disorder (ADHD) is one of the most common psychiatric disorders in young adults and causes significant psychosocial impairment and economic burden to society. Because of the paucity of long-term evidence and lack of national guidelines for diagnosis and management of adult ADHD, most of the data are based on experience derived from management of childhood ADHD. This article reviews the current evidence for the diagnosis and management of adult ADHD with special emphasis on the role of methylphenidate hydrochloride preparations in its treatment. Methylphenidate hydrochloride, a stimulant that acts through the dopaminergic and adrenergic pathways, has shown more than 75% efficacy in controlling the symptoms of adult ADHD. Although concern for diversion of the drug exists, recent data have shown benefits in preventing substance use disorders in patients with adult ADHD.
Nair, Rajasree; Moss, Shannon B
Normal coordinate analysis and vibrational spectra of 9-?-D-arabinofuranosyladenine hydrochloride (ara-A.HCl)
The vibrational spectra of a synthetic purine nucleoside with known antiviral activity, 9-ß-D-arabino-furanosyladenine hydrochloride (ara-A.HCl) are reported. The Fourier transform infrared (FT-IR) and Fourier transform Raman (FT-Raman) spectra were recorded in the 4000-30 cm-1 spectral region. The harmonic frequencies and potential energy distributions (PED) of the vibrational modes of ara-A.HCI were calculated by two different methods: a classical molecular mechanics
L. E. Bailey; A. Hernanz; R. Navarro; T. Theophanides
In vitro and in vivo evaluation of ranitidine hydrochloride loaded hollow microspheres in rabbits
The objective of this investigation was to develop the hollow microspheres as a new dosage form of floating drug delivery\\u000a systems with prolonged stomach retention time. Hollow microspheres containing ranitidine hydrochloride (RH) were prepared\\u000a by a novel solvent diffusion-evaporation method using ethyl cellulose (EC) dissolved in a mixture of ethanol and ether (6:1.0,\\u000a v\\/v). The yield and drug loading amount
Yu-meng Wei; Ling Zhao
Chromatographic separation and analysis of chloropheniramine maleate, methscopolamine nitrate and phenylephrine hydrochloride in sustained release capsules
Summary A high performance liquid chromatographic method has been developed for the simultaneous determination of chlorpheniramine\\u000a maleate (CPM), methscoplamine nitrate (MSN) and phenylephrine hydrochloride (PEH) in sustained release capsules. The separation\\u000a was carried out on a reverse-phase CN-column with use of a mobile phase consisting of 70% (v\\/v) solution of acetonitrile in water containing 2% (v\\/v) acetic acid and 0.005M sodium
M. E. S. Metwally
Design and Optimization of Mefloquine Hydrochloride Microparticles for Bitter Taste Masking
The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2),\\u000a of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and\\u000a sodium hydroxide as precipitant. A 32 full factorial design was used for optimization wherein the drug concentration (A) and polymer concentration (B) were selected\\u000a as
Punit P. Shah; Rajashree C. Mashru; Yogesh M. Rane; Arti Thakkar
Growth of nonlinear optical material: L-arginine hydrochloride and its characterisation
L-arginine hydrochloride crystals have been grown using water and ethanol+water mixture as solvent. Growth of the anhydrous form of LAHCl has also been carried out. The grown crystals were subjected to powder X-ray diffraction studies. FTIR studies have been carried out to identify the functional groups present in the crystal. TGA and optical transmission studies have also been made on the grown crystals. The grown crystals were subjected to etching and microhardness studies.
Meera, K.; Muralidharan, R.; Dhanasekaran, R.; Manyum, Prapun; Ramasamy, P.
Polymeric Matrix System for Prolonged Delivery of Tramadol Hydrochloride, Part II: Biological Evaluation
This study is an extrapolation of our previous one (part I) concerned with the formulation and physicochemical evaluation\\u000a of a novel, simple, monolayer, easy-to-use, cost-effective, and aesthetically acceptable bioadhesive transdermal patch for\\u000a tramadol hydrochloride. The current work is focused on bioadhesion, skin tolerability, and pharmacodynamic evaluation. Using\\u000a naked rat skin, chitosan–Eudragit® NE30D (1:1) film attained best bioadhesive properties. During in
Hussein O. Ammar; Mahmoud Ghorab; Soheir A. El-Nahhas; Rabab Kamel
An ESEEM investigation of single crystals and powders of copper-doped l -histidine hydrochloride monohydrate
In this paper we present an investigation of the remote nitrogen of imidazole in copper-dopedl-histidine hydrochloride monohydrate, which is a model system for a wide range of biologically important copper-imidazole\\u000a complexes. Since these systems are mostly not available in a crystalline form it is interesting to investigate to what extent\\u000a information that can be obtained from these disordered systems using
J. J. Shane; P. A. A. W. van der Heijden; E. J. Reijerse; E. de Boer
Preparation and controlled release of mesoporous MCM-41/propranolol hydrochloride composite drug.
This article used MCM-41 as a carrier for the assembly of propranolol hydrochloride by the impregnation method. By means of chemical analysis, powder X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and low-temperature N(2) adsorption-desorption at 77?K, the characterization was made for the prepared materials. The propranolol hydrochloride guest assembly capacity was 316.20?±?0.31?mg/g (drug/MCM-41). Powder XRD test results indicated that during the process of incorporation, the frameworks of the MCM-41 were not destroyed and the crystalline degrees of the host-guest nanocomposite materials prepared still remained highly ordered. Characterization by SEM and TEM showed that the composite material presented spherical particle and the average particle size of composite material was 186?nm. FT-IR spectra showed that the MCM-41 framework existed well in the (MCM-41)-propranolol hydrochloride composite. Low-temperature nitrogen adsorption-desorption results at 77?K showed that the guest partially occupied the channels of the molecular sieves. Results of the release of the prepared composite drug in simulated body fluid indicated that the drug can release up to 32?h and its maximum released amount was 99.20?±?0.11%. In the simulated gastric juice release pattern of drug, the maximum time for the drug release was discovered to be 6?h and the maximum cumulative released amount of propranolol hydrochloride was 45.13?±?0.23%. The drug sustained-release time was 10?h in simulated intestinal fluid and the maximum cumulative released amount was 62.05?±?0.13%. The prepared MCM-41 is a well-controlled drug delivery carrier. PMID:22894165
Zhai, Qing-Zhou
Compatibility and stability of ondansetron hydrochloride, dexamethasone, and lorazepam in injectable solutions.
The stability of ondansetron hydrochloride, dexamethasone sodium phosphate, and lorazepam in 5% dextrose injection or 0.9% sodium chloride injection in polyvinyl chloride (PVC) minibags and glass bottles was studied. Triplicate solutions of 8 or 32 mg of ondansetron (as the hydrochloride salt) mixed with 20 mg of dexamethasone phosphate (as the sodium salt) with or without 2 mg of lorazepam were compounded in 50-mL PVC minibags and glass bottles containing either 5% dextrose injection or 0.9% sodium chloride injection and stored at 23-25 degrees C. Duplicate measurements were performed when drugs were added and at 1, 2, 4, 8, and 24 hours after addition. Samples of the 32-mg ondansetron admixtures were collected under aseptic conditions to inspect for precipitation and to count particles with a laser particle analyzer. Samples of all admixtures were evaluated for chemical stability by stability-indicating high-performance liquid chromatography. Ondansetron hydrochloride and dexamethasone were physically compatible and chemically stable for up to 24 hours under the study conditions. The concentration of lorazepam in PVC containers dropped below 90% of the original concentration within four hours. In addition, particle counts in lorazepam-containing solutions were higher when 0.9% sodium chloride injection was the diluent than when 5% dextrose injection was the diluent. In admixtures containing all drugs, ondansetron hydrochloride and dexamethasone sodium phosphate in 5% dextrose injection or 0.9% sodium chloride injection were stable for up to 24 hours when stored in PVC bags or glass bottles.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:8362872
McGuire, T R; Narducci, W A; Fox, J L
An efficient, inexpensive, and shelf-stable diazotransfer reagent: imidazole-1-sulfonyl azide hydrochloride.
The design and synthesis of a new diazotransfer reagent, imidazole-1-sulfonyl azide hydrochloride, are reported. This reagent has proven to equal triflyl azide in its ability to act as a "diazo donor" in the conversion of both primary amines into azides and activated methylene substrates into diazo compounds. Crucially, this reagent can be prepared in a one-pot reaction on a large scale from inexpensive materials, is shelf-stable, and is conveniently crystalline. PMID:17713918
Goddard-Borger, Ethan D; Stick, Robert V
Extraction-spectrophotometric determination of amprolium hydrochloride using bromocresol green, bromophenol blue and bromothymol blue
A new procedure for the determination of amprolium hydrochloride by reaction with bromocresol green (BCG), bromophenol blue (BPB) and bromothymol blue (BTB) has been developed. The method consists of extracting the yellow ion-pair formed into chloroform from aqueous medium. The ion-pairs have absorption maxima at 420, 410 and 415 nm with molar absorptivities of 3.64 × 104, 3.12 × 104
Adel F. Shoukry; Mahmoud S. Rizk; Yousry M. Issa; Ehab M. Atia
Sevelamer hydrochloride attenuates kidney and cardiovascular calcifications in long-term experimental uremia
Sevelamer hydrochloride attenuates kidney and cardiovascular calcifications in long-term experimental uremia.BackgroundIn chronic renal failure (CRF), hyperphosphatemia and an elevated calcium-phosphate product are associated with vascular calcification and increased cardiovascular morbidity and mortality. Previous data have demonstrated that 3-month treatment of uremic rats with sevelamer was associated with less nephrocalcinosis compared to calcium carbonate (CaCO3), despite similar control of serum phosphorus,
Mario Cozzolino; Mark E. Staniforth; Helen Liapis; Jane Finch; Steven K. Burke; Adriana S. Dusso; Eduardo Slatopolsky
Formulation, evaluation, and comparison of bilayered and multilayered mucoadhesive buccal devices of propranolol hydrochloride
The purpose of this research work was to establish mucoadhesive buccal devices of propranolol hydrochloride (PRH) in the forms\\u000a of bilayered and multilayered tablets. The tablets were prepared using sodium carboxymethylcellulose (SCMC) and Carbopol-934\\u000a (CP) as bioadhesive polymers to impart mucoadhesion and ethyl cellulose (EC) to act as an impermeable backing layer. Buccal\\u000a devices were evaluated by different parameters such
Vishnu M. Patel; Bhupendra G. Prajapati; Madhabhai M. Patel
Formulation and Evaluation of Bilayer Tablet of Metoclopramide Hydrochloride and Ibuprofen
The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective\\u000a treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated\\u000a as immediate release layer by using various disintegrants like Ac-Di-Sol, Polyplasdone XL, Explotab, Agar and Gellan Gum.\\u000a Treated form of gellan gum
Bhavesh Shiyani; Surendra Gattani; Sanjay Surana
Determination of ambroxol hydrochloride in tablets using flow-injection UV spectrophotometry and HPLC
A flow-injection UV spectrophotometric method was developed for the determination of ambroxol hydrochloride in tablets. The\\u000a quantitative determination of ambroxol was performed at 245 nm using distilled water as the carrier solvent. In this study,\\u000a the flow rate, loop volume, and the number of injections per hour were 15 mL\\/min, 193 ?L, and 100, respectively. The analytical\\u000a signal of ambroxol
E. Satana; H. Basan; N. G. Go?er
Simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation by liquid chromatography
A rapid and accurate liquid chromatographic method is described for the simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation. Chromatographic separation of the two drugs was achieved on a Diamonsil™ C18 column (200mm×4.6mm, 5?m). The mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% ammonium acetate (39:11:50 (v\\/v), pH 5.5) was delivered at a
Meiling Qi; Peng Wang; Ruihua Cong; Jianjun Yang
Sequential injection chromatographic determination of ambroxol hydrochloride and doxycycline in pharmaceutical preparations
A new separation method based on a novel reversed-phase sequential injection chromatography (SIC) technique was used for simultaneous determination of ambroxol hydrochloride and doxycycline in pharmaceutical preparations in this contribution.The coupling of short monolith with SIA system results in an implementation of separation step to until no-separation low-pressure method.A Chromolith® Flash RP-18e, 25–4.6mm column (Merck, Germany) and a FIAlab® 3000
Dalibor Šatínský; Lucia M. L. Dos Santos; Hana Sklená?ová; Petr Solich; M. Conceiçăo B. S. M. Montenegro; Alberto N. Araújo
Gastroretentive drug delivery system of ranitidine hydrochloride: Formulation and in vitro evaluation
The purpose of this research was to prepare a gastroretentive drug delivery system of ranitidine hydrochloride. Guar gum,\\u000a xanthan gum, and hydroxypropyl methylcellulose were evaluated for gel-forming properties. Sodium bicarbonate was incorporated\\u000a as a gas-generating agent. The effects of citric acid and stearic acid on drug release profile and floating properties were\\u000a investigated. The addition of stearic acid reduces the
Brijesh S. Dave; Avani F. Amin; Madhabhai M. Patel
Preparation and Evaluation of Diltiazem Hydrochloride Diffusion-Controlled Transdermal Delivery System
The objective was to investigate the suitable polymeric films for the development of diltiazem hydrochloride (diltiazem HCl)\\u000a transdermal drug delivery systems. Hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC) were used as hydrophilic and\\u000a hydrophobic film formers, respectively. Effects of HPMC\\/EC ratios and plasticizers on mechanical properties of free films\\u000a were studied. Effects of HPMC\\/EC ratios on moisture uptake, in vitro release
Ekapol Limpongsa; Kraisri Umprayn
Adhesive properties of soy proteins modified by urea and guanidine hydrochloride
An investigation was conducted on the adhesive and water-resistance properties of soy protein isolates that were modified\\u000a by varying solutions of urea (1, 3, 5, and 8 M) or guanidine hydrochloride (GH) (0.5, 1, and 3 M) and applied on walnut, cherry,\\u000a and pine plywoods. Soy proteins modified by 1 and 3 M urea showed greater shear strengths than did
Weining Huang; Xiuzhi Sun
Effects of switching from sevelamer hydrochloride to bixalomer on laboratory parameters in hemodialysis patients.
In Japan, the clinical use of bixalomer, a new polymer preparation like sevelamer hydrochloride, became possible from 2012. In our study, in order to investigate the clinical characteristics of this new phosphorus (P) binder, bixalomer in a clinical practice, for 18 cases of hemodialysis patients at our hospital being treated with sevelamer hydrochloride, we switched the P binder to bixalomer, and compared the laboratory parameters before and after switching. Subjects used for analysis were nine cases in which it was possible to use bixalomer continuously for 10 months. The laboratory parameters measured were the concentrations of serum P, corrected calcium (Ca), whole parathyroid hormone (PTH), albumin and alkaline phosphatase (ALP) as indicators of mineral and bone disorder, and serum high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C) and triglyceride (TG) as indicators of lipid metabolism. Regarding the results after switching to bixalomer and starting treatment using the same dosage as the dosage previously used for sevelamer hydrochloride, there were many cases that showed increasing P concentrations that required increasing the dosage of bixalomer, the dosage after switching was increased significantly (P?=?0.002). In the comparison of laboratory parameters before and after switching, the concentrations of serum P and albumin decreased significantly (P?=?0.035 and 0.033). From these results, it was considered that the decreases in serum P concentrations were due not only to the effects of bixalomer, but that suppression of food intake by patients was another reason. There were no significant changes in corrected Ca, whole PTH or ALP. In addition, after changing the P binder, serum HDL-C concentration decreased significantly (P?=?0.015) and LDL-C increased significantly (P?0.001), and serum TG concentration showed no significant changes. This indicated that the beneficial effects of bixalomer on lipid metabolism may be less than those of sevelamer hydrochloride. PMID:24975888
Furukawa, Kazunori; Ikawa, Tomoyoshi; Yokoi, Sayuri; Yokouchi, Shuhei; Kato, Kieko; Ueno, Miki; Takahashi, Junichiro
Oxymorphone Hydrochloride, a Potent Opioid Analgesic, Is Not Carcinogenic in Rats or Mice
Despite their long history of chronic use, little information is available regarding the carcinogenicity of opioid analgesics. Oxy- morphoneisapotent morphinan-typemu-opioidanalgesicusedfor treatment of moderate-to-severe pain. Oxymorphone was tested for carcinogenicity in Crl:CD IGS BR rats and CD-1 mice. Oxy- morphone hydrochloride was administered orally once daily for 2 years to rats at doses of 2.5, 5 and 10 mg\\/kg\\/day (males) and
Dana L. Shuey; Cindy Woodland; Claudine Tremblay; Richard Gregson; Ronald J. Gerson
Early hemodynamic effects of olprinone hydrochloride after coronary artery bypass grafting
Our purpose was to evaluate the hemodynamic effects of olprinone hydrochloride early after coronary artery bypass grafting\\u000a (CABG). Fifteen patients undergoing CABG were administered a constant infusion of 0.1 ?g\\/kg\\/min of olprinone and continued\\u000a for 4 hours. No bolus infusion of olprinone was administered before continuous infusion. Systolic systemic arterial pressure,\\u000a systolic pulmonary arterial pressure, systemic vascular resistance and pulmonary
Akira Marui; Takaaki Mochizuki; Norimasa Mitsui; Tadaaki Koyama; Mayumi Horibe
Silicone adhesive matrix of verapamil hydrochloride to provide pH-independent sustained release.
Providing pH-independent oral release of weakly basic drugs with conventional matrix tablets can be challenging because of the pH-dependent solubility characteristics of the drugs and the changing pH environment along the gastrointestinal tract. The aim of the present study was to use a hydrophobic polymer to overcome the issue of pH-dependent release of weakly basic model drug verapamil hydrochloride from matrix tablets without the use of organic buffers in the matrix formulations. Silicone pressure-sensitive adhesive (PSA) polymer was evaluated because of its unique properties of low surface energy, hydrophobicity, low glass transition temperature, high electrical resistance, and barrier to hydrogen ion diffusion. Drug release, hydrogen ion diffusion, tablet contact angle, and internal tablet microenvironment pH with matrix tablets prepared using PSA were compared with those using water-insoluble ethyl cellulose (EC). Silicone PSA films showed higher resistance to hydrogen ion diffusion compared with EC films. Verapamil hydrochloride tablets prepared using silicone PSA showed higher hydrophobicity and lower water uptake than EC tablets. Silicone PSA tablets also showed pH-independent release of verapamil and decreased in dimensions during drug dissolution. By contrast, verapamil hydrochloride tablets prepared using EC did not achieve pH-independent release. PMID:24022347
Tolia, Gaurav; Li, S Kevin
Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride
The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1?h and 4-5th?h) using a 1%?w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2?h was 1069.87 ± 120.03??g/sq·cm compared to 744.81 ± 125.41??g/sq·cm after modulated alternating current iontophoresis for 2?h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71??g/sq·cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2?h at frequency of 1?kHz was found to be comparable to the continuous direct current iontophoresis for 1?h.
Banga, Ajay K.
Simultaneous Determination of Sitagliptin Phosphate Monohydrate and Metformin Hydrochloride in Tablets by a Validated UPLC Method
A novel approach was used to develop and validate a rapid, specific, accurate and precise reverse phase ultra performance liquid chromatographic (UPLC) method for the simultaneous determination of Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms. The chromatographic separation was achieved on Aquity UPLC BEH C8 100 × 2.1 mm, 1.7 ?m, column using a buffer consisting of 10 mM potassium dihydrogen phosphate and 2 mM hexane-1-sulfonic acid sodium salt (pH adjusted to 5.50 with diluted phosphoric acid) and acetonitrile as organic solvent in a gradient program. The flow rate was 0.2 mL min?1 and the detection wavelength was 210 nm. The limit of detection (LOD) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.2 and 0.06 ?g mL?1, respectively. The limit of quantification (LOQ) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.7 and 0.2 ?g mL?1, respectively. This method was validated with respect to linearity, accuracy, precision, specificity and robustness. The method was also found to be stability-indicating.
Malleswararao, Chellu S. N.; Suryanarayana, Mulukutla V.; Mukkanti, Khagga
Comparison of sevelamer hydrochloride and sevelamer carbonate: risk of metabolic acidosis and clinical implications.
Hyperphosphatemia is highly prevalent in patients with chronic kidney disease (CKD), particularly in those with advanced or end-stage renal disease. Sevelamer hydrochloride is an ion-exchange resin that reduces serum phosphorus concentrations. The agent also produces favorable lipid profile effects and does not cause hypercalcemia. However, reported drawbacks of this agent are metabolic acidosis, high pill burden, and a relatively low affinity and selectivity for phosphate anions. Sevelamer carbonate is a new buffered formulation that does not increase the risk of metabolic acidosis. To determine the roles of these two agents in the treatment of hyperphosphatemia in patients with CKD, we performed a MEDLINE search (June 1995-June 2008) focusing on the mechanism of action of resin binding with phosphate and the development of metabolic acidosis. We also reviewed studies that evaluated the effects of sevelamer hydrochloride or sevelamer carbonate on serum bicarbonate concentrations. Several studies in patients with CKD and hyperphosphatemia who received hemodialysis or peritoneal dialysis found decreases in serum bicarbonate concentrations with the use of sevelamer hydrochloride, whereas sevelamer carbonate did not have this negative effect on bicarbonate concentrations. Both drugs appear to be equivalent in their abilities to lower serum phosphorus concentrations. However, as sevelamer carbonate does not decrease serum bicarbonate levels, it may be more appropriate for patients at risk for metabolic acidosis who require phosphate binders that do not contain calcium or aluminum. PMID:19397463
Pai, Ashwini B; Shepler, Brian M
Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human.
1. The pharmacokinetics of a new calcium antagonist barnidipine hydrochloride, a stereochemically pure enantiomer, was studied after intravenous and oral dosing to the rat and dog, and oral to man. 2. After intravenous dosing, plasma concentrations of barnidipine hydrochloride declined bi-exponentially with the terminal half-lives of 0.6 h in the rat and 4.1 h in the dog. The blood clearance was 5.2 l/h/kg in the rat and 3.3 l/h/kg in the dog, and was comparable with hepatic blood flow in both species. 3. After oral dosing, plasma concentrations of barnidipine hydrochloride peaked rapidly (0.3-0.4 h in the rat and dog, 1.0-1.6 h in man). Cmax and AUC rose non-linearly with increasing doses in all three species. 4. The absolute bioavailability was low (11-18% in the rat and 6-9% in the dog), suggesting a marked first-pass metabolism. PMID:8592872
Teramura, T; Watanabe, T; Higuchi, S; Hashimoto, K
Application of Design of Experiment for Floating Drug Delivery of Tapentadol Hydrochloride
The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250?mg twice a day. For optimization 32 full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating.
Jagdale, Swati C.; Patil, Somnath; Kuchekar, Bhanudas S.
Stability of fluoxetine hydrochloride in fluoxetine solution diluted with common pharmaceutical diluents.
The stability of fluoxetine hydrochloride in fluoxetine solution diluted with five common pharmaceutical diluents was studied. Fluoxetine syrup, containing fluoxetine 4 mg/mL (as the hydrochloride salt), was diluted to 1 and 2 mg/mL in each of the following: deionized water; Simple Syrup, British Pharmacopeia; Simple Syrup, USP; Aromatic Elixir, USP; and grape-cranberry drink. Each solution was divided into eight 120-mL amber glass bottles: four stored at 5 degrees C and four stored at 30 degrees C. Samples were removed from each bottle at time zero and two, four, and eight weeks and assayed in triplicate with high-performance liquid chromatographic methods for determining fluoxetine concentration and concentration of its primary degradation product, alpha-[2-(methylamino)ethyl]benzene methanol. Stability was established if the fluoxetine concentration changed by < 10% and if the concentration of the degradation product was < 1% of the initial fluoxetine concentration. No test mixture dropped below 95% of the initial fluoxetine concentration or exceeded 0.5% degradation product during the study period. Fluoxetine hydrochloride was stable for eight weeks in fluoxetine solution diluted to 1 or 2 mg/mL with common pharmaceutical diluents and stored at 5 or 30 degrees C. PMID:8085574
Peterson, J A; Risley, D S; Anderson, P N; Hostettler, K F
Pharmacokinetic study of benfotiamine and the bioavailability assessment compared to thiamine hydrochloride.
Benfotiamine is a lipid-soluble thiamine precursor which can transform to thiamine in vivo and subsequently be metabolized to thiamine monophosphate (TMP) and thiamine diphosphate (TDP). This study investigated the pharmacokinetic profiles of thiamine and its phosphorylated metabolites after single- and multiple-dose administration of benfotiamine in healthy Chinese volunteers, and assessed the bioavailability of orally benfotiamine administration compared to thiamine hydrochloride. In addition, concentration of hippuric acid in urine which is produced in the transformation process of benfotiamine was determined. The results showed that thiamine and its phosphorylated metabolites exhibited different pharmacokinetic characteristics in plasma, blood and erythrocyte, and one-compartment model provided the best fit for pharmacokinetic profiles of thiamine. The transformation process of benfotiamine to thiamine produced large amount of hippuric acid. No accumulation of hippuric acid was observed after multiple-dose of benfotiamine. Compared to thiamine hydrochloride, the bioavailability of thiamine in plasma and TDP in erythrocyte after oral administration of benfotiamine were 1147.3?±?490.3% and 195.8?±?33.8%, respectively. The absorption rate and extent of benfotiamine systemic availability of thiamine were significantly increased indicating higher bioavailability of thiamine from oral dose of benfotiamine compared to oral dose of thiamine hydrochloride. PMID:24399744
Xie, Feifan; Cheng, Zeneng; Li, Sanwang; Liu, Xingling; Guo, Xin; Yu, Peng; Gu, Zhenkun
Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate.
Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L=dianion of the hydrazone, m=0-1, x=0-2, n=0-4 and z=0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms. PMID:24810030
Taha, Ali; Emara, Adel A A; Mashaly, Mahmoud M; Adly, Omima M I
Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate
Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L = dianion of the hydrazone, m = 0-1, x = 0-2, n = 0-4 and z = 0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms.
Taha, Ali; Emara, Adel A. A.; Mashaly, Mahmoud M.; Adly, Omima M. I.
Study on the resonance nonlinear scattering spectra of the interactions of promethazine hydrochloride and chlorpromazine hydrochloride with 12-tungstophosphoric acid and their analytical applications
In pH 1.0 HCl medium, 12-tungstophosphoric acid (TP) reacted with promethazine hydrochloride (PMZ) and chlorpromazine hydrochloride (CPZ) to form ion-association complexes, which led to a great enhancement of the resonance nonlinear scattering such as second-order scattering (SOS) and frequency doubling scattering (FDS). Their maximum SOS and FDS peaks were located at 585 nm (TP-PMZ), 584 nm (TP-CPZ) and 388 nm (TP-PMZ), 329 nm (TP-CPZ), respectively. These results provided some indication for the determination of PMZ and CPZ by SOS and FDS methods. The linear range of TP-PMZ and TP-CPZ systems were 0.0069-2.5 ?g mL -1, 0.102-5.0 ?g mL -1 (SOS) and 0.079-6.0 ?g mL -1, 0.0133-5.0 ?g mL -1 (FDS), respectively. The detection limits (3 ?) of PMZ and CPZ were 2.08 ng mL -1, 3.07 ng mL -1 (SOS) and 2.22 ng mL -1, 3.98 ng mL -1 (FDS), respectively. In this work, the optimum reaction conditions, the influences of coexisting substances and ionic strength and analytical application have been investigated. The methods have been successfully applied to the determination of PMZ and CPZ in tablets. In addition, the composition of ion-association complexes and the reaction mechanism are also discussed.
Chen, Peili; Hu, Xiaoli; Liu, Shaopu; Liu, Zhongfang; Song, Yanqi
Long-term effect of imidapril hydrochloride compared with dilazep hydrochloride administration on blood pressure and renal function in patients with chronic glomerulonephritis.
The objective of the present study was to compare the effects of imidapril hydrochloride, an angiotensin converting enzyme inhibitor, and dilazep hydrochloride, an antiplatelet agent, on urinary protein excretion and renal function in patients with chronic glomerulonephritis. Imidapril (2.5 or 5 mg/day) or dilazep (300 or 450 mg/day) was administered for 3 years. Blood pressure, proteinuria, and renal function were measured before and during the treatment. In the group administered imidapril (n = 11), urinary protein decreased by approximately 50% (2.16 +/- 1.57 versus 0.90 +/- 0.53 g/g Cr, P < 0.01) and blood pressure by 14/10 mmHg (139.6 +/- 17.4/93.6 +/- 8.7 mmHg versus 122.7 +/- 10.5/81.8 +/- 9.9 mmHg, P < 0.01) and both remained at low levels during the three years of treatment. No correlation was observed between the extent of blood pressure reduction and changes in urinary protein. Serum creatinine concentrations did not change significantly (1.3 +/- 0.3 versus 1.3 +/- 0.3 mg/dL, NS). In the dilazep group (n = 12), there were no significant changes in blood pressure, urinary protein, or serum creatinine. These findings demonstrate that imidapril reduces proteinuria and contributes to preserve renal function, suggesting its usefulness in the treatment of patients with chronic glomerulonephritis. PMID:16157961
Satonaka, Hiroshi; Suzuki, Etsu; Hayakawa, Hiroshi; Nishimatsu, Hiroaki; Nagata, Daisuke; Oba, Shigeyoshi; Kamijo, Atsuko; Takeda, Ryo; Takahashi, Masao; Yamamoto, Yuji; Kimura, Kenjiro; Hirata, Yasunobu
A new hydrophilic interaction liquid chromatographic (HILIC) procedure for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold formulations.
A new HILIC method has been developed for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold syrup. Mobile phase consists of methanol:water (containing 6.0 g of ammonium acetate and 10 mL of triethylamine per liter, pH adjusted to 5.2 with orthophosphoric acid), 95:5 (v/v). Column containing porous silica particles (Supelcosil LC-Si, 25 cm x 4.6 mm, 5 microm) is used as stationary phase. Detection is carried out using a variable wavelength UV-vis detector at 254 nm for PSH and DPH, and at 280 nm for DXH. Solutions are injected into the chromatograph under isocratic condition at constant flow rate of 1.2 mL/min. Linearity range and percent recoveries for PSH, DPH and DXH were 150-600, 62.5-250, 75-300 microg/mL and 100.7%, 100.1% and 100.8%, respectively. Method is stability indicating and excipients like saccharin sodium, sodium citrate, flavour and sodium benzoate did not interfere in the analysis. Compounds elute in order of increasing ionization degree caused by cation-exchange mechanism in a run time of less than 15 min. Mobile phase pH is manipulated to regulate ionization and ion-exchange interaction and thereby retention of compounds. PMID:16887317
Ali, Mohammed Shahid; Ghori, Mohsin; Rafiuddin, Syed; Khatri, Aamer Roshanali
In vitro interactions of amantadine hydrochloride, R-(-)-deprenyl hydrochloride and valproic acid sodium salt with antifungal agents against filamentous fungal species causing central nervous system infection.
The mortality rates of fungal infections that affect the central nervous system are high in consequence of the absence of effective antifungal drugs with good penetration across the blood-brain barrier and the blood-cerebrospinal fluid barrier. In the present work in vitro antifungal activities of three good penetrating non-antifungal drugs (amantadine hydrochloride, R-(-)-deprenyl hydrochloride, valproic acid sodium salt) and their combinations with three antifungal agents (amphotericin B, itraconazole, terbinafine) were tested with broth microdilution method against eight fungal isolates belonging to Zygomycetes (Lichtheimia corymbifera, Rhizomucor miehei, Rhizopus microsporus var. rhizopodiformis, Saksenaeavasiformis) and Aspergillus genus (A. flavus, A. fumigatus, A. nidulans, A. terreus). These are known to be possible agents of central nervous fungal infections (CNFI). When used alone, the investigated nonantifungal drugs exerted slight antifungal effects. In their combinations with antifungal agents they acted antagonistically, additively and synergistically against zygomyceteous isolates. Primarily antagonistic interactions were revealed between the investigated drugs in case of Aspergilli, but additive and synergistic interactions were also observed. The additive and synergistic combinations allowed the usage of reduced concentrations of antifungal agents to inhibit the fungal growth in our study. These combinations would be a basis of an effective, less toxic therapy for treatment of CNFI. PMID:23134606
Galgóczy, L; Tóth, Liliána; Virágh, M; Papp, T; Vágvölgyi, C S
A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation
A stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method was developed for simultaneous determination of ambroxol hydrochloride (AMB), cetirizine hydrochloride (CTZ), methylparaben (MP) and propylparaben (PP) in liquid pharmaceutical formulation. The desired chromatographic separation was achieved on an Agilent Eclipse plus C18, 1.8 ?m (50 × 2.1 mm) column using gradient elution at 237 nm detector wavelength. The optimized mobile phase consists of a mixture of 0.01 M phosphate buffer and 0.1 % triethylamine as a solvent-A and acetonitrile as a solvent-B. The developed method separates AMB, CTZ, MP and PP in presence of twelve known impurities/degradation products and one unknown degradation product within 3.5 min. Stability indicating capability was established by forced degradation experiments and seperation of known and unknown degradation products. The lower limit of quantification was established for AMB, CTZ, MP and PP. The developed RP-UPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method is applied for simultaneous estimation of AMB, CTZ, MP and PP in commercially available syrup samples. Further, the method can be extended for estimation of AMB, CTZ, MP, PP and levo-cetirizine (LCTZ) in various commercially available dosage forms.
Trivedi, Rakshit Kanubhai; Patel, Mukesh C.; Jadhav, Sushant B.
A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation.
A stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method was developed for simultaneous determination of ambroxol hydrochloride (AMB), cetirizine hydrochloride (CTZ), methylparaben (MP) and propylparaben (PP) in liquid pharmaceutical formulation. The desired chromatographic separation was achieved on an Agilent Eclipse plus C18, 1.8 ?m (50 × 2.1 mm) column using gradient elution at 237 nm detector wavelength. The optimized mobile phase consists of a mixture of 0.01 M phosphate buffer and 0.1 % triethylamine as a solvent-A and acetonitrile as a solvent-B. The developed method separates AMB, CTZ, MP and PP in presence of twelve known impurities/degradation products and one unknown degradation product within 3.5 min. Stability indicating capability was established by forced degradation experiments and seperation of known and unknown degradation products. The lower limit of quantification was established for AMB, CTZ, MP and PP. The developed RP-UPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method is applied for simultaneous estimation of AMB, CTZ, MP and PP in commercially available syrup samples. Further, the method can be extended for estimation of AMB, CTZ, MP, PP and levo-cetirizine (LCTZ) in various commercially available dosage forms. PMID:21886901
Trivedi, Rakshit Kanubhai; Patel, Mukesh C; Jadhav, Sushant B
Dietary zilpaterol hydrochloride. I. Feedlot performance and carcass traits of steers and heifers.
Experiments were conducted at 3 US locations (CA, ID, and TX) to determine the effects of dietary zilpaterol hydrochloride (Zilmax, Intervet Inc., Millsboro, DE) and duration of zilpaterol feeding on performance and carcass merit of finishing steers and heifers. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d -1) and assigned randomly within BW strata to 1 of 4 treatments in a randomized complete block design (4 blocks/treatment for each sex). The 4 treatments were arranged in a 2 (no zilpaterol vs. zilpaterol) x 2 (20 or 40 d duration of zilpaterol feeding) factorial arrangement of treatments. When included in the diet, zilpaterol was supplemented at 8.3 mg/kg of DM. Each pen consisted of 10 animals. Each animal was individually weighed unshrunk on d 1, 21 or 41, and 66 of the experiment. Following d 66, cattle were slaughtered and carcass data collected. Feeding zilpaterol increased (P<0.01) final BW of steers and heifers by 11.6 and 6.7 kg, respectively. In addition, feeding zilpaterol hydrochloride increased (P or= 0.12) and KPH (P >or= 0.70) were not affected by feeding zilpaterol to steers or heifers. Feeding zilpaterol decreased (i.e., improved; P=0.02) calculated yield grade of steer and heifer carcasses. Marbling score (P=0.002) and quality grade (P=0.002) were decreased when zilpaterol hydrochloride was fed to steers, and the decrease in marbling score and quality grade tended to be greater when zilpaterol was fed for 40 compared with 20 d (zilpaterol x duration interaction, P=0.07). For heifers, marbling score tended (P=0.07) to be decreased and quality grade was decreased (P=0.05) when zilpaterol hydrochloride was fed. In general, it appears from these data that zilpaterol hydrochloride fed for 20 to 40 d at the end of the finishing period enhances growth performance and carcass muscle deposition for steers and heifers. PMID:19098247
Montgomery, J L; Krehbiel, C R; Cranston, J J; Yates, D A; Hutcheson, J P; Nichols, W T; Streeter, M N; Bechtol, D T; Johnson, E; TerHune, T; Montgomery, T H
Synthesis, characterization and molecular sensing behavior of [ZnCl 2(? 3-N,N,O-dpkbh)] (dpkbh = di-2-pyridyl ketone benzoyl hydrazone)
The reaction between ZnCl 2 and di-2-pyridyl ketone benzoyl hydrazone (dpkbh) in acetonitrile under ultrasonic or reflux conditions gave [ZnCl 2(? 3-N,N,O-dpkbh)] in good yield. The identity of the compound was established from the results of its elemental analysis and a number of spectroscopic measurements. Solid-state infrared spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] reveal the coordination of dpkbh, the presence of the amide proton and binding of the oxygen atom of dpkbh. 1H NMR spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] show sensitivity to solvent and temperature variations and confirm the coordination of dpkbh. The electronic absorption spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] in non-aqueous media show high sensitivity to changes in their surroundings and divulge two interlocked intra-ligand-charge transfer (ILCT) transitions of the donor-acceptor type between 300 and 500 nm. Optical measurements show reversible inter-conversion between two forms of [ZnCl 2(? 3-N,N,O-dpkbh)] that may be due to complex-substrate interactions and thermodynamic analysis gave changes in enthalpy (? H?) of -23.3 and +14.1 kJ mol -1, entropy (? S?) of -51 and +31 J mol -1K -1, and free energy (? G?) of -8.16 and +4.54 kJ mol -1 at 298.15 K in DMF and DMSO, respectively. Substrates in concentrations as low as 10 -5 M can be detected and determined using [ZnCl 2(? 3-N,N,O-dpkbh)] in polar solvents. A provisional model for the binding of substrate to [ZnCl 2(? 3-N,N,O-dpkbh)] is developed and a binding constant in the range 6000-8000 M -1 is obtained in the case of ZnCl 2 in DMSO. Electrochemical measurements on [ZnCl 2(? 3-N,N,O-dpkbh)] in DMF show irreversible metal and ligand-based redox processes, and electrochemical reactions of dpkbh with ZnCl 2 show facile coordination of ZnCl 2 and formation of [ZnCl 2(? 3-N,N,O-dpkbh)]. X-ray structural analysis done on a crystal grown from a DMF solution of [ZnCl 2(? 3-N,N,O-dpkbh)] confirmed the identity of [ZnCl 2(? 3-N,N,O-dpkbh)] and shows an extensive network of non-covalent interactions that connects all molecules.
Bakir, Mohammed; Green, Orville; Mulder, Willem H.
Tetratopic pyrimidine-hydrazone ligands modified with terminal hydroxymethyl and acryloyl arms and their Pb(II), Zn(II), Cu(II) and Ag(I) complexes.
The first tetratopic pyrimidine-hydrazone (pym-hyz) molecular strands containing terminal hydroxymethyl (L1) and acryloyl (L2) functional groups have been synthesised. L1 was produced by step-wise imine condensation reactions, starting with 6-hydroxymethyl-2-pyridinecarboxaldehyde. L2 was then synthesised through the treatment of L1 with acryloyl chloride. NMR spectroscopy and X-ray crystallography showed that the ligands adopted a helical shape, comprised of 1 and 1/3 helical turns. Both L1 and L2 uncoiled upon reaction with an excess amount of Pb(II), Zn(II) and Cu(II) ions, resulting in linear M4LA8 complexes (where M = Pb(II), Zn(II), or Cu(II); L = L1 or L2; and A = ClO4(-), SO3CF3(-) or BF4(-)). Horse-shoe shaped Pb2LA4 complexes were also formed by reacting Pb(II) ions with either L1 or L2 in a 2?:?1 metal to ligand ratio. The addition of Ag(I) ions to either L1 or L2 resulted in Ag2L2A2 double helicates, which were stable in the presence of excess Ag(I). The Pb(II), Zn(II) and Ag(I) complexes were characterised by NMR spectroscopy, while UV-Vis spectroscopy was used to probe the Cu(II) complexes. In addition, X-ray crystallography was used to analyse the linear Pb4L1A8, horse-shoe shaped Pb2L1(ClO4)4, twisted Cu3L2(SO3CF3)6, and double helicate Ag2L12(SO3CF3)2 complexes yielding the structures [Pb4L1(ClO4)7(H2O)]ClO4·4CH3NO2 (1), [Pb4L1(SO3CF3)8]2·6CH3CN·H2O (2), [Pb2L1(ClO4)2(CH3CN)(H2O)](ClO4)2·2CH3CN·C4H10O·H2O (3), [Cu3L2(SO3CF3)3(CH3CN)2(H2O)](SO3CF3)3·2CH3CN·H2O (4) and [Ag2L12](SO3CF3)2·CH3CN·H2O (5), respectively. PMID:24667979
Hutchinson, Daniel J; Hanton, Lyall R; Moratti, Stephen C
Sarpogrelate hydrochloride decreases cardio-ankle vascular index accompanied by increased serum lipoprotein lipase mass in type 2 diabetic patients.
The 5-hydroxytryptamine2A receptor antagonist sarpogrelate hydrochloride exerts its effect not only by inhibition of platelet aggregation, but also by some pleiotropic effects. We have reported that a low serum lipoprotein lipase (LPL) mass level reflects insulin resistance and may be a risk factor for atherosclerotic diseases. The aim of this prospective study was to clarify the effect of sarpogrelate on serum LPL mass and cardio-ankle vascular index (CAVI) as a marker related to arterial stiffness.Thirty-five type 2 diabetic patients (21 males and 14 females) with ankle brachial indices higher than 0.90 received sarpogrelate hydrochloride 300 mg/day for 6 months. Serum LPL mass and CAVI were measured during the study.After 6 months of sarpogrelate hydrochloride treatment, CAVI decreased significantly (10.11 ± 0.92 to 9.87 ± 0.97, P < 0.05) and serum LPL mass increased significantly (58.2 ± 17.5 to 63.5 ± 21.4, P < 0.05). A negative correlation between change in CAVI and change in serum LPL mass was observed (r = -0.34, P < 0.05). Multiple regression analysis identified a change in serum LPL mass as a significant independent predictor for change in CAVI.We demonstrated that sarpogrelate hydrochloride decreased CAVI accompanied by increased serum LPL mass in type 2 diabetic patients. This result suggests that sarpogrelate hydrochloride improves arterial stiffness and is a potential treatment for diabetic angiopathy. PMID:24898600
Nagayama, Daiji; Ohira, Masahiro; Saiki, Atsuhito; Shirai, Kohji; Tatsuno, Ichiro
A Rapid Stability-Indicating RP-HPLC Method for the Determination of Betaxolol Hydrochloride in Pharmaceutical Tablets.
A stability-indicating reversed-phase high performance liquid chromatography (RP-HPLC) method was developed for the determination of betaxolol hydrochloride, a drug used in the treatment of hypertension and glaucoma. The desired chromatographic separation was achieved on a Nucleosil C18, 4 ?m (150 × 4.6 mm) column, using isocratic elution at a 220 nm detector wavelength. The optimized mobile phase consisted of a 0.02 M potassium dihydrogen phosphate: methanol (40:60, v/v, pH 3.0 adjusted with o- phosphoric acid) as solvent. The flow rate was 1.6 mL/min and the retention time of betaxolol hydrochloride was 1.72 min. The linearity for betaxolol hydrochloride was in the range of 25 to 200 ?g/mL. Recovery for betaxolol hydrochloride was calculated as 100.01%-101.35%. The stability-indicating capability was established by forced degradation experiments and the separation of unknown degradation products. The developed RP-HPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method was applied for the estimation of betaxolol hydrochloride in commercially available tablets. PMID:23531643
Auvity, Sylvain; Chiadmi, Fouad; Cisternino, Salvatore; Fontan, Jean-Eudes; Schlatter, Joël
A Rapid Stability-Indicating RP-HPLC Method for the Determination of Betaxolol Hydrochloride in Pharmaceutical Tablets
A stability-indicating reversed-phase high performance liquid chromatography (RP-HPLC) method was developed for the determination of betaxolol hydrochloride, a drug used in the treatment of hypertension and glaucoma. The desired chromatographic separation was achieved on a Nucleosil C18, 4 ?m (150 × 4.6 mm) column, using isocratic elution at a 220 nm detector wavelength. The optimized mobile phase consisted of a 0.02 M potassium dihydrogen phosphate: methanol (40:60, v/v, pH 3.0 adjusted with o- phosphoric acid) as solvent. The flow rate was 1.6 mL/min and the retention time of betaxolol hydrochloride was 1.72 min. The linearity for betaxolol hydrochloride was in the range of 25 to 200 ?g/mL. Recovery for betaxolol hydrochloride was calculated as 100.01%–101.35%. The stability-indicating capability was established by forced degradation experiments and the separation of unknown degradation products. The developed RP-HPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method was applied for the estimation of betaxolol hydrochloride in commercially available tablets.
Auvity, Sylvain; Chiadmi, Fouad; Cisternino, Salvatore; Fontan, Jean-Eudes; Schlatter, Joel
An HPLC method for the determination of nifekalant hydrochloride in canine plasma and its application to a pharmacokinetic study.
In this study, a simple and selective high-performance liquid chromatography method was developed and validated for the determination of nifekalant hydrochloride in canine plasma. Liquid-liquid extraction was used to separate nifekalant hydrochloride from canine plasma and the mean extraction recoveries of nifekalant hydrochloride and the internal standard were 82.31 and 94.81%, respectively. The chromatographic separation was performed on a Dikma Diamonsil column with a mobile phase consisting of acetonitrile-20mM phosphate buffer (pH 6.2; 30:70, v/v) with flow rate of 1.0 mL/min. The standard curve was linear over the concentration range of 20-10,000 ng/mL (r(2) > 0.99). The intra-batch and inter-batch accuracy for nifekalant hydrochloride at four concentrations were 93.14-100.47% and 96.12-103.77%, respectively. The relative standard deviations were less than 15%. The method was successfully applied to a pharmacokinetic study after the intravenous administration of nifekalant hydrochloride to beagle dogs. PMID:23169932
Zhou, Yi; Liu, Xiu-Mei; Wang, Ling; Jiang, Xue-Hua
Determination and validation of duloxetine hydrochloride in capsules by HPLC with pre-column derivatization and fluorescence detection.
A high-performance liquid chromatographic (HPLC) method is described for the determination of duloxetine hydrochloride in capsules. The method was based on pre-column derivatization with 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole using the fluorimetric detection technique. Duloxetine hydrochloride was analyzed by HPLC using an Inertsil C18 column (5 ?m, 150 × 4.6 mm) and mobile phase consisted of methanol and water (65:35, v/v). The fluorescence detector was adjusted at excitation and emission wavelengths of 461 and 521 nm, respectively. The linearity of the method was in the range of 10-600 ng/mL. Limits of detection and quantification were 0.51 and 1.53 ng/mL, respectively. The proposed method was successfully applied for determination of duloxetine hydrochloride in its pharmaceutical preparation. The results were in good agreement with those obtained using a reference method. PMID:22511287
Tatar Ulu, Sevgi
Comparison of Neurotropic Effects of L-Glutamic Acid and Its New Derivative ?-Phenylglutamic Acid Hydrochloride (RGPU-135, Glutarone).
In contrast to L-glutamic acid (200 mg/kg), ?-phenylglutamic acid hydrochloride (26 mg/kg) produces no anticonvulsant effects during generalized convulsions induced by "maximum electric shock". However, ?-phenylglutamic acid hydrochloride was more potent than L-glutamic acid in increasing survival rate, promoting recovery of spontaneous motor activity, and maintainance locomotor and exploratory activity in the open fi eld test and cognitive functions in conditioned passive avoidance test, i.e. exhibited neuroprotective activity. This substance did not change the threshold of pain induced by electric stimulation of paws (up to vocalization) and thermal tail stimulation (tail-fl ick), whereas L-glutamic acid decreased this parameter. ?-Phenylglutamic acid suppressed aggression in the test for provoked unmotivated aggression, while L-glutamic acid enhanced it. Due to these neurotropic effects, ?-phenylglutamic acid hydrochloride can be used as the basis for the development of drugs with antidepressant, anxiolytic, and neuroprotective actions. PMID:24824696
Tyurenkov, I N; Bagmetova, V V; Chernysheva, Yu V; Merkushenkova, O V
Hydrogen bonds in the crystal packings of mesalazine and mesalazine hydrochloride
The crystal structures of pharmaceutical product mesalazine (marketed also under different proprietary names as Salofalk, Asacol, Asacolitin, and Claversal) and its hydrochloride are reported. In the crystal mesalazine is in zwitterion form as 5-ammoniosalicylate ( 1) whereas mesalazine hydrochloride crystallizes in an ionized form as 5-ammoniosalicylium chloride ( 2). Compound 1 (C 7H 7O 3N) crystallizes in the monoclinic space group {P2 1}/{n} with a = 3.769(1) Ĺ, b = 7.353(2) Ĺ, c = 23.475(5) Ĺ, ? = 94.38(2)°, V = 648.7(8) Ĺ3, Z = 4, Dc = 1.568 g cm -3 and ?( MoK?) = 1.2 cm -1. Compound 2 (C 7H 8O 3NCl) crystallizes in the triclinic space group P 1Ż with a = 4.4839(2) Ĺ, b = 5.7936(2) Ĺ, c = 15.6819(5) Ĺ, ? = 81.329(3)°, ? = 88.026(3)°, ? = 79.317(4)°, V = 395.74(3) Ĺ3, Z = 2, Dc = 1.591 g cm -3 and ?(CuK ?) = 40.8 cm -1. The crystal structures were solved by direct methods and refined to R = 0.041 for 1 and 0.028 for 2, using 607 and 1374 observed reflections, respectively. The configuration of both molecules, with the ortho hydroxyl to a carboxyl group, favours the intramolecular hydrogen bonds. Very complex systems of intermolecular hydrogen bonds were observed in both crystal packings. They are discussed in terms of graph-set notation. The mesalazine crystal structure is characterized by two-dimensional network of hydrogen bonds in the ab plane. The crystal structure pattern of mesalazine hydrochloride is a three-dimensional network significantly supported by N +?H⋯Cl - interactions.
Bani?-Tomiši?, Z.; Koji?-Prodi?, B.; Širola, I.
Comparison of two different formulations of mebeverine hydrochloride in irritable bowel syndrome.
A total of 213 patients were recruited to a multicentre, randomised, double-blind, double dummy, general practice study lasting eight weeks. The objectives of the study were (i) to demonstrate therapeutic equivalence of mebeverine hydrochloride 200 mg b.i.d. capsules (Colofac MR) and 135 mg t.i.d. tablets (Colofac) in the treatment of abdominal pain in irritable bowel syndrome (IBS) and (ii) to evaluate safety and physicians' and patients' assessments of therapeutic response. Patients were randomised at day 0 and assessments performed after four and eight weeks. Primary and secondary efficacy endpoints were number of responders (response being defined as 50% or more improvement in global mean visual analogue scale for abdominal pain); patients' and physicians' global assessment of therapeutic response; and physicians' global impression of patient symptoms. Safety was assessed from adverse event reports and routine laboratory tests. Therapeutic equivalence was proven statistically (difference < 18%; p = 0.003), with 65/92 (71%) of the 135 mg t.i.d. group and 64/92 (70%) of the 200 mg b.i.d. group classified as responders. The patients' evaluation of response (week 8) was that 75% of 135 mg t.i.d. and 81% of 200 mg b.i.d. improved; the physicians' assessment of therapeutic response (week 8) was that 64% of 135 mg t.i.d. and 70% of 200 mg b.i.d. had no or mild symptoms. In conclusion, Mebeverine hydrochloride 200 mg b.i.d. (Colofac MR) was shown to be therapeutically equivalent to mebeverine hydrochloride 135 mg t.i.d. (Colofac) in the treatment of abdominal pain in IBS. Results for the secondary efficacy variables were comparable. No safety concerns were identified. PMID:11070572
Gilbody, J S; Fletcher, C P; Hughes, I W; Kidman, S P
Denaverine hydrochloride and carbetocin increased welfare during and after parturition and enhanced subsequent fertility in cattle.
The objectives of the current study were to investigate the influence of denaverine hydrochloride and carbetocin on softening and dilatation of the birth canal, the need for assistance during parturition, calf mortality, retention of fetal membranes, endometritis, and subsequent fertility. Altogether 200 animals (100 cows and 100 heifers) of the Simmental breed were divided into 2 groups: treatment (n=100) and control (n=100). Animals in the treatment group received denaverine hydrochloride and carbetocin (a maximum of twice for each, depending on the progression of labor) during delivery over a maximum of 4 waiting periods (30min each), whereas control animals experienced the same waiting periods but received no treatment. The treatment protocol had a positive influence on the ease of calving and postpartum reproductive health. The treatment increased the number of animals with the birth canal dilated by more than 25cm, and halved the need for any assistance at parturition. In addition, treatment decreased the occurrence of difficult calving, the need for episiotomy, the appearance of birth canal lesions, and clinical endometritis. The treatment protocol had an effect throughout the entire puerperal period, as treated animals conceived with fewer artificial inseminations (1.3 vs. 1.6 artificial inseminations/pregnancy) and sooner (67 vs. 78d open) compared with control animals. Denaverine hydrochloride and carbetocin administered in combination during parturition affected the progression and ease of calving, and thus the welfare of cows in labor and subsequently. However, further studies are needed to confirm the findings and to establish best practices. PMID:24731624
Zobel, Robert; Taponen, Juhani
Zilpaterol Hydrochloride on Performance and Sperm Quality of Lambs Fed Wet Brewers Grains
Aguilera-Soto, J.I., Ramirez, R.G., Arechiga, C.F., Mendez-Llorente, F., Lopez-Carlos, M.A., Silva-Ramos, J.M., Rincón-Delgado, R.M. and Duran-Roldan, F.M. 2008. Zilpaterol hydrochloride on performance and sperm quality of lambs fed wet brewers grain. J. Appl. Anim. Res., 34: 17–21.Forty Rambouillet × elibuey male lambs were grouped as light-weight (LW; n =20; 28±1.2 kg BW) and heavy-weight (HW; n = 20; 40.5±1.6 kg
J. I. Aguilera-Soto; R. G. Ramirez; C. F. Arechiga; F. Mendez-Llorente; M. A. Lopez-Carlos; J. M. Silva-Ramos; R. M. Rincon-Delgado; F. M. Duran-Roldan
Metabolomic Analyses of Blood Plasma after Oral Administration of D-Glucosamine Hydrochloride to Dogs
D-Glucosamine hydrochloride (GlcN?HCl) is an endogenous amino monosaccharide synthesized from glucose that is useful in the treatment of joint diseases in both humans and animals. The aim of this study was to examine amino acid metabolism in dogs after oral administration of GlcN?HCl. Accelerated fumarate respiration and elevated plasma levels of lactic acid and alanine were observed after administration. These results suggest that oral administration of GlcN?HCl induces anaerobic respiration and starvation in cells, and we hypothesize that these conditions promote cartilage regeneration. Further studies are required to evaluate the expression of transforming growth factor-beta (TGF-?).
Osaki, Tomohiro; Azuma, Kazuo; Kurozumi, Seiji; Takamori, Yoshimori; Tsuka, Takeshi; Imagawa, Tomohiro; Okamoto, Yoshiharu; Minami, Saburo
Melt-in-Mouth Pellets of Fexofenadine Hydrochloride Using Crospovidone as an Extrusion–Spheronisation Aid
Microcrystalline cellulose (MCC) is well established as an extrusion spheronisation aid for the preparation of pellets. Crospovidone\\u000a (Polyplasdone® XL-10) is compared with microcrystalline cellulose for the preparation of melt-in-mouth pellets. Taste-masked\\u000a fexofenadine hydrochloride was incorporated in the melt-in-mouth formulation. Crospovidone was found to be well suited as\\u000a extrusion–spheronisation aid for the preparation of melt-in-mouth pellets. The great advantage of crospovidone
Satishkumar P. Jain; Dharmini C. Mehta; Sejal P. Shah; Pirthi Pal Singh; Purnima D. Amin
Photostabilization of doxorubicin hydrochloride with radioprotective and photoprotective agents: Potential mechanism for enhancing chemotherapy during radiotherapy
p-Aminobenzoic acid (PABA), urocanic acid, and sodium urate were found to significantly enhance the photostability of doxorubicin hydrochloride (adriamycin, (ADR)). d1-Methionine, thiourea, and glycine also increased the photostability of this drug, but to a lesser degree. Sodium thiosulfate on the other hand, was found to be detrimental to the photostability of ADR. The photostabilizing effect of PABA was found to increase with increase of its concentration and was influenced by the pH and the buffer species of the vehicle. The findings would have an impact on the enhancement of therapeutic efficacy of adriamycin when administered during radiation therapy.
Habib, M.J.; Asker, A.F.
[Effect of promethazine hydrochloride (pipolphen) on the stability of R plasmid resistance in Escherichia coli].
The influence of promethazin hydrochloride (pipolphen) on stability of R plasmid inheritance in Escherichia coli strains of various serogroups was studied. The strains were isolated from patients with acute intestinal infection and from healthy persons. It was shown that in subbacteriostatic concentrations (100 to 450 micrograms/ml) pipolphen promoted elimination of the R plasmids. Decreased stability of the R plasmid inheritance was not associated with the pipolphen concentration. No influence of the drug on the biochemical characteristics, antigenic properties and nutritional requirements of the plasmid-free derivatives was detected. The eliminating action of pipolphen and ethidium bromide in some strans of Escherichia coli was shown to be different. PMID:9334148
Evdokimova, O V; Smirnov, I V; Artem'eva, N A; Rozhkova, E A
[Testing of bioequivalence of a new sotalol hydrochloride preparation in comparison to a standard formulation].
An investigation on the bioavailability of a new tablet with 160 mg sotalol hydrochloride (CAS 959-24-0, Rentibloc 160), was performed in a two-way cross-over study with 16 volunteers. The relative bioavailability with respect to a reference preparation for AUC0-infinity was 98.1% and for Cmax 100.8%. A positive decision for bioequivalence derived from the usual confidence intervals for both parameters. The difference in tmax showed no clinical relevance. The new formulation is bioequivalent to the reference. PMID:7575745
Micro-determination of warfarin sodium, nicoumalone and acebutolol hydrochloride in pharmaceutical preparations.
A simple, selective and sensitive spectrophotometric method has been developed for the determination of microgram quantities of warfarin sodium (WS), nicoumalone (NIC) and acebutolol hydrochloride (ACBH), either in pure form or in pharmaceutical preparations. This method is based on the haloform reaction with a known and excess of standard iodine solution under alkaline conditions. The excess of iodine is determined at pH 3.0 with metol-INH. The absorbance of the resulting p-N-methyl-benzoquinonemonoimine-INH charge-transfer complex is measured at 620 nm. PMID:18965268
Sastry, C S; Rao, T T; Sailaja, A; Rao, J V
Suppression of Glutamate-Induced Excitotoxicity by 2-Cyclopropylimino-3-methyl-1,3-thiazoline Hydrochloride in Rat Glial Cultures
We have screened new drugs with a view to developing effective drugs against glutamate-induced excitotoxicity. In the present\\u000a work, we show effects of a new drug, 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride against glutamate-induced excitotoxicity\\u000a in primary rat glial cultures. Pretreatment of glial cells with 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride for\\u000a 2 h significantly protected glial cells against glutamate-induced excitotoxicity in a time- and dose-dependent manner with\\u000a an
Eun-A Kim; Hoh-Gyu Hahn; Key-Sun Kim; Tae Ue Kim; Soo Young Choi; Sung-Woo Cho
Intake of ethanol, sodium chloride, sucrose, citric acid, and quinine hydrochloride solutions by mice: A genetic analysis
Mice of the 129\\/J (129) and C57BL\\/6ByJ (B6) strains and their reciprocal F1 and F2 hybrids were offered solutions of ethanol, sucrose, citric acid, quinine hydrochloride, and NaCl in two-bottle choice tests.\\u000a Consistent with earlier work, the B6 mice drank more ethanol, sucrose, citric acid, and quinine hydrochloride solution and\\u000a less NaCl solution than did 129 mice. Analyses of each
A. A. Bachmanov; D. R. Reed; M. G. Tordoff; R. A. Price; G. K. Beauchamp
Effect of donepezil hydrochloride (E2020) on basal concentration of extracellular acetylcholine in the hippocampus of rats
The effects of oral administration of the centrally acting acetylcholinesterase (AChE) inhibitors, donepezil hydrochloride (donepezil: E2020: (±)-2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-indan-1-one monohydrochloride), tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride) and ENA-713 (rivastigmine: (S)-N-ethyl-3-[(1-dimethyl-amino)ethyl]-N-methyl-phenylcarbamate hydrogentartrate), which have been developed for the treatment of Alzheimer's disease, on the extracellular acetylcholine concentration in the hippocampus of rats were evaluated by using a microdialysis technique without adding cholinesterase inhibitor to the perfusion
Takashi Kosasa; Yuka Kuriya; Kenji Matsui; Yoshiharu Yamanishi
[Successful anesthetic management of three patients with cardiac dysfunction for non-cardiac surgery using olprinone hydrochloride].
Non-cardiac surgery presents significant risks to patients with cardiac dysfunction. The relative safety of different anesthetic techniques has been studied without mentioning any clear indication. The depression of myocardial contractility by anesthetic agents limits their use in patients with cardiac dysfunction, especially for induction of anesthesia. We used olprinone hydrochloride perioperatively in the anesthetic management of three patients. In all cases, anesthetic induction, intraoperative course and the postoperative period proceeded uneventfully. We consider that perioperative use of continuous olprinone hydrochloride infusion may be suitable for patients with cardiac dysfunction for non-cardiac surgery. PMID:16026056
Arai, Takero; Cho, Tamihiro; Enomoto, Sumie; Ichiki, Akemi; Kase, Sachiko; Sato, Eiru; Tsuchida, Misa; Kuno, Yuichiro; Inoue, Hisashi; Okuda, Yasuhisa
[Effect of glucosamine hydrochloride in combination with paracetamol on chondrocyte apoptosis under conditions of systemic steroidal arthritis development in rats].
The effect of a combination of glucosamine hydrochloride with paracetamol on the apoptosis of chondrocytes in the articular cartilage of rats with experimental steroidal dystrophy (osteoarthritis) has been studied by hystochemical methods. Untreated control rats are characterized by a significant increase in the fraction of chondrocytes involved in the processes of apoptosis. The treatment of animals by a combination of glucosamine hydrocloride with paracetamol substantially reduced the percentage of apoptic chondrocytes. The pronounced antiapoptic effect of the investigated combination differed but little from the effect of glucosamine hydrochloride alone, but significantly exceeded the antiapoptic activity of paracetamol. PMID:22702110
Zupanets, I A; Tuliakov, V A; Shebeko, S K
Cerebral perfusion imaging in Alzheimer's disease. Use of single photon emission computed tomography and iofetamine hydrochloride I 123
We used single photon emission computed tomography (SPECT) to study 15 patients with Alzheimer's disease and nine controls. Iofetamine hydrochloride I 123 uptake data were recorded from the entire brain using a rotating gamma camera. Activity ratios were measured for the frontal, posterior parietal, posterior, medial, and lateral cortical temporal regions and striate cortex and were normalized by the activity in the cerebellum. Abnormalities in iofetamine hydrochloride I 123 activity were similar to the abnormalities in glucose metabolism observed with positron emission tomography. Cortical tracer activity was globally depressed in patients with Alzheimer's disease, with the greatest reduction in the posterior parietal cortex.
Johnson, K.A.; Mueller, S.T.; Walshe, T.M.; English, R.J.; Holman, B.L.
Pediatric oral solutions with propranolol hydrochloride for extemporaneous compounding: the formulation and stability study.
The aim of this study is to formulate an extemporaneous pediatric oral solution of propranolol hydrochloride (PRO) 2 mg/ml for the therapy of infantile haemangioma or hypertension in a target age group of 1 month to school children and to evaluate its stability. A citric acid solution and/or a citrate-phosphate buffer solution, res