65480
document
Development and in vitro/in vivo evaluation of immediate release perindopril tablets . Perindopril erbumine ( PE ) is a BCS ( Biopharmaceutics Classification System ) class 3 drug with high solubility and low permeability . It is an inhibitor of the enzyme that converts angiotensin I ( Angiotensin Converting Enzyme , ACE ) into angiotensin II as well as causing the degradation of the vasodilator bradykinin into an inactive heptapeptide . The aim of this study was to develop an alternative drug product by using a different salt of perindopril and to evaluate the bioequivalence between PE , not still licensed , and perindopril arginine ( PA ) , licensed in many countries , and to prepare PE tablets by using direct compression method . Many different formulations were prepared , among which F3-coded formulation was only selected due to releasing of 98.03 % active substance at 45th minute . Bioequivalence study was planned as a cross-designed , randomized , open-labeled , single-dose , single-center study and conducted in 24 male healthy volunteers via peroral route . The results of bioequivalence study were evaluated for Perindopril and Perindoprilat according to Cmax , tmax and AUC criteria . The geometric mean ratios ( 90 % CI ) of perindopril and perindoprilat followed test and reference drug were calculated for AUC0-t and Cmax , 105.946 % ( 100.218-112.002 % ) and 110.437 % ( 102.534-118.948 % ) ; 109.542 % ( 98.364-121.992 % ) and 115.729 % ( 101.031-132.565 % ) , respectively . The 90 % confidence intervals of them were found within the standard bioequivalence range ( 80-125 % ) .
65481
Intervention_Pharmacological
perindopril tablets
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Intervention_Pharmacological
Perindopril erbumine ( PE )
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Intervention_Pharmacological
perindopril
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Intervention_Pharmacological
F3-coded formulation
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Intervention_Pharmacological
Perindopril
65486
Intervention_Pharmacological
Perindoprilat
65487
Intervention_Pharmacological
perindopril
65488
Intervention_Pharmacological
perindoprilat
65489
Outcome_Other
Cmax
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Outcome_Other
tmax and AUC criteria
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Outcome_Other
geometric mean ratios
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Outcome_Other
AUC0-t
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Outcome_Other
Cmax
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Outcome_Physical
bioequivalence range
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Participant_Sample-size
24
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Participant_Sex
male
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Participant_Condition
healthy volunteers via peroral route