生物学的同等性とバイオアベイラビリティのジャーナル

概要

Comparative Biological Availability of Clopidogrel Formulation in Healthy Volunteers After a Single Dose Administration

Eduardo Abib Junior, Luciana Fernandes Duarte, Moisés Luís Pirasol Vanunci, Daniela Aparecida de Oliveira, Tatiane Antonelli Stein, Renata Pereira, Antonio Ricardo Amarante, Eunice Mayumi Suenaga and Alessandro de Carvalho Cruz

The study was performed to compare the bioavailability of two clopidogrel 75 mg tablet formulation (Clopidogrel from Sandoz as test formulation and Plavix from Sanofi- Synthelabo Ltda, Brazil, as reference formulation) in 42 volunteers of both sexes. The study was conducted open with randomized two period crossover design and a one week wash out period. Plasma samples were obtained over a 48 hour interval. The carboxylic acid of Clopidogrel, major metabolite of Clopidogrel, was analyzed by LC-MS-MS, in the presence of enalapril maleate as internal standard. With plasma concentration vs. time curves, data obtained from this metabolite, the following pharmacokinetics parameters were obtained: AUC 0-t , AUC 0-inf and C max . Geometric mean of Clopidogrel/Plavix 75 mg individual percent ratio was 100.33% AUC 0-t , 98.96% for AUC 0-inf and 105.83% for C max . The 9 0% confidence intervals were 95.50–105.40%, 94 .45–103.69%, 95.91–116.78%, respectively. Since the 90% confidence intervals for C max , AUC 0-t and AUC 0-inf we r e within the 80–125% interval proposed by Food a nd Drug Administration, it was concluded that Clopidogrel 75 mg Tablet was bioequivalent to Plavix 75 mg tablet according to both the rate and extent of absorption.