Comparative biodisponibility of a single dose captopril Formulations

Abstract

The aim of this study was to evaluate, on human volunteers, the performance of one captopril tablet formulation (Neo-Química Comércio Indústria Ltda) against one standard tablet formulation (Capoten® 50mg Bristol-Myers Squibb Brasil S.A).Twenty-four healthy volunteers, as assessed by clinical and laboratory test evaluations, were enrolled in the study. The study was of a two way randomised crossover design comparing both captopril formulations. Plasma samples for determination of captopril were obtained by pre-dose and at frequent intervals for up to 24h post to one of the single dose formulations and were quantified by a validated method employing high-pressure liquid chromatography coupled to mass spectrometry (LCMSMS). The subjects were monitored through-out the study and the formulations were considered to be well tolerated. The maximum reached concentration (Cmax) and areas under the curve (AUC0-24h) were compared. Captopril Cmax geometric mean ratio was 108.5% (90% IC=101.8-115.7) of Capoten® values. Captopril AUC(0-24h) geometric mean ratio was 109.3% (90% CI=102.7-116.3) of Capoten®. Since 90% CI for both Cmax and ratio AUC(0-24h) for captopril were within the 80 to 125% interval proposed by both the Food and Drug Administration (FDA) and the National Sanitary Surveillance Agency (ANVISA), it is concluded that Captopril Neo- Química was bioequivalent to Capoten® for both the rate and extent of absorption.