Bioequivalence study of two clopidogrel film-coated tablet formulations in healthy volunteers

Abstract

The present study was performed to compare the bioavailability of two clopidogrel 75 mg film-coated tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 24 healthy adult male and female subjects under fasting condition. The pharmacokinetic parameters were assessed based on the concentrations of clopidogrel (CAS 120202-66-6) parent compound. In each of the two study periods (separated by a washout of one week) a single dose of test or reference drug was administered.

Plasma concentrations of the drug were determined by LC-MS/MS method. The pharmacokinetic parameters assessed in this study were area under the plasma concentration-time curve from time zero to 24 h (AUC_t), area under the plasma concentration-time curve from time zero to infinity (AUC_inf), the peak plasma concentration of the drug (C_max), time needed to achieve the peak plasma concentration (t_max), and the elimination half life (t_1/2).

The geometric mean ratios (90% CI) of the test drug/reference drug for clopidogrel parent compound were 95.19% (81.63–110.90%) for AUC_t,95.55% (80.50–113.42%) for AUC_inf, and 100.18% (80.87–124.09%) for C_max. The 90% confidence intervals calculated for AUC_t and C_max of clopidogrel parent compound were within the standard bioequivalence range (80–125% for AUC and C_max). It was concluded that the two clopidogrel film-coated tablets (test and reference drug) were bioequivalent in terms of the rate and extent of absorption.

Key words

Adenylate cyclase-coupled ADP receptors - Bioavailability - Bioequivalence - Clopidogrel bisulphate - Clopidogrel parent compound - Pharmacokinetics

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