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 (AUCt), area under the plasma concentration-time curve from time zero to infinity (AUCinf), the peak plasma concentration of the drug (Cmax), time needed to achieve the peak plasma concentration (tmax), and the elimination half life (t1/2).
The geometric mean ratios (90% CI) of the test drug/reference drug for clopidogrel
parent compound were 95.19% (81.63–110.90%) for AUCt,95.55% (80.50–113.42%) for AUCinf, and 100.18% (80.87–124.09%) for Cmax. The 90% confidence intervals calculated for AUCt and Cmax of clopidogrel parent compound were within the standard bioequivalence range (80–125%
for AUC and Cmax). 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
