Single-dose randomized, open-label, 2-way crossover bioequivalence study of clopidogrel 75 mg tablet in healthy volunteers under fasting conditions

Int J Clin Pharmacol Ther. 2009 Mar;47(3):187-94. doi: 10.5414/cpp47187.

Abstract

Aim: This study aimed to assess the bioequivalence of 2 formulations of 75 mg clopidogrel hydrogen sulphate film-coated tablet, under fasting conditions.

Subjects and methods: 64 healthy subjects, age ranging from 19 to 55 years, were enrolled in a single-centre, randomized, single-dose, open-label, 2-way crossover study, with a minimum washout period of 7 days. Plasma samples were collected up to 24 h post dosing. Clopidogrel and clopidogrel carboxylic acid levels were determined by reverse-phase high-performance chromatography coupled to tandem mass spectrometry detection, LC-MS-MS method. Pharmacokinetic parameters used for bioequivalence assessment were the AUClast (area under the concentration-time curve from time zero to time of last observed nonzero concentration) and the Cmax (maximum observed concentration). These parameters were determined from the clopidogrel concentration data using non-compartmental analysis as well for clopidogrel carboxylic acid concentration data.

Results: The 90% CI (90% confidence intervals), obtained by analysis of variance (ANOVA) were within the predefined ranges (80.00 - 125.00%) for both analytes.

Conclusion: Bioequivalence between test and formulations, under fasting conditions, was concluded both in terms of rate and extent of absorption.

Publication types

  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Area Under Curve
  • Chromatography, High Pressure Liquid
  • Clopidogrel
  • Cross-Over Studies
  • Fasting*
  • Female
  • Humans
  • Male
  • Middle Aged
  • Platelet Aggregation Inhibitors / administration & dosage
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / pharmacokinetics*
  • Tablets
  • Tandem Mass Spectrometry
  • Therapeutic Equivalency
  • Ticlopidine / administration & dosage
  • Ticlopidine / adverse effects
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / pharmacokinetics

Substances

  • Platelet Aggregation Inhibitors
  • Tablets
  • Clopidogrel
  • Ticlopidine