Truncated AUC in the evaluation of fluconazole bioequivalence. A cross-over, randomised, open-label study in healthy volunteers

Arzneimittelforschung. 2004;54(11):752-6. doi: 10.1055/s-0031-1297032.

Abstract

The bioequivalence of two capsule formulations (test and reference) containing 200 mg fluconazole (CAS 86386-73-4) was assessed in 24 healthy volunteers in an open, randomised, crossover, 2 periods x 2 sequences single dose study with a minimum washout period of 14 days. Plasma samples were obtained over 168 h (at baseline, 1 h, 2 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 24 h, 48 h, 72 h, 120 h and 168 h after administration) and fluconazole concentrations were determined by means of an HPLC-WV method (limit of quantification: 0.2 microg/mL). Pharmacokinetic parameters used for bioequivalence assessment (AUClast, AUCinf and Cmax) were determined from the fluconazole concentration data using non-compartmental analysis. The results showed that all 90% confidence intervals (obtained by ANOVA) were 100.89-110.24 for Cmax, 99.07-107.35 for AUClast and 95.42-105.17 for AUCinf, that is, all within the predefined ranges. Furthermore AUCs truncated at 24, 48, 72 and 120 h were also within the 80-125% range. It may be therefore concluded that the evaluated formulations are bioequivalent in terms of rate and extent of absorption.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics*
  • Area Under Curve
  • Calibration
  • Chemistry, Pharmaceutical
  • Cross-Over Studies
  • Female
  • Fluconazole / adverse effects
  • Fluconazole / pharmacokinetics*
  • Humans
  • Male
  • Therapeutic Equivalency

Substances

  • Antifungal Agents
  • Fluconazole