Pharmacokinetics and Bioequivalence of Fluconazole Capsules Manufactured in France and China in Healthy Chinese Participants: Open-Label, Randomized, Single-Dose, 2-Way, Crossover Bioequivalence Study Under Fasted and Fed Conditions

Abstract

This was an open-label, randomized study in healthy Chinese participants to assess the bioequivalence of 2 fluconazole 150-mg capsules under fasted and fed conditions. The study consisted of 2 treatment periods, separated by a 14-day washout period. Thirty-six participants were enrolled, with 18 participants each in the fasted and fed groups. In each treatment period, participants received a single oral dose of the test or reference fluconazole 150-mg capsule. After washout, participants received the alternate treatment. Blood samples for pharmacokinetic analysis were collected from 1 hour before dosing to 72 hours after dosing. The median plasma concentration-time profiles were similar for both treatments under fasted and fed conditions. Bioequivalence of fluconazole between the 2 capsules was demonstrated as 90% confidence intervals of the geometric mean ratios for the maximum plasma concentration and area under the plasma concentration-time curve from time 0 to 72 hours after dosing under fasted and fed conditions were within the acceptable range of 80%-125%. Overall, 7 participants reported at least 1 treatment-emergent adverse event; all were mild in severity. No serious adverse events or deaths were reported. The test fluconazole capsule was bioequivalent to the reference capsule, and a single dose was well tolerated. Clinicaltrials.gov ID: NCT03621072.

Keywords: bioequivalence; clinical trial; fluconazole; healthy Chinese; pharmacokinetics.