Comparative bioavailability of two fluconazole capsule formulations in healthy volunteers.

This work reports the bioavailability of two fluconazole (CAS 86386-73-4) capsule formulations in 24 healthy volunteers of both sexes who received a single oral dose (150 mg). The study was conducted using an open, randomized, two-period crossover design with two-week washout interval. Plasma samples were obtained up to 168 h after drug administration and fluconazole concentration were analyzed using electrospray tandem mass spectrometry coupled to liquid chromatography. The pharmacokinetic parameters obtained for fluconazole after the administration of each formulation included the area under the curve (AUC) (0-168h), AUC (o-∞) , maximum concentration (C max ), time to reach C max (T max ), elimination constant (K e ) and half-life (T 1/2 )- The 90 % confidence interval for the geometric mean of the individual ratio test formulation/reference formulation were 97.18-108.60 % for AUC 0-168h), 90.87-111.11 % for AUC (0-∞) , 104.88-114.88 % for C max 90.38-136.79 % for K e , 91.87-108.93 % for T 1/2 and (-) 1.5-(-)0.10 for T max (for individual differences). Since for both C max or AUC the 90 % CI are within the interval proposed by the Food and Drug Administration (FDA), the test formulation (Zoltrix™). is bioequivalent to the reference formulation for both the rate and the extent of absorption after single dose administration.