Pharmacokinetics and bioequivalence study of two indapamide formulations after single-dose administration in healthy chinese male volunteers

Abstract

The pharmacokinetics and relative bioavailability/bioequivalence of 2 formulations of indapamide were assessed in this paper. The study was conducted in 20 healthy Chinese male volunteers according to an open, randomized, single-blind, 2-way crossover study design with a wash-out phase of 7 days. Blood samples for pharmacokinetic profiling were taken up to 84 h post-dose, and indapamide concentrations in plasma were determined by a validated liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) method. Based on the plasma concentration-time data of each individual in each period, pharmacokinetic parameters, Cmax, AUC0-τ, AUC 0-∞ and t1/2, were calculated by non-compartmental analysis. Pharmacokinetic parameters for test and reference formulations were analyzed statistically to assess bioequivalence of the 2 formulations. The values of Cmax, Tmax, t1/2, AUC 0-τ, AUC0-∞for test and reference formulations were 49.53±5.53 and 47.79±4.68 ng/mL, 1.9±0.6 and 2.0±0.5 h, 22.49±5.93 and 23.23±4.48 h, 859.51±160.92 and 840.90±170.62 ng·h/mL, 934.35±190.60 and 919.52±179.74 ng·h/mL, respectively. The 90% confidence intervals of the T/R-ratios of logarithmically transformed data were within the accepted range of 80-125%. It showed that the 2 formulations of indapamide were bioequivalent. Both preparations were well tolerated and no adverse reactions were found throughout the study. © Georg Thieme Verlag KG Stuttgart · New York.