Bioequivalence and food effect study of two zaltoprofen preparations in healthy Chinese volunteers .

Abstract

Zaltoprofen, a propionic acid derivative of nonsteroidal anti-inflammatory drug (NSAID), has powerful anti-inflammatory and analgesic effects on inflammatory pain. This study was undertaken to investigate the effect of food on the pharmacokinetic parameters of zaltoprofen capsule (trial preparation, T) and tablet (reference preparation, R), and to assess the relative bioequivalence of two zaltoprofen preparations. In this open-label, randomized, crossover, two-state, four-period study, 24healthy Chinese volunteers were randomized to receive a single oral dose of zaltoprofen capsule/tablet (80mg) under fasting and fed state. Plasma samples were obtained for 24hours and measured by a developed LC-MS/MS method. Pharmacokinetic parameters were calculated using noncompartmental analysis. Safety and tolerability were assessed throughout the study. 24healthy participants received two zaltoprofen preparations. For zaltoprofen capsule and tablet, coadministration of high-fat food significantly decreased C_max by 23 and 22%, respectively; t_max was prolonged by 0.7hours and 0.8hours, while the AUC_last (for T, geometric mean ratio (GMR): 101.81%, 90% confidence interval (CI): 94.71-108.14%; for R, GMR: 101.02%, 90%CI: 93.78-107.12%) was not significantly affect by the food. Under fasting or fed condition, the 90% CI of T/R ratios of the geometric means for the primary pharmacokinetic parameters AUC and C_max were within the acceptance range of 80-125%. These data suggest that the absorption of zaltoprofen is delayed by high-fat-food administration while total exposure is not affected. The two zaltoprofen preparations (capsule and tablet) are bioequivalent under fasting and fed state. .