Objective To compare the pharmacokinetic parameters of nimesulide dispersible tablets(test preparation)and nimesulide tablets(reference preparation)in Chinese healthy subjects and to evaluate the bioequivalence of two formulations.Methods This trial used a single-centre,randomised,open,two-preparation,two-cycle,two-way crossover experimental design.28 subjects were enrolled under fasting and fed conditions,who received a single oral dose of 0.1 g of nimesulide in the test or reference formulation each cycle.Plasma nimesulide concentration was determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS),calculation of pharmacokinetic parameters and bioequivalence evaluation.Results In fasting group,main pharmacokinetic parameters of the subject and reference formulations of nimesulide:Cmax were(6 262.14±1 213.98)and(6 625.36±1 230.09)ng·mL-1,AUC0-t were(4.48 × 104±1.66 × 104)and(4.50 × 104±1.53 × 104)h·ng·mL-1,AUC0-∞ were(4.60 × 104±1.83 × 104)and(4.62 × 104±1.68 × 104)h·ng·mL-1.In fed group,main pharmacokinetic parameters of the subject and reference formulations of nimesulide:Cmax were(6 934.29±1 371.00)and(6 551.85±1 383.91)ng·mL-1,AUC0-t were(4.43 × 104±1.52 × 104)and(4.50 × 104±1.47 × 104)h·ng·mL-1,AUC0-∞ were(4.56 × 104±1.67 × 104)and(4.64 × 104±1.60 × 104)h·ng·mL-1.The 90％confidence intervals for the geometric means of Cmax,AUC0-t,AUC0-∞ for reference and test preparations in the fasting and fed groups were in the range of 80.00％to 125.00％.The incidence of adverse events in both fasting and fed trials was 25.00％(7 cases/28 cases).Conclusion Nimesulide dispersible tablets were bioequivalent to the reference formulation nimesulide tablets in Chinese healthy subjects when taken under both fasting and fed conditions.
关键词
尼美舒利分散片/生物等效性/安全性评价/液相色谱-串联质谱法
Key words
nimesulide dispersible tablets/bioequivalence/safety evaluation/liquid chromatography-tandem mass spectrometry
维普
万方数据