摘要
Abstract
Objective To study the pharmacokinetics and bioequivalence of iguratimod tablets in healthy Chinese volunteers.Meth-ods A single-center,two-formulation,two-period,two-sequence crossover design was adopted.32 and 36 healthy volunteers were enrolled in the fasting and postprandial trials,respectively.Volunteers in both the fasting and postprandial groups were administered a single oral dose of 25 mg of the test formulation(T)or the reference formulation(R)of iguratimod tablets in each cycle,with a 7-day washout period.The plasma concentrations of iguratimod were determined by ultra-performance liquid chromatography-tandem mass spectrometry,and the phar-macokinetic parameters were calculated to evaluate the bioequivalence of the two formulations.Results In the fasting group,the Cmax,AUC0-t,and AUC0-∞ of iguratimod after oral administration of T and R were(979.98±207.40)and(893.07±205.60)ng/mL,(12630.13±2709.51)and(12155.84±3010.61)h·ng/mL,and(12911.13±2822.90)and(12531.60±3161.81)h·ng/mL,respectively.In the postprandial group,the Cmax,AUC0-t,and AUC0-∞of iguratimod after oral administration of T and R were(868.32±137.77)and(882.39±135.67)ng/mL,(11152.60±2284.61)and(10956.43±2258.92)h·ng/mL,and(11376.03±2305.92)and(11178.83±2264.61)h·ng/mL,respectively.The 90％confidence intervals(CI)of the geometric mean ratios of Cmax,AUC0-t,and AUC0-∞ for the two preparations under fasting and postprandial trials were 109.81％(101.59％～118.68％)and 99.10％(96.10％～102.19％),105.06％(100.17％～110.18％)and 101.63％(98.42％～104.96％),and 104.11％(99.71％～108.70％)and 101.57％(98.65％～104.59％),respectively,all within the range of 80.00％～125.00％.Conclusion The test and reference formulations of igura-timod tablets have bioequivalence in fasting and postprandial trials.关键词
艾拉莫德片/药动学/生物等效性/安全性Key words
Iguratimod tablets/Pharmacokinetics/Bioequivalence/Safety分类
医药卫生
