乌苯美司胶囊人体药代动力学和生物等效性试验

目的:采用HPLC-MS/MS法研究乌苯美司胶囊在人体的药代动力学,并评价生物等效性。方法:24例健康男性受试者单次交叉口服30 mg乌苯美司胶囊受试制剂和参比制剂,测定给药后不同时间点血浆中乌苯美司经时血药浓度,采用DAS 2.0软件进行药代动力学参数计算和生物等效性评价。结果:受试者单次口服试验制剂与参比制剂后,达峰时间分别为(0.72±0.28)和(0.80±0.15)h;峰浓度分别为(2 416.83±379.56)和(2 291.57±418.92)μg.L-1;AUC0～t分别为(3 950.66±589.84)和(4 012.93±521.49)μg.L-1.h;AUC0～∞分别为(3 957.04±590.19)和(4 016.23±520.60)μg.L-1.h;t1/2分别为(3.49±1.91)和(2.80±1.51)h。试验制剂与参比制剂的生物等效性为98.0%(94.2%～101.9%)。结论:乌苯美司胶囊试验制剂与参比制剂生物等效。

Pharmacokinetics and bioavailability of ubenimex capsule in healthy volunteers

Objective: To study the pharmacokinetics and bioavailability of ubenimex capsules by HPLC-MS/MS in healthy volunteers.Methods: Twenty-four healthy male volunteers were enrolled in the study.The subjects were orally administered with a single dose of 30 mg ubenimex test or reference preparations.The plasma concentrations of ubenimex were assessed and data were analyzed automatically with DAS 2.0 Pharmacokinetic program.The relative bioavailability of ubenimex capsules was calculated.Results: The parameters of ubenimex test and reference preparations were as following: Tmax,(0.72±0.28) and(0.80±0.15) h;Cmax,(2 416.83±379.56) and(2 291.57±418.92) μg·L-1;AUC0-t,(3 950.66±589.84) and(4 012.93±521.49) μg·L-1·h;AUC0-∞,(3 957.04±590.19) and(4 016.23±520.60) μg·L-1·h;t1/2,(3.49±1.91) and(2.80±1.51) h,respectively.The relative bioavailability of ubenimex capsules was 98.0%(94.2%~101.9%).Conclusion: Ubenimex test preparation is bioequivalent to reference preparation.