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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。
OBJECTIVE: To study the pharmacokinetics of ubenimex in human by HPLC-MS / MS and to evaluate the bioequivalence. Methods: Twenty-four healthy male subjects were given oral administration of 30 mg ubenimex capsules and reference preparations in a single crossover study. The plasma concentrations of ubenimex in different time points after administration were determined by DAS 2.0 Software was used to calculate pharmacokinetic parameters and evaluate bioequivalence. Results: The peak time was (0.72 ± 0.28) and (0.80 ± 0.15) h after the single oral administration of the test preparation and the reference preparation. The peak concentrations were (2 416.83 ± 379.56) and (2 291.57 ± 418.92 ) μg · L-1; AUC0 ~ t were (3 950.66 ± 589.84) and (4 012.93 ± 521.49) μg.L-1.h; AUC0 ~ ∞ were (3 957.04 ± 590.19) and (4 016.23 ± 520.60 ) μg.L-1.h; t1 / 2 were (3.49 ± 1.91) and (2.80 ± 1.51) h, respectively. The bioequivalence of test and reference formulations was 98.0% (94.2% -101.9%). Conclusion: Ubenimex capsules are bioequivalent to the reference formulation.