两种米非司酮片人体生物等效性研究

目的:比较2种米非司酮制剂的人体生物等效性。方法:将24名健康女性志愿者随机交叉单剂量口服米非司酮片(受试制剂)与米非司酮片(参比制剂)50mg,采用LC-MS/MS法测定人血浆中米非司酮浓度,用BAPP2.2版软件和DAS2.1.1版软件计算药动学参数和生物利用度。结果:口服受试制剂与参比制剂后的人体药动学参数分别为Cmax(1405.70±380.50)和(1263.80±258.80)ng·h·mL-1,tmax(0.70±0.30)和(0.60±0.30)h,t1/2β(31.70±7.80)和(28.70±9.40)h,AUC0~120(17821.50±4316.90)和(17612.90±6667.40)ng·h·mL-1,AUC0~∞(19286.40±5024.80)和(19053.40±7742.30)ng·h·mL-1。受试制剂的相对生物利用度为114.60%,AUC0~96的90%置信区间在参比制剂的等效范围内。结论:2种米非司酮制剂生物利用度等效。

Studies on Bioequivalence of Mifepristone Tablets in Healthy Volunteers

Objective：To investigate the bioequivalence of two minefristone preparations in healthy volunteers.Methods：A total of 24 healthy female volunteers were enrolled in arandomized crossover study in which the subjects were randomly assigned to receive single dose of 50 mg minefristone tablet（test preparation）or minefristone tablet （reference preparation）.Plasma concentrations of minefristone were determined by LC-MS-MS method.The pharmaco- kinetic parameters and bioequivalence were calculated with BAPP 2.2 and DAS 2.1 software.Results： The main pharmacokinetic parameters of test and reference preparations were as follows：Cmax（1 405.70±380.50） and （1 263.80±258.80） ng？h？mL-1,tmax （0.70±0.30） and （0.60±0.30） h,t1/2β（31.70±7.80） and （28.70±9.40） h,AUC0~120 （17 821.50± 4 316.90） and （17 612.90±6 667.40） ng？h？mL-1,AUC0~∞（19 286.40±5 024.80） and （19 053.40±7 142.30） ng？h？mL-1.The relative bioavailability of minefristone tablets was114.60%.The 90% confidential intervals（CI）of AUC0~96 of the test preparation was among the bioequivalent threshold compared with that of the reference preparation.Conclusion： Test and reference preparations of mifepristone are bioequivalent.