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建立HPLC法同时测定血浆中米非司酮及其3个代谢物(单去甲米非司酮、双去甲米非司酮和丙炔醇米非司酮)浓度,评价米非司酮人体药代动力学特征。20名中国健康女性受试者分别单次口服米非司酮75 mg,分别于给药前和给药后0.25,0.5,1.0,1.5,2.0,4.0,8.0,12.0,24.0,48.0,72.0和96.0 h取肘静脉血。采用高效液相色谱法测定米非司酮及其3个代谢物经时血药浓度,液液萃取法进行血浆样品预处理,提取液为乙酸乙酯,内标选用氯雷他定,流动相为甲醇乙腈水三乙胺(25∶47∶28∶0.1),流速1 mL.min 1,检测波长290 nm。米非司酮及其代谢物经DAS 2.0实用药代动力学程序处理,计算主要药代动力学参数Cmax,tmax,MRT,t1/2,V,CL,AUC0 96 h和AUC0∞。本法操作简单、快速、灵敏度高、专属性强,可用于米非司酮体内药代动力学的研究,为其临床应用提供试验依据。
To establish a HPLC method for the simultaneous determination of plasma concentrations of mifepristone and its 3 metabolites (mono-to-mifepristone, bis-mifepristone and propynol-mifepristone) and to evaluate the effect of mifepristone on human Pharmacokinetic characteristics. Twenty healthy female subjects in China were given single oral mifepristone 75 mg respectively before and after 0.25, 0.5, 1.0, 1.5, 2.0, 4.0, 8.0, 12.0, 24.0, 48.0, 96.0 h Elbow vein blood. The plasma concentrations of mifepristone and its three metabolites were determined by HPLC. The plasma samples were pretreated by liquid-liquid extraction. The extract was ethyl acetate. The internal standard was selected with loratadine, mobile phase Methanol acetonitrile water triethylamine (25:47:28:0.1), flow rate 1 mL.min 1, detection wavelength 290 nm. Mifepristone and its metabolites were processed by DAS 2.0 practical pharmacokinetic program to calculate the main pharmacokinetic parameters Cmax, tmax, MRT, t1 / 2, V, CL, AUC0 96 h and AUC0∞. The method is simple, rapid, sensitive and specific. It can be used to study the pharmacokinetics of mifepristone in vivo and provide experimental basis for its clinical application.