中国健康女性口服低剂量米非司酮片剂的人体药代动力学

Pharmacokinetics of mifepristone after low oral dose in healthy Chinese women

目的 研究口服低剂量米非司酮在人体内的药代动力学特征。方法18名健康女性志愿者单剂量口服25mg米非司酮片,用HPLC-UV法检测血清中米非司酮及其代谢产物单去甲米非司酮的浓度,用3P97程序对血药浓度—时间数据进行统计处理。结果 米非司酮在人体内的动力学过程较好地符合一级吸收、二室模型,平均t_(max)为0.93h,平均C_(max)为1.12μg·mL_(-1)。平均末端消除相半衰期(t_(1/2 β))为25.4h,平均表观分布体积(V_d/F)为94.8L,平均药时曲线下面积AUC_(0～∝)为11.20μg·h·mL^(-1),平均总清除率为2.7L·h^(-1),平均滞留时间为29.5h。结论 口服25mg米非司酮在人体内药代动力学过程可以用一级吸收、开放的二室模型描述。

Objective To study the pharmacokinetic characteristics of low dose mifepristone given to healthy Chinese women. Methods Eighteen healthy women received a single oral dose of 25 mg mifepristone tablets. The serum concentrations of unchanged mifepristone and its active metabolite, monodemetylated mifepristone were determined by HPLC-UV method. The pharmacokinetc parameters were fitted with the use of 3P97 practical pharmacokinetic program. Results The fitted curves for mifepristone correspond to an open two-compartment model. The pharmacokinetic parameters were as following: tmax was 0.93 h, Cmax was 1.12 ng·mL-1, t1/2B was 25.4 h, Vd/F was 94.8 L, AUC0-. was11.20μg.h·mL-1, CL/F was 2.7 L·h-1, and MRT was 29.5 h. Conclusion A two compartment model with first-order absorption characterized the time course of mifepristone concentrations in healthy Chinese women after oral administration of 25 mg mifepristone.