Determinations of mifepristone and its metabolites and their pharmacokinetics in healthy female Chinese subjects.
- Author:
Yanni TENG
;
Ruiqian DONG
;
Benjie WANG
;
Huanjun LIU
;
Zhimei JIANG
;
Chunmin WEI
;
Rui ZHANG
;
Guiyan YUAN
;
Xiaoyan LIU
;
Ruichen GUO
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2011;46(10):1241-5
- CountryChina
- Language:English
-
Abstract:
The aim of this study is to establish an HPLC method for simultaneous determinations of mifepristone and its metabolites, mono-demethylated mifepristone, di-demethylated mifepristone and C-hydroxylated mifepristone in plasma and to evaluate the pharmacokinetic characteristics of mifepristone tablet. Twenty healthy female Chinese subjects were recruited and a series of blood samples were collected before and after 0.25, 0.5, 1.0, 1.5, 2.0, 4.0, 8.0, 12.0, 24.0, 48.0, 72.0 and 96.0 hours administration by a single oral dose of 75 mg mifepristone tablet. Mifepristone and its three metabolites were extracted from plasma using ethyl acetate and determined by high performance liquid chromatography. The main pharmacokinetic parameters of mifepristone and its metabolites, including Cmax, tmax, MRT, t(1/2), V, CL, AUC(0-96 h) and AUC(0-infinity), were calculated by Drug and Statistical Software Version 2.0. The simple, accurate and stable method allows the sensitive determinations ofmifepristone and its metabolites in human plasma up to 4 days after oral administration of 75 mg mifepristone tablet and the clinical applications of their pharmacokinetic studies.
