Stereoselective Pharmacokinetics of Diniconazole Enantiomers in Rabbits

文献类型： 外文期刊

第一作者： Cao, Aocheng

作者： Cao, Aocheng;Qiu, Jing;Zhou, Zhiqiang;Zhu, Wentao;Dang, Ziheng;Wang, Xinquan

作者机构：

关键词： stereoselectivity;diniconazole;pharmacokinetics;rabbit

期刊名称：CHIRALITY （ 影响因子：2.437； 五年影响因子：2.204 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： Diniconazole [(E)-(RS)-1-(2,4,-dichlorophenyl)-4,4-dimethyl-2-(1H-1,2,4-triazole-1-yl ) pent-1-en-3-ol)] is a potent triazole fungicide. The enantioselective pharmacokinetics of diniconazole enantiomers in rabbits was studied via intravenous (i.v.) injection. The pharmacokinetics and the enantiomer fraction (EF) were determined using normal high-performance liquid chromatography with diode array detection and a cellulose-tris-(3,5-dimethylphenylcarbamate)-based chiral stationary phase (CDMPC-CSP). The time-concentration curves in plasma were fitted by a two-compartment open mode. The results showed that the concentration of S-diniconazole in plasma decreased faster than that of R-diniconazole, and EFs increased with time after administration of racemic diniconazole (rac-diniconazole). The R-/S-enantiomer ratio of the area under the time-plasma concentration curve (AUC(0-infinity)) after administration was 1.52. The total plasma clearance value of S-enantiomer was 1.57-fold higher than that of the R-diniconazole. These results indicate substantial stereoselectivity in the kinetics of diniconazole enantiomers in rabbit.

分类号： O641

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