文献类型： 外文期刊
作者： Wang, Qiuxia 1 ; Qiu, Jing 2 ; Zhou, Zhiqiang 3 ; Cao, Aocheng 1 ; Wang, Xinquan 4 ; Zhu, Wentao 3 ; Dang, Ziheng 3 ;
作者机构： 1.Chinese Acad Agr Sci, Inst Plant Protect, Beijing, Peoples R China
2.Chinese Acad Agr Sci, Inst Qual Stand & Testing Technol Agroprod, Beijing, Peoples R China
3.China Agr Univ, Dept Appl Chem, Beijing 100094, Peoples R China
4.Zhejiang Acad Agr Sci, Inst Qual & Stand Agroprod, Hangzhou, Zhejiang, Peoples R China
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.
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