Zeng S, Mao H Q
School of Pharmacy, Zhejiang University, Hangzhou, People's Republic of China.
J Chromatogr B Biomed Sci Appl. 1999 Apr 30;727(1-2):107-12. doi: 10.1016/s0378-4347(99)00044-4.
An enantioselective assay for l- and d-fenfluramine in rat liver microsomal incubates was developed. The method involves extraction of fenfluramine from the microsomal incubates, and formation of fenfluramine diastereomeric derivatives with the chiral reagent S-(-)-N-trifluoroacetyl prolyl chloride. Separation and quantitation of the diastereomeric fenfluramine derivatives are carried out by a capillary gas chromatographic system with flame ionization detection. The assay is linear from 1 to 50 microg/ml for each enantiomer. The analytical method affords average recoveries of 92.28 and 96.44% for l- and d-fenfluramine, respectively. The limits of detection and quantitation for the method are 0.1 and 1.0 microg/ml for the l- and d-fenfluramine isomers, respectively. The reproducibility of the assay was <10% (RSD). The method allowed study of the depletion of l- and d-fenfluramine in rat liver microsomal incubates. The stereoselectivity of fenfluramine phase I metabolism was observed.
建立了一种用于测定大鼠肝微粒体孵育物中左旋和右旋芬氟拉明的对映体选择性分析方法。该方法包括从微粒体孵育物中提取芬氟拉明，并与手性试剂S-(-)-N-三氟乙酰脯氨酰氯形成芬氟拉明非对映体衍生物。通过带有火焰离子化检测的毛细管气相色谱系统对芬氟拉明非对映体衍生物进行分离和定量。该分析方法对每种对映体在1至50微克/毫升范围内呈线性。该分析方法对左旋和右旋芬氟拉明的平均回收率分别为92.28%和96.44%。该方法对左旋和右旋芬氟拉明异构体的检测限和定量限分别为0.1和1.0微克/毫升。该分析方法的重现性<10%（相对标准偏差）。该方法可用于研究大鼠肝微粒体孵育物中左旋和右旋芬氟拉明的消耗情况。观察到了芬氟拉明I相代谢的立体选择性。
