氯代正丁苯酞在大鼠肝微粒体中的代谢研究  

STUDIES ON METABOLISM OF 6-CHLORO BUTYL PHTHALIDE BY RATLIVER MICROSOMES

作　　者：彭仕华[1] 崔燕岩[1] 周同惠[1] 

机构地区：[1]中国医学科学院,中国协和医科大学药物研究所分析室

出　　处：《药学学报》1996年第6期466-471,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：用大鼠肝微粒体体外温孵方法进行了氯代正丁苯酞（ＣＢＰ）代谢转化研究，优化了温孵体系的组成，建立了反相ＨＰＬＣ－ＤＡＤ在线同时分离检测ＣＢＰ及其４个体外代谢产物的分析方法，并比较了在苯巴比妥（ＰＢ）与３－甲基胆蒽（３－ＭＣ）诱导的微粒体中代谢差别。利用ＴＬＣ、柱色谱与制备ＨＰＬＣ分离纯化了３个主要代谢产物，并进行了ＮＭＲ，ＭＳ，ＵＶ等光谱鉴定，确定了其主要代谢产物为γ－羟基氯代正丁苯酞与β－羟基氯代正丁苯酞及它们的立体异构体。The in vitro metabolism of 6-chloro -butyl phthalide(CBP)was studied bv rathepatic microsomes.The constitution of the incubation system was optimized and a RP-HPLC-DADmethod was developed for the on-line analysis of CBP and its metabelites.The difference of themetabolism profiles of CBP by rat liver microsomes induced by phenoharbital(PB)and3-methylcholanthrene(3-MC)was also compared.TLC,column chromatography and preparativeHPLC were used for the isolation and purification of the major metabotites and they were identified as(R/S)γ-hydroxy-CBP and(R/S)β-hydroxy-CBP by UV,NMR and MS.

关 键 词：氯代正丁苯酞 体外代谢 HPLC 肝微粒体 抗癫痫药 

分 类 号：R971.6[医药卫生—药品]