高效液相色谱法测定肝微粒体中氯胺酮代谢速率  

Measurement of metabolic rate of ketamine in human hepatic microsome by high-performance liquid chromatography

作　　者：赵芸慧[1] 梁悦[2] 唐冰[1] 虞建刚[1] 冯婉玉[2] 马虹[1] 王俊科[1] 

机构地区：[1]中国医科大学附属第一医院,辽宁沈阳110001 [2]中国医科大学临床药理教研室

出　　处：《山东医药》2008年第11期28-29,共2页Shandong Medical Journal

基　　金：辽宁省教育厅课题项目(编号05L551)

摘　　要：目的为氯胺酮（KET）体外代谢研究提供新方法。方法于人体肝组织线粒体孵育液中加入不同浓度的KET；用高效液相色谱法（HPLC）测定孵育液中不同时点KET的药物浓度，计算KET的代谢速率。结果20例人肝脏微粒体中KET的代谢速率为5．4～11．2（平均8．2）nmol／（min·mg）protein；KET与内标布比卡因分离完全，不受微粒体内源性物质的干扰，保留时间分别为3．4min和5．8min。结论HPLC检测肝微粒体KET体外孵育液中的浓度灵敏度高，专一性强，适用于药物体外代谢速率的研究。Objective To measure the metabolic rate of ketamine in human hepatic microsome by high-performance liguid chromatography （HPLC）. Methods The change of ketamine concentration in an incubation mixture with human liver microsomes was determined by high performance liquid chromatography （HPLC） at the different time points, to calculate the metabolic rate of ketamine . Results The metabolic rate of ketamine in the twenty cases of microsomes was 8. 2 nmol · min^-1 · mg^-1 protein（7.3 - 10. 8）on average. The most rapid rate was 11.2 nmol · min^-1 · mg^-1 protein and was about double to that of the slowest rate, which was 5.4 nmol · min^-1 · mg^-1 protein. On the condition of this study ketamine was totally separated with internal standard bupivacaine and suffered no endogenous material intervention. Retention time of ketamine and internal standard bupivacaine was 3.4 and 5.8 min respectively. Conclusion HPLC method is sensitive and specific to detect the metabolic rate of ketamine in human hepatic microsome and helpful to investigate metabolism of drugs in vitro.

关 键 词：氯胺酮 高效液相色谱法 微粒体 肝 

分 类 号：R969.1[医药卫生—药理学] R917.2[医药卫生—药学]