利多卡因在人肝微粒体中的体外生物转化  

In Vitro Biotransformation of Lidocaine in Human Liver Microsomes

作　　者：张顺国[1] 唐跃年[1] 李方[1] 

机构地区：[1]上海第二医科大学附属新华医院药剂科,200092

出　　处：《医药导报》2005年第6期459-461,共3页Herald of Medicine

摘　　要：目的建立人肝微粒体体外生物转化利多卡因的方法。方法分别改变反应体系中人肝微粒体的浓度、生物转化时间、利多卡因的浓度,以高效液相色谱(HPLC)法测定利多卡因及其代谢产物单乙基甘氨二甲基苯酰胺(MEGX)和甘氨二甲基苯酰胺(GX)的含量。结果最佳的生物转化条件为:2.0mg·L1利多卡因在1.0g·L1微粒体中,生物转化60min。结论该方法快速有效,可用于利多卡因在人肝微粒体体外代谢的研究。Objective To set up a method for assaying the in vitro biotransformation of lidocaine in human liver microsomes. Methods The concentration of human liver microsomes ,the incubation time and the concentration of lidocaine in the reaction system were separately subjected to scheduled alterations. The contents of lidocaine and its two active metabolites monoethylglycinexylidide and glycinexylidide were determined with HPLC. Results The optimal condition of the reaction system was: 2.0 mg·L -1 of lidocaine in 1.0 g·L -1 microsomal protein reacting for 60 min.. Conclusion The method was shown to be simple, rapid and accurate and may be used in the study of the in vitro metabolism of lidocaine.

关 键 词：利多卡因 单乙基甘氨二甲基苯酰胺 甘氨二甲基苯酰胺 人肝微粒体 高效液相色谱法 

分 类 号：R972.2[医药卫生—药品] R965[医药卫生—药学]