I相反应体系中蛇床子素及其代谢物的测定  

Determination of osthol and its metabolites in a phase I reaction system

作　　者：苑振亭[1] 徐海燕[2] 王可[1] 高培平[3] 赵中华[1] MING Hu 

机构地区：[1]中国人民解放军第230医院,辽宁丹东118000 [2]沈阳药科大学,辽宁沈阳110016 [3]泰安市中心医院,山东泰安271000 [4]Department of Pharmacological and Pharmaceutical Sci- ences, College of Pharmacy, University of Houston, TX, Houston, USA 77030

出　　处：《中国医院药学杂志》2010年第9期732-735,共4页Chinese Journal of Hospital Pharmacy

基　　金：“十一五”军队中医药研发推广专项课题(编号:2006013004)

摘　　要：目的:建立HPLC测定I相反应体系中蛇床子素及其代谢物。方法:采用鼠肝微粒体研究蛇床子素在I相反应体系的代谢情况,用高效液相色谱法(C18柱)测定其蛇床子素的含量,紫外检测波长为320nm,以7-羟基香豆素内标,线性梯度洗脱。采用HPLC-MS-MS分析蛇床子素及其代谢物。结果:回归方程为Y=0.0224X+7.0×10-5(r=0.9998),蛇床子素在0.47～60μmol.L-1范围内,线性关系良好;蛇床子素的最低检测量(LLOD)和最低定量限(LLOQ)分别是0.2,0.47μmol.L-1。方法回收率均大于98.70%,日内、日间RSD均小于5%。采用HPLC-MS/MS检测到5个代谢产物,推测可能是去甲基蛇床子素和蛇床子素去氢代谢产物的多个顺反异构体。结论:此法简便准确,可用于I相反应体系中蛇床子素及其代谢物的测定。OBJECTIVE To develope a straightforward and sensitive method for determination of osthol and its metabolites in phase I reaction system. METHODS A phase I metabolic reaction with rat liver microsomes of osthol in vitro were performed. The samples were analyzed by reverse-phase HPLC using umbelliferone as internal standard. Osthol was monitored at 320 nm and eluted with a gradient method. Osthol and its metabolites in phase I reaction system were analyzed by HPLC-MS/ MS. RESULTS The linear response range was 0. 47-60umol. L^-1. The recovery rate was all more than 98. 70%. Inter-day and intra-day relative standard deviation was all less than 5%. CONCLUSION The analytical method is simple,accurate and can be used to determine the concentration of osthol in phase I reaction system. When analyzed by HPLC-MS/MS, five metabolites were detected in a phase I reaction system. The major metabolites appeared to be desmethyl osthol and multiple isomers of dehydro-osthol.

关 键 词：蛇床子素 肝微粒体 高效液相色谱法 高效液相色谱-质谱串联法 

分 类 号：R927.2[医药卫生—药学]