柴胡提取物对氯苯那敏经大鼠肝微粒体代谢抑制的考察  

Inhibition of Bupleurum smithii extract on chlorpheniramine metabolism in rat liver microsomes in vitro

作　　者：惠俊敏[1] 郭延垒[1] 赵德璋[1] 吴明军[1] 于超[1] 

机构地区：[1]重庆医科大学生命科学研究院,重庆400016

出　　处：《中国医院药学杂志》2013年第23期1911-1914,共4页Chinese Journal of Hospital Pharmacy

基　　金：国家科技重大专项(编号:2010ZX09401-306-1-1);重庆市自然科学基金(编号:CSTC;2009BA5083)

摘　　要：目的:研究柴胡提取物对氯苯那敏经肝微粒体代谢的影响。方法:采用HPLC建立氯苯那敏经肝微粒体酶代谢动力学测定方法,以Graphhpad prism5.01软件计算Vmax与Km值及代谢清除率(CLint)值;采用体外温孵法评价柴胡提取物对氯苯那敏经大鼠肝微粒体代谢的影响。结果:氯苯那敏与其代谢产物分离良好且温孵体系内无其他内源性物质干扰;测得氯苯那敏体外酶动力学参数:Vmax为0.625 7 nmol·min-1·mg-1;Km为23.68μmol·L-1;Clint为0.083 mL·min-1·mg-1;柴胡提取物对氯苯那敏经大鼠肝微粒体的代谢产生明显抑制。结论:柴胡提取物对氯苯那敏经大鼠肝微粒体的代谢产生明显抑制,二者联合使用可能产生药物-药物相互作用。OBJECTIVE To investigate the inhibitory effect of Bupleurum smithii extract on chlorpheniramine metabolism in rat liver microsomes in vitro. METHODS A .HPLC method was used to detect the activity of rat liver microsomes by calculation the residual content of chlorpheniramine and the V Km and CLint, were calculated by Graphhpad prism 5.01. Effect of Bupleururn smithii extract on metabolism of chlorpheniramine was evaluated by rat liver microsomes incubation system in vitro. RESULTS Chlorpheniramine was separated well with its metabolite and both were not disturbed by endogenesis substances. The value of Vmax,Km and Glint were calculated as 0. 625 7 nmol.min-1 .mg-1 , 23. 68μmol.L-1 and 0. 083 mL-min·mg^-1, respectively. Bupleurum srnithii extract showed obvious inhibitory effect on chlorpheniramine metabolism in rat liver microsomes in vitro. CONCLUSION Bupleurum smithii extract co-administered with chlorpheniramine could produce drugdrug interactions.

关 键 词：柴胡提取物 氯苯那敏 大鼠肝微粒体 药动学 

分 类 号：R28[医药卫生—中药学]