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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 study the effects of Bupleurum extract on the metabolism of chlorpheniramine in liver microsomes. Methods: The HPLC method was used to establish chlorpheniramine microsomal enzyme kinetic assay. Vmax and Km values and CLint values were calculated by Graphhpad prism 5.01 software. The in vitro incubation method was used to evaluate the effects of Bupleurum chinense extract Effects of chlorpheniramine on the metabolism of liver microsomes in rats. Results: Chlorphenamine and its metabolites were well separated and no other endogenous substances were interfered in the incubation system. The kinetic parameters of chlorpheniramine in vitro were: Vmax of 0.625 7 nmol · min-1 · mg-1, Km was 23.68μmol·L-1; Clint was 0.083 mL · min-1 · mg-1; Bupleurum extract significantly inhibited the metabolism of chlorpheniramine in rat liver microsomes. Conclusion: Bupleurum chinense extract can significantly inhibit the metabolism of chlorpheniramine in rat liver microsomes. The combined use of Bupleurum chingii and Radix Bupleuri may result in the drug-drug interaction.