目的 研究苦碟子注射液对大鼠肝微粒体CYP450酶的体外抑制作用。方法 制备大鼠肝微粒体。将苦碟子注射液分别与混合探针药物非那西丁、甲苯磺丁脲、奥美拉唑、睾酮和氯唑沙宗共同孵育，UPLC-MS/MS法检测各探针药物的代谢物。结果 在测定浓度范围内，苦碟子注射液对CYP2E1、CYP2C9和CYP2C19的活性抑制率小于50%；对CYP1A2、CYP3A4的IC₅₀值分别为12.68%、8.11%，远高于临床日用药浓度0.20%~0.80%。结论 在正常剂量下，苦碟子注射液对大鼠CYP2E1、CYP2C9、CYP2C19几乎不显示抑制作用，对CYP1A2、CYP3A4几乎没有抑制作用。

Objective To study the inhibitory effect of Kudiezi Injection on rats liver microsomes CYP450 enzyme in vitro. Methods Rat liver microsomes were prepared. Kudiezi Injection was incubated with mixed probe substrates (phenacetin, tolbutamide, omeprazole, testosterone, and chlorzoxazone) in the liver microsome incubation system, respectively. The quantitation of metabolites of substrates were determined by UPLC-MS/MS method. Results In the range of measured concentrations, the activity inhibition rates of Kudiezi Injection on CYP2E1, CYP2C9, and CYP2C19 were less than 50%. The IC₅₀ values to CYP1A2 and CYP3A4 were 12.68%, 8.11%, which were exceeded the daily clinical dose concentrations of Kudiezi Injection from 0.20% to 0.80%. Conclusion At the normal doses, Kudiezi Injection has almost no inhibitory effect on CYP2E1, CYP2C9, and CYP2C19 in rats, and nearly no inhibitory effect on CYP1A2 and CYP3A4.

国家自然科学基金青年基金资助项目（81503244）；北京中医药大学基本科研业务费资助项目（2015-JYB-JSMS042）