目的 研究苦碟子注射液對(duì)大鼠肝微粒體CYP450酶的體外抑制作用。方法 制備大鼠肝微粒體。將苦碟子注射液分別與混合探針?biāo)幬锓悄俏鞫?、甲苯磺丁脲、奧美拉唑、睪酮和氯唑沙宗共同孵育，UPLC-MS/MS法檢測(cè)各探針?biāo)幬锏拇x物。結(jié)果 在測(cè)定濃度范圍內(nèi)，苦碟子注射液對(duì)CYP2E1、CYP2C9和CYP2C19的活性抑制率小于50%；對(duì)CYP1A2、CYP3A4的IC₅₀值分別為12.68%、8.11%，遠(yuǎn)高于臨床日用藥濃度0.20%~0.80%。結(jié)論 在正常劑量下，苦碟子注射液對(duì)大鼠CYP2E1、CYP2C9、CYP2C19幾乎不顯示抑制作用，對(duì)CYP1A2、CYP3A4幾乎沒有抑制作用。

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.

國家自然科學(xué)基金青年基金資助項(xiàng)目（81503244）；北京中醫(yī)藥大學(xué)基本科研業(yè)務(wù)費(fèi)資助項(xiàng)目（2015-JYB-JSMS042）