目的 研究注射用益气复脉（冻干，YQFM）对人肝微粒体的细胞色素P450亚型酶CYP1A2、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4活性的影响。方法 差速离心法制备人肝微粒体，体外人肝微粒体、YQFM （6.5、32.5、65.0、325.0、650.0、3 250.0和6 500.0 μg/mL）和7种底物探针在还原型辅酶β-NADPH的作用下，37℃水浴孵育30 min，同时设置阴性对照（空白缓冲液）和阳性对照（各亚酶的选择性抑制剂）组；应用液相色谱-串联质谱（LC-MS/MS）法测定探针底物的代谢产物生成量，酶活性以相对阴性对照的百分比表示。结果 与阴性对照组比较，32.5、65.0、325.0、650.0、3 250.0浓度的YQFM对CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4活性均不发挥抑制作用；半数抑制浓度（IC₅₀）均大于6 500 μg/mL。结论 YQFM在临床使用过程中发生药物相互作用的概率较小。

Objective To study the influence of YiqiFumai Lyophilized Injection(YQFM) on the activities of cytochrome P450 enzymes of human liver microsomes CYP450 in vitro by cocktail probe drugs approach.Methods Human liver microsomes were prepared by differential centrifugation. Human liver microsomea and seven probes were incubated with different concentrations (32.5, 65.0, 325.0, 650.0, 3 250μg/mL) of YQFM at 37℃ in presence of β-NADPH. The concentrations of produced metabolites in the reaction solution were de.termined by liquid chromatography tandem mass spectrometry (LC-MS/MS) method assay. The enzyme activity was expressed as a percentage of the relative negative control.Results Compared with negative control group, YQFM of 32.5, 650, 325, 650, 3250,6 500.0 μg/mL played no inhibitory effect on liver microsomal CYP1A2,CYP2B6, CYP2C19 and CYP3A4 activity, and the median inhibitory concentration (IC₅₀) was greater than 6 500 μg/mL.Conclusion The probability of drug interaction in the process of clinical use of YQFM is small.

天津市中药注射剂关键技术校企协同创新实验室建设项目（17PTSYJC00090）