目的 研究注射用益氣復(fù)脈（凍干，YQFM）對人肝微粒體的細(xì)胞色素P450亞型酶CYP1A2、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4活性的影響。方法 差速離心法制備人肝微粒體，體外人肝微粒體、YQFM （6.5、32.5、65.0、325.0、650.0、3 250.0和6 500.0 μg/mL）和7種底物探針在還原型輔酶β-NADPH的作用下，37℃水浴孵育30 min，同時設(shè)置陰性對照（空白緩沖液）和陽性對照（各亞酶的選擇性抑制劑）組；應(yīng)用液相色譜-串聯(lián)質(zhì)譜（LC-MS/MS）法測定探針底物的代謝產(chǎn)物生成量，酶活性以相對陰性對照的百分比表示。結(jié)果 與陰性對照組比較，32.5、65.0、325.0、650.0、3 250.0濃度的YQFM對CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6和CYP3A4活性均不發(fā)揮抑制作用；半數(shù)抑制濃度（IC₅₀）均大于6 500 μg/mL。結(jié)論 YQFM在臨床使用過程中發(fā)生藥物相互作用的概率較小。

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.

天津市中藥注射劑關(guān)鍵技術(shù)校企協(xié)同創(chuàng)新實(shí)驗(yàn)室建設(shè)項目（17PTSYJC00090）