中文摘要：

目的研究艾迪注射液（斑蝥、人参、黄芪等）对体外人和大鼠肝微粒体中细胞色素P450（CYP450）酶的抑制作用,并比较种属差异性,评价其发生药物相互作用的可能性。方法在肝微粒体孵育体系中,将艾迪注射液分别与混合探针底物（非那西丁/CYP1A2、氯唑沙宗/CYP2E1、右美沙芬/CYP2D6、奥美拉唑/CYP2C19、甲苯磺丁脲/CYP2C9、咪达唑仑/CYP3A4、睾酮/CYP3A4）共同孵育,UPLC-MS/MS检测各探针底物的代谢物生成量,采用Graph Pad v5.0软件计算半数抑制浓度（IC50）。结果艾迪注射液对人和大鼠肝微粒体中CYP1A2、CYP2E1、CYP2D6、CYP2C19和CYP2C9的IC50值在4.101%~10.07%范围内,对人和大鼠肝微粒体中CYP3A4（咪达唑仑）的IC50值分别为169.6%和9.133%,对CYP3A4（睾酮）的IC50值分别为8.472%和49.25%。结论艾迪注射液对CYP1A2、CYP2E1、CYP2D6、CYP2C19、CYP2C9和CYP3A4有不同程度的抑制作用,其中CYP3A4具有明显的种属差异性。

英文摘要：

AIM To investigate the inhibitory effects of Aidi Injection（ Mylabris,Ginseng Radix et Rhizoma,Astragali Radix,etc.） on cytochrome P450（ CYP450） enzymes of human and rat liver microsomes in vitro,and the species difference was compared. In addition,the possibility of drug interaction with Aidi Injection was evaluated. METHODS Aidi Injection was incubated with mixed probe substrates（ phenacetin / CYP1A2,chlorzoxazone /CYP2E1,dextromethorphan / CYP2D6,omeprazole / CYP2C19,tolbutamide / CYP2C19,midazolam / CYP3A4,testosterone / CYP3A4） in the liver microsome incubation system,respectively. The quantitation of metabolites of substrates was achieved by UPLC-MS / MS,the IC50 values were calculated by Graph Pad v5. 0 software. RESULTSThe IC50 values of Aidi Injection on CYP1A2,CYP2E1,CYP2D6,CYP2C19 and CYP2C9 of human and rat liver microsomes were in the range of 4. 101%-10. 07%,those on CYP3A4（ midazolam） of human and rat liver microsomes were 169. 6% and 9. 133%,and those on CYP3A4（ testosterone） were 8. 472% and 49. 25%,respectively. CONCLUSION Aidi Injection shows different degrees of inhibitory effects on CYP1A2,CYP2E1,CYP2D6,CYP2C19,CYP2C9 and CYP3A4. The obvious species difference exists in CYP3A4.