参松养心胶囊对4种CYP450亚型酶活性的影响

Effects of Shensong-Yangxin Capsule on the Four Subtypes of CYP450 in Rats

目的:采用"Cocktail"探针药物法研究参松养心胶囊对大鼠体内4种细胞色素P450(CYP450)亚型酶(CYP3A1、CYP2D1、CYP2C11、CYPIA2)的影响。方法:大鼠灌胃给与低、中、高浓度参松养心胶囊,连续15 d,第16天各组大鼠腹腔注射混合"Cocktail"探针药物(咪达唑仑、美托洛尔、奥美拉唑、咖啡因),测定大鼠给药前后体内4种探针药物的血药浓度并计算各探针药物的药代动力学参数。结果:与空白组相比,低、中、高浓度参松养心胶囊对奥美拉唑、美托洛尔、咪达唑仑的药代动力学参数影响显著,但对咖啡因的药代动力学参数无明显影响。结论:参松养心胶囊对CYP2C11、CYP2D1、CYP3A1酶活性可能存在抑制作用,对CYPIA2酶活性作用不明显。

Objective:To study the effects of Shensong-yangxin capsule on four subtypes of CYP450(CYP3 A1,CYP2 D1,CYP2 C11 and CYP1 A2)in rats by using the method of"Cocktail"probe drugs.Methods:Low,middle and high concentrations of Shensongyangxin capsule were orally administered to rats for 15 days,respectively.On the 16 th day,rats in each group were intraperitoneally injected with"Cocktail"probe drugs(midazolam,metoprolol,omeprazole and caffeine),and plasma concentrations and pharmacokinetic parameters of each probe were determined.Results:Compared with the control group,low,middle and high concentrations of Shengsong-yangxin capsule had significant effects on the pharmacokinetic parameters of omeprazole,metoprolol and midazolam decreased,but no significant influence in caffeine.Conclusion:Shensong-yangxin capsule has no obvious effects on the activity of CYP1 A2,and it may have inhibitory effects on the activities of CYP2 C11,CYP2 D1,and CYP3 A1.