Objective To observe the effect of the compound Ginkgo Biloba (CG;B) on CYP2E1 and CYP3A4 activity in hepatic alcohol-injuried rats. Methods CGB was orally administrated to the normal and the alcohol-injured hepatic injury model rats. Two group rats underwent 2-cycle pharmacokinetic experiments before and after being treated with CGB ( 250 mg· kg-1 · d - 1 ) for 7 days, in which the rats were concomitantly administered Chlorzoxazone (50 mg/kg) and Dapsone (20 mg/kg) by gastrogavage followed by blood-withdrawing from orbital bleeding at different intervals within 24 hours. Results Before being treated with CGB, compared with normal control group, the AUC0-24 and Cmax of Chlorzoxazone and Dapsone in the model group were decreased significantly ( P ＜ 0.05, P ＜ 0.01 ). However, the AUC0-24, and Cmax of Chlorzoxazone and Dapsone after being treated with CGB in the model group were both larger than those before treatment( P ＜0. 05, P ＜ 0.01 ), and the t1/2 of Chlorzoxazon than that that before treatment. Conclusion CGB could inhibit activities of CYP2E1 and CYP3A4 in alcohol-injuried rats.%目的 研究复方银杏叶胶囊(CGB)对酒精性肝损伤大鼠CYP2E1、CYP3A4活性的影响.方法 正常组和酒精性肝损伤模型组均以CGB [(250 mg/(kg·d)]灌胃,分别在灌胃CGB前及灌胃1周后,灌胃探针药氯唑沙宗(50 mg/kg)及氮苯砜(20 mg/kg),于探针药灌后24 h内不同时间点采血,测定各探针药血药浓度.结果 灌胃CGB前,模型组氯唑沙宗和氨苯砜的AUC0-24、Cmax均显著低于正常组(P＜0.05或P＜0.01).灌胃CGB后,模型组氯唑沙宗和氨苯砜的AUC0-24、Cmax均较灌胃前显著升高(P＜0.05或P＜0.01);且氯唑沙宗的t1/2灌胃CGB后明显高于灌胃前(P＜0.05).结论 CGB能够明显抑制酒精性肝损伤大鼠CYP2E1、CYP3A4酶活性.
展开▼
