中国临床药理学与治疗学2009，Vol.14Issue(4)：386-390,5.
Cocktail法研究脉络宁注射液对大鼠CYP1A2、CYP2E1和CYP3A4活性的影响
Effects of Mailuoning injection on rat activities of CYP1A2,CYP2E1 and CYP3A4 using a three-drug Cocktail approach
摘要
Abstract
AIM: To investigate the effects of Mai-luoning injection on rat activities of CYP1A2, CYP2E1 and CYP3A4. METHODS: 14 rats were randomly and equally divided into two groups, I.e. Clinically-equivalent-dose group and higher-dose group. Two group rats underwent 2-cycle pharmacokinetie experiments before and after being treated with two doses of Mailuoning injection for 14 days, in which the rats were concomitantly administered Theophylline (30 mg/kg), Chlorzoxazone (50 mg/kg) and Dapsone (20 mg/kg) by gastrogavage, followed by blood-withdrawing from orbital bleeding at different intervals within 24 hours. High-performance liquid chromatography (HPLC) was utilized to simultaneously quantitate 3 probe compounds in rat plasma, and DAS 2.0 Software was used to fit plasma concentration-time curve and calculate their corresponding principal pharmacokinetie parameters, among which the statistical differences were evaluated by Paried t-test. RESULTS: In the 14-day administration period, the 2-cycle pharmacokinetie parameters of 3 probes for the clinically-equivalent-dose group rats exhibited insignificant differences (P > 0.05), meanwhile, after being treated with higher-dose Mailuoning injection, there were no significant differences for theophylline pharmacokinetics in rats, but AUC_(0-24 h), of dapsone and chlorzoxazone after treatment were 1.27 and 1.44 times larger than those before treatment, respectively and chlorzoxazone CL/F became smaller. CONCLUSION: Clinically-equivalent-dose Mailuoning injection did not affect the activities of rat CYP1A2, CYP2E1 and CYP3A4; higher-dose Mailuoning injection could not insignificantly change CYP1A2 activity, but could weakly inhibit activities of CYP2E1 and-CYP3A4.关键词
脉络宁注射液/细胞色素P450/茶碱/氯唑沙宗/氨苯砜Key words
Mailuoning injection/ cytochrome P450/ Theophylline/ Chlorzoxazone/ Dapsone分类
医药卫生引用本文复制引用
陈为烤,居文政,许黎君,刘史佳,谈恒山..Cocktail法研究脉络宁注射液对大鼠CYP1A2、CYP2E1和CYP3A4活性的影响[J].中国临床药理学与治疗学,2009,14(4):386-390,5.基金项目
科技部"十一五"支撑计划课题-药物临床研究关键技术研究与应用(2006BAI14B07) （2006BAI14B07）
