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目的:研究脉络宁注射液对大鼠CYP1A2、CYP2E1和CYP3A4活性的影响.方法:14只大鼠随机均分成临床等效剂量组和高剂量组,连续2周静脉给予脉络宁注射液(临床等效剂量组,2 mL/kg;高剂量组,4 mL/kg)前后,均同时灌胃给予3个探针底物(茶碱,30 mg/kg;氯唑沙宗,50 mg/kg;氨苯砜,20 mg/kg),进行采血试验.用HPLC法同时测定大鼠体内各探针的血药浓度,DAS 1.0软件计算药动学参数,并以配对t检验对各组大鼠前后两轮主要药动学参数进行差异性比较.结果:在1个给药疗程(14 d)内,临床等效剂量组大鼠用药前后,3个探针的药动学参数均无显著性变化(P＞0.05);高剂量组大鼠用药后,与用药前相比,茶碱的药动学参数没有显著变化(P＞0.05);氨苯砜和氯唑沙宗的AUC0-24h均有升高趋势(P＜0.05),给药后分别是给药前的1.44倍和1.28倍,同时氯唑沙宗的CL显著降低(P＜0.05).结论:临床等效剂量脉络宁对大鼠CYP1A2、CYP2E1和CYP3A4活性均无显著影响,而高剂量脉络宁对大鼠CYP2E1和CYP3A4均有弱抑制作用.“,”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.