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目的:研究注射用益气复脉(冻干)对大鼠3种细胞色素P450酶亚型1A2,3A和2E1体内代谢活性的影响。方法:将大鼠随机分为3组,低、高剂量组和空白对照组。低和高剂量组分别尾静脉注射益气复脉542和1 084 mg·kg-1·d-1,空白对照组给予等体积0.9%Na Cl溶液,连续7 d。d 8灌胃(ig)给予探针药混合溶液,用UPLC检测各探针的血药浓度。结果:与空白对照组相比,高剂量组氯唑沙宗的清除率(CL/F)升高,差异有统计学意义(P<0.05)。各组茶碱和氨苯砜的主要药动学参数均无显著差异。结论:高剂量益气复脉对大鼠CYP2E1有一定的诱导作用,而对CYP1A2和3A并无显著性影响。
AIM: To investigate the effects of Yiqi Fumai Injection (lyophilized injection) on the metabolic activity of three cytochrome P450 enzyme subtypes 1A2, 3A and 2E1 in rats. Methods: The rats were randomly divided into three groups, low and high dose group and blank control group. The low-dose and high-dose groups were injected 542 and 1 084 mg · kg-1 · d-1 of Yiqi Fumai at the tail vein respectively, while the blank control group was given 0.9% NaCl solution at the same volume for 7 days. d 8 gavage (ig) given probe mixture, using UPLC detection of the plasma concentration of each probe. Results: Compared with the blank control group, the clearance rate (CL / F) of chlorzoxazone in the high-dose group increased significantly (P <0.05). The main pharmacokinetic parameters of theophylline and dapsone group showed no significant difference. Conclusion: High-dose Yiqi Fumai can induce CYP2E1 in rats, but not CYP1A2 and 3A.