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目的以氯唑沙宗作为探针药物,研究苦参对大鼠细胞色素P450 2E1(CYP 2E1)体内代谢活性的影响。方法将Wistar大鼠随机分为对照组、苦参组、苯巴比妥阳性对照组。苦参组大鼠ig给予苦参颗粒(100 mg/kg)溶液,对照组ig给予等体积的生理盐水,阳性对照组ip苯巴比妥注射液50 mg/kg,各组均每日给药1次,连续5 d。第6天各组大鼠尾iv氯唑沙宗(5 mg/kg)溶液,于给药前及给药后不同时间点眼内眦静脉取血0.8 mL,HPLC法测定氯唑沙宗血药浓度。结果与对照组相比,苦参组给予苦参5 d后,氯唑沙宗的AUC和Cmax明显降低(P<0.05、0.01),CL明显升高(P<0.05);而苦参组的主要药动学参数与苯巴比妥组比较无显著差异(P>0.05)。结论苦参可明显诱导大鼠CYP 2E1的体内代谢活性,其作用强度与苯巴比妥相当。
Objective To investigate the effect of Sophora flavescens on the metabolic activity of cytochrome P450 2E1 (CYP 2E1) in rats using chlorzoxazone as a probe drug. Methods Wistar rats were randomly divided into control group, Sophora flavescens group and phenobarbital positive control group. Oxymatrine (100 mg / kg) solution was given to the rats of Sophora flavescens group, and the same volume of normal saline was given to the control group. In the positive control group, the ip phenobarbital injection 50 mg / kg was given to each group daily 1 times for 5 days. On the 6th day, the rats in each group were caudal mixed with chlorzoxazone (5 mg / kg) solution, and 0.8 mL of intraocular vein was taken before administration and at different time points after administration. The plasma concentrations of chlorzoxazone . Results Compared with the control group, the AUC and Cmax of chlorzoxazone significantly decreased (P <0.05, 0.01) and the CL significantly increased (P <0.05) The main pharmacokinetic parameters and phenobarbital group no significant difference (P> 0.05). Conclusion Sophora flavescens can obviously induce the in vivo metabolic activity of CYP 2E1 in rats, and its action intensity is comparable to that of phenobarbital.