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目的用Cocktail探针药物法,研究血栓通注射液对大鼠肝细胞细胞色素P450(CYP450)的影响。方法分别以茶碱、氯唑沙宗和咪哒唑仑作为CYP1A2,CYP2E1及CYP3A4的探针药,将大鼠随机分为低剂量和高剂量两组,每日尾静脉注射血栓通注射液,采用高效液相色谱法测定连续使用血栓通注射液前后大鼠血浆中相应的探针药物的浓度及其药动学参数。结果连续注射14 d后,与用药前比较,茶碱、氨苯砜的血药浓度及其药动学参数未见显著性改变;但低剂量组和高剂量组中氯唑沙宗的AUC0t-减少,mρax明显降低,CL/F显著增加,t1/2和Vd/F变化不明显。高剂量组中tm ax有所降低(P<0.05)。结论连续注射血栓通注射液14 d后,对CYP2E1酶活性有显著诱导作用,而对CYP3A4、CYP1A2酶活性无影响。
Objective To study the effect of Xueshuantong injection on rat hepatocyte cytochrome P450 (CYP450) by using Cocktail probe drug method. Methods Theophylline, chlorzoxazone and midazolam were used as probe drugs for CYP1A2, CYP2E1 and CYP3A4 respectively. The rats were randomly divided into two groups, low dose and high dose. Thromboxane injection was injected into tail vein each day, The concentrations of the corresponding probe drugs in the plasma of rats before and after the continuous use of Xuesaitong injection and their pharmacokinetic parameters were determined by high performance liquid chromatography. Results After 14 days of continuous injection, no significant changes were found in the plasma concentrations and pharmacokinetic parameters of theophylline and dapsone compared with those before treatment. However, the AUC0t- Decreased, mρax decreased significantly, CL / F increased significantly, t1 / 2 and Vd / F changes were not obvious. Tm ax in high-dose group decreased (P <0.05). Conclusion The continuous injection of Xueshuantong injection for 14 d significantly induced CYP2E1 enzyme activity, but had no effect on CYP3A4 and CYP1A2 enzyme activities.