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利用探针药物法研究艾瑞昔布对大鼠体内CYP2C9酶的影响。将大鼠随机分为试验组和对照组,每组18只,试验组经口灌胃艾瑞昔布,对照组经口灌胃等量蒸馏水,连续给药7 d(2次/d)。d8,每只大鼠经口灌胃甲苯磺丁脲,并于给药后24 h内眼内眦取血,以HPLC法测定血浆药物浓度,拟合药动学参数,并对两组的药动学参数进行统计学分析。结果表明,试验组的AUC0→24 h、AUC0→∞、tmax、CL和V与对照组相比均有显著性差异(P<0.05)。合用艾瑞昔布后,甲苯磺丁脲的AUC0→24 h和AUC0→∞显著降低,CL明显增加,表明艾瑞昔布诱导CYP2C9酶的活性,加快甲苯磺丁脲的代谢。
Effect of Erucicol on CYP2C9 enzyme in rats by probe drug method. The rats were randomly divided into experimental group and control group, with 18 rats in each group. The experimental group was orally administered with irisoxib by oral gavage, and the control group was orally administered with equal volume of distilled water for 7 days (twice / d). d8. Tolbutamide was orally administered to each rat, and blood was collected from the eye for 24 h after administration. The plasma drug concentration was determined by HPLC, and the pharmacokinetic parameters were fitted. Dynamic parameters for statistical analysis. The results showed that the AUC0 → 24 h, AUC0 → ∞, tmax, CL and V of the experimental group were significantly different from the control group (P <0.05). After using eriocitidine, the toluidineuron AUC0 → 24 h and AUC0 → ∞ decreased significantly, CL increased significantly, indicating that erioxib induced CYP2C9 enzyme activity and speed up the metabolism of tolbutamide.