CYP2C9抑制剂对艾瑞昔布大鼠体内药动学的影响

发布时间：2018-03-31 01:01

  本文选题：艾瑞昔布　切入点：细胞色素P酶　出处：《中国医院药学杂志》2017年16期

【摘要】：目的:考察CYP2C9抑制剂胺碘酮对艾瑞昔布在大鼠体内药动学的影响。方法:40只健康雄性SD大鼠随机分为2组(n=20),实验组连续7 d灌胃胺碘酮灌胃液(40 mg·kg~(-1),qd),对照组灌胃等量空白灌胃液。2组均于第8天单次灌胃艾瑞昔布灌胃液20 mg·kg~(-1),按确定时间点取血,LC-MS/MS法测定艾瑞昔布血药浓度,DAS 2.1.1软件拟合药时曲线并计算药动学参数,SPSS 13.0软件进行统计学分析。结果:实验组和对照组的主要药动学参数如下:AUC0-24 h分别为(1 814.8±693.4)ng·h·mL~(-1)和(1 125.1±457.6)ng·h·mL~(-1);AUC0-∞分别为(2 091.6±887.1)ng·h·mL~(-1)和(1 331.3±592.6)ng·h·mL~(-1);t1/2分别为(7.8±4.5)h和(7.4±3.8)h;tmax分别为(1.7±0.6)h和(1.46±0.60)h;CL分别为(0.01±0.01)L·h~(-1)·kg~(-1)和(0.02±0.01)L·h~(-1)·kg~(-1);V分别为(0.11±0.05)L·kg~(-1)和(0.17±0.07)L·kg~(-1);Cmax分别为(268.2±115.7)ng·mL~(-1)和(162.2±53.0)ng·mL~(-1)。与对照组相比,实验组大鼠的AUC0-24 h、AUC0-∞、Cmax显著增大(P0.05),V、CL显著减小(P0.05),其他参数差异无统计学意义(P0.05)。结论:CYP2C9抑制剂(胺碘酮)对艾瑞昔布在大鼠体内的药动学产生影响。
[Abstract]:Objective: to investigate the effect of CYP2C9 inhibitor amiodarone on pharmacokinetics of irixib in rats. Methods: 40 healthy male SD rats were randomly divided into 2 groups. The experimental group was perfused with amiodarone for 7 days and the control group was given intragastric administration of Amiodarone. On the 8th day, 20 mg 路kg ~ (-1) 路L ~ (-1) of eroxib was perfused into gastric juice. The plasma concentration of eroxib was determined by LC-MS / MS method and the time curve was fitted by DAS 2.1.1 software and the pharmacokinetic parameters were calculated by SPSS 13.0 software. Results: the main pharmacokinetic parameters of the experimental group and the control group were as follows: 1 814.8 卤693.4)ng 路h mL-1 and 1 125.1 卤887.1)ng h mLLL-1) and 1 331.3 卤592.6)ng h mLL-1) and 1 331.3 卤592.6)ng h mLL-1 respectively. The main pharmacokinetic parameters of the experimental group and the control group were 1 814.8 卤4. 5 h and 7. 7 卤3. 8 h ~ 0. 6 h and 1. 46 卤0. 60 h ~ (-1) L ~ (-1) and 0. 02 卤0. 01 卤0. 01 h ~ (-1) L ~ (-1) and 0. 11 卤0. 05 L ~ (-1) ~ (-1) and 0. 11 卤0. 05 L ~ (-1) L ~ (-1) and 0. 011 卤0. 05 L ~ (-1) 路kg ~ (-1) C ~ (-1), respectively, of the experimental group and the control group, respectively. The pharmacokinetic parameters of the experimental group and the control group were 1 814.8 卤0. 6 h and 1. 46 卤0. 60 h, respectively. The results showed that the pharmacokinetic parameters of the experimental group and the control group were 0. 814.8 卤0. 01 887.1)ng 路h ~ (-1) and 0. 02 卤0. 01 887.1)ng h ~ (-1) respectively. They were 268.2 卤115.7)ng mL-1) and 162.2 卤53.0)ng mLL-1 respectively. Compared with the control group, there were no significant differences between the control group and the control group. AUC 0- 鈭，

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