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目的:考察艾瑞昔布对静脉注射咪达唑仑在大鼠体内药动学的影响,探讨艾瑞昔布对CYP3A酶是否有诱导或者抑制作用。方法:将大鼠随机分为实验组和对照组,每组20只,实验组每天灌胃艾瑞昔布灌胃液20 mg·kg-1,对照组每天灌胃等量纯化水,bid,连续7 d。第8天,每只大鼠尾静脉注射咪达唑仑10 mg·kg-1,于给药后不同时间点眼内眦取血,高效液相色谱法测定血浆药物浓度,绘制药时曲线,DAS 2.1.1软件拟合药动学参数,使用SPSS 13.1软件对2组的药动学参数进行统计学分析。结果:实验组与对照组主要药动学参数:AUC0-24h分别为(3.42±0.91)mg·h·L-1和(3.83±0.84)mg·h·L-1;AUC0-∞分别为(3.34±0.88)mg·h·L-1和(3.77±0.86)mg·h·L-1;t1/2分别为(0.37±0.07)h和(0.35±0.08)h;Cmax分别为(11.85±4.45)mg·L-1和(12.36±3.48)mg·L-1;V分别为(1.62±0.45)L·kg-1和(1.37±0.39)L·kg-1;CL分别为(3.14±0.85)L·h-1·kg-1和(2.74±0.66)L·h-1·kg-1。2组药动学参数之间的差异无统计学意义(P>0.05)。结论:合用艾瑞昔布前后咪达唑仑体内药动学参数无显著性变化,艾瑞昔布对大鼠静脉注射咪达唑仑的药动学无影响。
Objective: To investigate the effect of irisoxib on the pharmacokinetics of intravenous midazolam in rats and to explore whether or not eriocetin induces or inhibits the CYP3A enzyme. Methods: The rats were randomly divided into experimental group and control group, with 20 rats in each group. The experimental group was given intragastric administration of irisoxab in 20 mg · kg-1 daily, while the control group was given equal amount of purified water, bid, continuous 7 d. On the 8th day, each rat was injected midazolam 10 mg · kg-1 into the caudal vein to take blood at different time points after administration. Plasma drug concentrations were determined by HPLC. 2.1.1 Software fitting pharmacokinetic parameters, the use of SPSS 13.1 software on the two groups of pharmacokinetic parameters for statistical analysis. Results: The main pharmacokinetic parameters of AUC0-24h were (3.42 ± 0.91) mg · h · L-1 and (3.83 ± 0.84) mg · h · L-1, respectively. The AUC0- 3.34 ± 0.88) mg · h · L-1 and (3.77 ± 0.86) mg · h · L-1, respectively; t 1/2 was (0.37 ± 0.07) h and (0.35 ± 0.08) h respectively; Cmax was (11.85 ± 4.45) mg · L-1 and (12.36 ± 3.48) mg · L-1, respectively, and 1.62 ± 0.45 L · kg-1 and 1.37 ± 0.39 L · kg- 0.85) L · h-1 · kg-1 and (2.74 ± 0.66) L · h-1 · kg-1.2 groups, there was no significant difference between the two groups (P> 0.05). CONCLUSION: There was no significant change in pharmacokinetics of midazolam before and after the combination of erectile function and irrecoxib in pharmacokinetics of intravenous midazolam in rats.