非布司他片在健康人体内的药动学研究

发布时间：2018-02-28 09:10

本文关键词： 高效液相色谱-串联质谱非布司他血药浓度单剂量给药试验药动学　出处：《药物分析杂志》2015年07期 　论文类型：期刊论文

【摘要】：目的:建立血浆中非布司他的HPLC-MS/MS定量分析方法,对非布司他片的人体药动学进行研究,为该药临床合理使用提供参考。方法:对12名中国健康志愿者(男、女各半)依次进行40 mg与80 mg 2个剂量单次口服给药,以及80 mg剂量每天1次连续7 d的多次口服给药。采用HPLC-MS/MS法测定血药浓度,Win Non Lin 6.3软件计算药动学参数,IBM SPSS Statistics 19软件对结果进行统计分析。结果:单次口服非布司他片40、80 mg和多次口服80 mg后,血浆中非布司他的AUC0→t分别为(7 320±2 198)、(15 121±4 328)、(14 376±4 089)ng·h·m L-1,Cmax分别为(2 078±533.2)、(4 094±1 282)、(3 841±1071)ng·m L-1,Tmax分别为(1.69±0.91)、(1.54±0.74)、(1.58±1.06)h,t1/2分别为(6.09±1.72)、(7.07±2.37)、(6.19±1.94)h。结论:单剂量口服给药试验表明,在40到80 mg剂量范围内,口服非布司他在健康中国人体内的药动学过程呈现剂量依赖性;多剂量口服给药试验表明,非布司他在健康中国人体内几乎无蓄积现象;非布司他在不同性别中国人群体内的药动学过程无明显差异。
[Abstract]:Objective: to establish a HPLC-MS/MS quantitative analysis method for plasma nonbustrast tablets, and to study the pharmacokinetics of the tablets in order to provide a reference for the rational clinical use of the drug. Methods: 12 healthy volunteers (male, male) were enrolled in this study. Two doses of 40 mg and 80 mg were given orally. The pharmacokinetic parameters were calculated by HPLC-MS/MS Non Lin 6.3 software and the results were statistically analyzed by IBM SPSS Statistics 19 software. After 40mg of statin and 80 mg of oral administration, Plasma AUC0 of Nabostatin. 鈫扵 = 7 320 卤2 198 1 1 Tmax = 15 121 卤4 3288H / L = 14 376 卤4 089 ng 路h 路ml -1 C max = 2 078 卤53 3.2n 4 094 卤1 282 + 1 841 卤10 71 ng 路m -1 Tmax = 1.69 卤0. 911 卤0. 74ht1.58 卤1. 06 Hz / L = 6.09 卤1. 22O 7 卤2 377.07 卤2 377.07 卤2 377.07 卤2 377.19 卤1 94h. conclusion: in the single oral dose range of 40 to 80 mg / L, the dose was 1. 69 卤0. 01 卤0. 74ht1.58 卤1. 06 卤1. 06 Ht1 / 2, and 6.09 卤1. 722 卤2. 377.07 卤2. 377 卤1. 94 / h, respectively. Conclusion: in the single oral dose range of 40 to 80 mg, the Tmax is 1. 69 卤0. 001 卤0. 74 htl. The pharmacokinetic process of oral fentinast in healthy Chinese human body was dose-dependent, and the multiple dose oral administration test showed that there was almost no accumulation phenomenon in healthy Chinese human body. There was no significant difference in pharmacokinetic processes between different genders in Chinese population.
【作者单位】：上海奉贤区中心医院;第四军医大学西京医院药剂科;成都蓉药集团四川长威制药有限公司;
【分类号】：R969.1

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