吡嘧司特钾片在中国健康人体内的药动学研究

发布时间：2018-04-27 17:15

  本文选题：吡嘧司特钾片 + 药动学　； 参考：《中国新药杂志》2015年02期

【摘要】：目的:建立人血浆中吡嘧司特钾浓度的LC-MS/MS测定法,研究吡嘧司特钾片在中国健康人体内的药动学。方法:21例中国男性健康受试者单剂量空腹口服10 mg吡嘧司特钾片,0~24 h间隔采集肘静脉血,血浆样品采用0.1%盐酸化乙腈沉淀蛋白处理,LC-MS/MS法测定吡嘧司特钾血药浓度,DAS 2.0软件计算药动学参数。结果:建立的LC-MS/MS法测定吡嘧司特钾血浆浓度在2.0~400 ng·m L-1范围内线性关系良好,最低定量限为2.0 ng·m L-1,经方法验证符合生物样品测定要求。测得受试者单剂量口服10 mg吡嘧司特钾片后的主要药动学参数:Cmax为(1 007±135)ng·m L-1,Tmax为(1.8±0.6)h,t1/2为(4.1±0.8)h,AUC0~24为(5 851±992)ng·h·m L-1,AUC0~∞为(5 986±1 068)ng·h·m L-1,CL为(1.8±0.3)L·h-1,Vd为(10.5±1.5)L。结论:建立的LC-MS/MS测定法专属、灵敏,满足吡嘧司特钾片药动学研究的要求。
[Abstract]:Objective: to establish a LC-MS/MS determination method for the concentration of pyridin potassium in human plasma and to study the pharmacokinetics of Pemirolast potassium tablets in Chinese healthy volunteers. Methods: 21 Chinese male healthy subjects were treated with a single dose of 10 mg Pemirolast potassium tablets, 0~24 h interval and 0.1% hydrochloric acetonitrile precipitated protein, and the plasma samples were treated with 0.1% hydrochloric acetonitrile precipitating protein. LC-MS/MS method was used to determine the concentration of ppipyridine potassium and DAS 2 software to calculate the pharmacokinetic parameters. Results: the LC-MS/MS method was used to determine the plasma concentration of pyridin potassium in the 2.0~400 ng. M L-1, and the minimum quantitative limit was 2 ng. M L-1. The method was proved to be in accordance with the requirements of biological samples. The single dose of 10 of the subjects was 10. Mg Pemirolast potassium tablets's main pharmacokinetic parameters: Cmax (1007 + 135) ng / m L-1, Tmax (1.8 + 0.6) h, t1/2 (4.1 + 0.8) h, AUC0~24 for (5851 + 992) ng H. Requirements for pharmacokinetic studies.

【作者单位】： 中国药科大学药物分析教研室;中国医学科学院皮肤病医院;
【分类号】：R969.1
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本文编号：1811599