甲磺酸帕珠沙星片健康人体多次给药药动学研究
Pharmacokinetics of multiple dose pazufloxacin mesylate tablets in Chinese healthy subjects
赵彩芸 1吕媛 1魏敏吉 1张朴 1侯芳 1贺锐锐 1夏亚红 1田继红 1刘燕1
作者信息
- 1. 北京大学第一医院临床药理研究所,北京100034
- 折叠
摘要
目的 研究甲磺酸帕珠沙星片在中国健康受试者多次给药的药动学.方法 12名健康受试者男女各半,口服甲磺酸帕珠沙星片,每天2次,每次500mg,连续用药至第7天,收集第1天和第7天血、尿样本,用LC-MS/MS方法测定帕珠沙星的血、尿浓度.结果 受试者多次口服甲磺酸帕珠沙星第1天和第7天主要药动学参数分别是,Cmax为(9.79±2.18)、(9.37±1.58)mg/L;AUC0-t为(25.44±3.86)、(25.23±5.06) h·mg/L;t1/2为(1.81±0.28)、(1.78±0.23)h;Tmax为(0.72±o.27)、(0.73±0.31)h;多剂给药后第1天和第7天原型药物尿中累积排泄百分率分别为(71.93±23.20)、(87.41±16.10)％.第1天与第7天主要药动学参数比较差异均无统计学意义.结论 多次连续给药后第1天和第7天主要药动学参数结果相似,药物在体内无蓄积,口服给药耐受性良好.
Abstract
Objective To evaluate the pharmacokinetics of multiple dose of pazufloxacin mesylate tablets in Chinese healthy subjects.Methods Twelve subjects (6 male and 6 female) were administrated pazufloxacin mesylate tablets 500mg,twice daily for 7 days.The blood and urine samples were collected at day 1 and day 7 respectively.The concentrations of pazufloxacin in plasma and urine were determinated by LC-MS/MS method.Results The main pharmacokinetics parameters at day 1 and day 7 were as follows:Cmax were (9.79±2.18) and (9.37±1.58) mg/ L;AUC0-t were (25.44±3.86) and (25.23±5.06)h·mg/L;t1/2 were (1.81±0.28) and (1.78 ±0.23)h;Tmax were (0.72±0.27) and (0.73±0.31)h;respectively.Urinary recovery rates were (71.93±23.20) and (87.41±16.10)％ at day 1 and day 7,respectively.Conclusion The results showed that the main pharmacokinetics parameters of pazufloxacin mesylate at day 1 and day 7 were similar.There was no accumulation in human body.All subjects were well tolerated.
关键词
甲磺酸帕珠沙星片/药动学/多次给药/LC-MS/MSKey words
Pazufloxacin mesylate tablets/Multiple-dose/Pharmacokinetic/LC-MS/MS引用本文复制引用
出版年
2015
NETL
NSTL
维普
万方数据