普拉克索片在健康人体的药动学研究及安全性评价
发布时间：2019-04-26 18:57
【摘要】：目的研究健康受试者口服0.125mg和0.25mg普拉克索片的药动学过程,并评价该制剂的安全性,为注册治疗不宁腿综合征(restless leg syndrome,RLS)提供药动学依据。方法采用随机、开放、双向交叉试验设计,12名健康受试者(男女各半)分两个阶段分别进行单次口服普拉克索片0.125mg和0.25mg的药动学试验,两次给药间隔13天,每次给药前及给药后采集血样,采用液相色谱-串联质谱联用法(LC-MS/MS)测定健康受试者给药后血浆中普拉克索的浓度。采用WinNonlin(R)6.0版软件计算普拉克索片的药动学参数(AUC0-t、AUC0-∞ρmaxtmaxt1/2CL/F等)。整个试验过程进行全面安全性评估。结果单次口服普拉克索片0.125mg和0.25mg后,ρmax分别为(237±83)μg/L和(493±155)μg/L,tmax分别为(1.71±1.64)h和(1.21±1.01)h,t1/2分别为(6.12±2.21)h和(7.27±2.17)h,AUC0-∞分别为(1 791±765)μg·h·L-1和(4 419±1 932)μg·h·L-1,不同性别的药动学参数差异无统计学意义(P0.05).试验过程无严重不良事件发生。结论单次口服0.125mg或0.25mg普拉克索吸收很快,吸收程度随剂量增加而增加,药动学过程不受性别影响.本研究制剂安全性较好,可按试验剂量给药治疗RLS。
[Abstract]:Aim to study the pharmacokinetic process of 0.125mg and 0.25mg Prac tablets orally in healthy subjects and to evaluate the safety of the preparation in order to provide the pharmacokinetic basis for registered treatment of restless leg syndrome (restless leg syndrome,RLS). Methods A randomized, open, two-way crossover trial was conducted in 12 healthy subjects (half male and half male) for a single oral administration of 0.125mg and 0.25mg at a intervals of 13 days. Blood samples were collected before and after each administration. The plasma concentration of Praxol in healthy subjects was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The pharmacokinetic parameters (AUC0-t,AUC0- 鈭，
本文编号：2466315
[Abstract]:Aim to study the pharmacokinetic process of 0.125mg and 0.25mg Prac tablets orally in healthy subjects and to evaluate the safety of the preparation in order to provide the pharmacokinetic basis for registered treatment of restless leg syndrome (restless leg syndrome,RLS). Methods A randomized, open, two-way crossover trial was conducted in 12 healthy subjects (half male and half male) for a single oral administration of 0.125mg and 0.25mg at a intervals of 13 days. Blood samples were collected before and after each administration. The plasma concentration of Praxol in healthy subjects was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The pharmacokinetic parameters (AUC0-t,AUC0- 鈭，
本文编号：2466315
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