發(fā)布時間：2019-04-26 18:57

【摘要】：目的研究健康受試者口服0.125mg和0.25mg普拉克索片的藥動學(xué)過程,并評價該制劑的安全性,為注冊治療不寧腿綜合征(restless leg syndrome,RLS)提供藥動學(xué)依據(jù)。方法采用隨機、開放、雙向交叉試驗設(shè)計,12名健康受試者(男女各半)分兩個階段分別進行單次口服普拉克索片0.125mg和0.25mg的藥動學(xué)試驗,兩次給藥間隔13天,每次給藥前及給藥后采集血樣,采用液相色譜-串聯(lián)質(zhì)譜聯(lián)用法(LC-MS/MS)測定健康受試者給藥后血漿中普拉克索的濃度。采用WinNonlin(R)6.0版軟件計算普拉克索片的藥動學(xué)參數(shù)(AUC0-t、AUC0-∞ρmaxtmaxt1/2CL/F等)。整個試驗過程進行全面安全性評估。結(jié)果單次口服普拉克索片0.125mg和0.25mg后,ρmax分別為(237±83)μg/L和(493±155)μg/L,tmax分別為(1.71±1.64)h和(1.21±1.01)h,t1/2分別為(6.12±2.21)h和(7.27±2.17)h,AUC0-∞分別為(1 791±765)μg·h·L-1和(4 419±1 932)μg·h·L-1,不同性別的藥動學(xué)參數(shù)差異無統(tǒng)計學(xué)意義(P0.05).試驗過程無嚴(yán)重不良事件發(fā)生。結(jié)論單次口服0.125mg或0.25mg普拉克索吸收很快,吸收程度隨劑量增加而增加,藥動學(xué)過程不受性別影響.本研究制劑安全性較好,可按試驗劑量給藥治療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，

本文編號：2466315