【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(dòng)學(xué)過(guò)程,并評(píng)價(jià)該制劑的安全性,為注冊(cè)治療不寧腿綜合征(restless leg syndrome,RLS)提供藥動(dòng)學(xué)依據(jù)。方法采用隨機(jī)、開放、雙向交叉試驗(yàn)設(shè)計(jì),12名健康受試者(男女各半)分兩個(gè)階段分別進(jìn)行單次口服普拉克索片0.125mg和0.25mg的藥動(dòng)學(xué)試驗(yàn),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(cè)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(jì)算普拉克索片的藥動(dòng)學(xué)參數(shù)(AUC0-t、AUC0-∞ρmaxtmaxt1/2CL/F等)。整個(gè)試驗(yàn)過(guò)程進(jìn)行全面安全性評(píng)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(dòng)學(xué)參數(shù)差異無(wú)統(tǒng)計(jì)學(xué)意義(P0.05).試驗(yàn)過(guò)程無(wú)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(dòng)學(xué)過(guò)程不受性別影響.本研究制劑安全性較好,可按試驗(yàn)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，

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