本文選題：羅匹尼羅　切入點(diǎn)：液相色譜-質(zhì)譜聯(lián)用　出處：《中國新藥雜志》2015年12期 　論文類型：期刊論文

【摘要】：目的:通過大鼠血漿及紋狀體組織勻漿中羅匹尼羅的液相色譜-質(zhì)譜聯(lián)用(LC-MS/MS)檢測方法,研究其在血漿和紋狀體的藥動學(xué)特征。方法:通過LC-MS/MS檢測分析血漿和紋狀體組織勻漿樣品。大鼠尾靜脈注射羅匹尼羅(0.27 mg·kg-1),分別于給藥前和給藥后不同時(shí)間點(diǎn)采集血漿、制備紋狀體組織勻漿樣品,測定濃度,計(jì)算血漿藥動學(xué)參數(shù),考察紋狀體分布特征。結(jié)果:血漿和組織勻漿中羅匹尼羅在1~100ng·m L-1濃度范圍內(nèi)線性關(guān)系良好(r20.99)。羅匹尼羅在大鼠血漿中消除半衰期t1/2為(0.49±0.30)h,藥-時(shí)曲線下面積AUC0~∞為(29.48±11.49)ng·h·m L-1,紋狀體中消除半衰期t1/2為(0.29±0.04)h,藥-時(shí)曲線下面積AUC0~∞為(75.66±16.06)ng·h·g-1,其濃度隨血藥濃度下降而下降。結(jié)論:該方法重復(fù)性好、靈敏度高、特異性強(qiáng)。羅匹尼羅可迅速透過血腦屏障并在紋狀體富集,是一種高效多巴胺D2受體激動劑。
[Abstract]:Objective: to detect ropigniro in rat plasma and striatum tissue homogenate by liquid chromatography-mass spectrometry (LC-MS / MS). Methods: the plasma and striatum homogenate samples were analyzed by LC-MS/MS. The plasma samples were collected at different time points before and after administration of ropionidone 0.27 mg 路kg -1 by tail vein injection in rats. The samples of striatum homogenate were prepared, the concentration was determined, and the plasma pharmacokinetic parameters were calculated. Results: in plasma and tissue homogenate, there was a good linear relationship between ropigniro and tissue homogenate in the concentration range of 100 ng 路mL ~ (-1). The elimination half-life t _ (1 / 2) was 0.49 鹵0.30 min 路m ~ (-1) and the area under the drug time curve was 29.48 鹵11.49 ng 路m ~ (-1) 路m ~ (-1). T ~ (1 / 2) in striatum was 0.29 鹵0.04 h, AUC _ 0 ~ 鈭，

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