液相色谱-质谱联用法研究大鼠血浆及纹状体中罗匹尼罗药动学

发布时间：2018-03-05 19:37

  本文选题：罗匹尼罗　切入点：液相色谱-质谱联用　出处：《中国新药杂志》2015年12期 　论文类型：期刊论文

【摘要】：目的:通过大鼠血浆及纹状体组织匀浆中罗匹尼罗的液相色谱-质谱联用(LC-MS/MS)检测方法,研究其在血浆和纹状体的药动学特征。方法:通过LC-MS/MS检测分析血浆和纹状体组织匀浆样品。大鼠尾静脉注射罗匹尼罗(0.27 mg·kg-1),分别于给药前和给药后不同时间点采集血浆、制备纹状体组织匀浆样品,测定浓度,计算血浆药动学参数,考察纹状体分布特征。结果:血浆和组织匀浆中罗匹尼罗在1~100ng·m L-1浓度范围内线性关系良好(r20.99)。罗匹尼罗在大鼠血浆中消除半衰期t1/2为(0.49±0.30)h,药-时曲线下面积AUC0~∞为(29.48±11.49)ng·h·m L-1,纹状体中消除半衰期t1/2为(0.29±0.04)h,药-时曲线下面积AUC0~∞为(75.66±16.06)ng·h·g-1,其浓度随血药浓度下降而下降。结论:该方法重复性好、灵敏度高、特异性强。罗匹尼罗可迅速透过血脑屏障并在纹状体富集,是一种高效多巴胺D2受体激动剂。
[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 卤0.30 min 路m ~ (-1) and the area under the drug time curve was 29.48 卤11.49 ng 路m ~ (-1) 路m ~ (-1). T ~ (1 / 2) in striatum was 0.29 卤0.04 h, AUC _ 0 ~ 鈭，

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