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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(r2>0.99)。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。
OBJECTIVE: To study the pharmacokinetics of ropinirole in plasma and striatum by liquid chromatography-mass spectrometry (LC-MS / MS) method in rat plasma and striatum. Methods: Plasma and striatal tissue homogenates were analyzed by LC-MS / MS. Ropiviril (0.27 mg · kg-1) was injected into the tail vein of rats. Plasma was collected before administration and at different time points after administration. Striatal samples of homogenate of the striatum were prepared, and the concentrations were determined. Plasma pharmacokinetics Parameters, examine the distribution of striatum. RESULTS: Ropinirole in plasma and tissue homogenates showed a good linearity (r2> 0.99) over a concentration range of 1 to 100 ng · mL -1. The half-life of ropinirole in plasma was t1 (0.49 ± 0.30) h, and the area under the drug-time curve was (29.48 ± 11.49) ng · h · m L-1 in striatum The half-life (t1 / 2) was (0.29 ± 0.04) h, and the area under the drug-time curve was (75.66 ± 16.06) ng · h · g-1. The concentration decreased with the decrease of plasma concentration. Conclusion: This method has good repeatability, high sensitivity and specificity. Ropinirole rapidly penetrates the blood-brain barrier and is enriched in the striatum, and is a potent dopamine D2 receptor agonist.