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观察维脑路通注射液中总羟乙基芦丁在大鼠体内的药物动力学。方法:大鼠静脉注射羟乙基芦丁20,40和50mg·kg-1后,用反相高效液相色谱多组分峰共积分测定法,测定在不同时间各组织和体液中总羟乙基芦丁的含量以及蛋白结合率。结果:羟乙基芦丁在血浆中的药物动力学符合一室开放模型,有关参数除Cl外,血浆蛋白结合率、Co、T1/2(3.01~5.33h)、Vc(2.40~4.16L)、AUC(36.26~92.38mg·h·L-1)均具有剂量依赖性,药物血浆蛋白结合率的62%,药物在体内各组织分布广泛且含量相差不大,但脂肪组织中最低,给药8h后各组织中含量明显下降,在粪、尿和胆汁中原形药物总排出量占给药量(40mg·kg-1)的11.7%。实验中建立的高效液相色谱法适于体内羟乙基芦丁的测定,检测下限为1μg·L-1,线性范围0.1~15mg·L-1。结论:羟乙基芦丁在大鼠体内各组织分布广泛,主要经代谢途径被清除。
To observe the pharmacokinetics of total hydroxyethyl rutin in Weitailuetong injection in rats. Methods: After intravenous injection of hydroxyethyl rutin 20,40 and 50 mg · kg-1 in rats, the content of total hydroxyl groups in tissues and body fluids at different time was determined by RP-HPLC- Ethyl rutin content and protein binding rate. Results: The pharmacokinetics of hydroxyethyl rutin in plasma conformed to the one-compartment open model. The plasma protein binding rate, Co, T1 / 2 (3.01-5.33h), Vc (2) 40 ~ 4.16L), AUC (36.26 ~ 92.38mg · h · L-1) were dose-dependent, drug plasma protein binding rate of 62%, the drug in the body of various tissues are widely distributed and the content is not significantly different , But the lowest in adipose tissue. The contents of all kinds of tissues decreased obviously after 8h administration, and the total output of prototype drugs in dung, urine and bile accounted for 11.7% of the dosage (40mg · kg-1). The established HPLC was suitable for the determination of hydroxyethyl rutin in vivo. The detection limit was 1μg · L-1 and the linear range was 0.1-15mg · L-1. Conclusion: Hydroxyethyl rutin is widely distributed in various tissues of rats and is mainly eliminated by metabolic pathway.