羟乙基芦丁在大鼠体内的药物动力学  

Pharmacokinetics tissue distribution and excretion of venoruton in rats

作　　者：袁成[1] 曹晓芝[1] 王景祥[1] 

机构地区：[1]济南军区总医院

出　　处：《中国医院药学杂志》1999年第2期67-69,共3页Chinese Journal of Hospital Pharmacy

摘　　要：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。OBJECTIVE:To understand distribution,metabolizm and excretion of venoruton in rats.METHODS:The content of venoruton in tissue and body fluid was determined with an RP HPLC method(all components in venoruton were looked upon as one componet) after 20,40 and 50 mg·kg -1 intravenous injection dose.RESULTS:The drug was found to conform to an one compartment model with t 1/2 = 3.01 ～ 5.33 h, V o= 2.40 ～ 4.16 L, AUC = 36.26 ～ 92.38 mg·h·L -1 and Cl = 0.55 , 0.57 and 0.54 L·h -1 ,and to distribut with a high concentrations to most tissues except fat. The protein binding rate in plasma was about 60%. The results of total excretion 11.7% of the dose within 24 h in urine, bile and stool showed that the drug was trans formed to supersession product to clear out. The detection limit was 1 μg·L -1 .CONCLUSIONS: There was a wide tissue distribution for venoruton in rat, that was metabolized.

关 键 词：羟乙基芦丁 药物动力学 高效液相色谱法 

分 类 号：R972[医药卫生—药品] R969.1[医药卫生—药学]