通脉活血灵胶囊中大黄酚在大鼠血浆中的浓度及药代动力学研究.DOCVIP

临床医学论文-通脉活血灵胶囊中大黄酚在大鼠血浆中的浓度及药代动力学研究 ????????????????????? 作者：李兰芳， 张勤增， 解丽君， 杨凤旭 【关键词】? 通脉活血灵胶囊;,,大黄酚;,,血药浓度;,,HPLC 　　摘要：目的：观察大鼠口服通脉活血灵胶囊后，其效能成分大黄酚在大鼠体内的药动学过程。方法：大鼠单次灌服通脉活血灵胶囊，用反相高效液相法测定不同时间的血药浓度，采用DAS2.0药动学软件拟合处理该药的药动学参数。结果：通脉活血灵胶囊中大黄酚在大鼠体内的药动学参数：T1/2α，T1/2β，AUC(o-∞)，K10，K12，K21，Tmax，Cmax分别为：1.054h，4.197h，2479.555 mg/L，0.077 1/h，0.222 1/h，0.407 1/h，0.5h，230.58 mg/L。结论：单次灌服通脉活血灵胶囊后，大黄酚在大鼠体内的药动学过程符合开放型二室模型，吸收快，消除慢，同服用单味大黄后大黄酚在家兔体内的药动学过程有一定的差异。 　　关键词：? 通脉活血灵胶囊;? 大黄酚;? 血药浓度;? HPLC 　　Determination of chrysophanol from Tongmaihuoxueling Capsules in rat’s plasma and study on its pharmacokinetics? 　　Abstract: Objective: To study the pharmacokinetics of chrysophanol in rats after ig administration of Tongmaihuoxueling capsules(TC). Methods: The concentrations of chrysophanol in plasma were determined by RP-HPLC method after single ig administration of TC. The parameters of pharmacokinetics were computed by DAS 2.0 program.? Results: The pharmacokinetic parameters of chrysophanol from TC in rats were as follows: T1/2α，T1/2β，AUC(o-∞)，K10，K12，K21，Tmax，Cmax; Their value were respectively 1.054h，4.197h，2479.555 mg/L，0.077 1/h，0.222 1/h，0.407 1/h，0.5 h，230.58 mg/L.Conclusion: After single ig administration of TC in rats, the concentration-time curves of chrysophanol in plasma fitted a two-compartment open model. The pharmacokinetic of chrysophanol from TC shows a rapid absorption and slow elimination process in rats, which is different from the pharmacokinetic of chrysophanol after ig administration of rhubarb in rabbits. 　　Key words:?? Tongmaihuoxueling capsules;? Chrysophanol;? Plasma concentration;? HPLC??? 　　 　　通脉活血灵胶囊由丹参、大黄、槐米、制首乌、川芎、鸡内金等组成，具有活血通脉、益气健脾之功效，现代研究表明具有降低血液粘度、预防心脑血管血栓形成、改善供血的作用。主要用于高粘血症、动脉粥样硬化、脑梗塞等病的治疗。大黄为主药之一，具有泻下、降脂、抑制血小板聚集等多种功能［1］。阐明其主要成分大黄酚在机体内药代动力学行为，有助于指导该复方的临床应用以及探讨大黄酚在全面发挥药理作用的地位和机制。本研究应用反相高效液相色谱法测定了大鼠单次口服通脉活血灵胶囊后动物血浆中大黄酚的浓度，并应用药动学统计软件拟合了大黄酚在大鼠体内的药动学过程。为进一步开展该复方的药动学-药效学研究奠定了基础。 　　1?? 材料 　　1.1? 仪器：Aglient1100高效液相色谱仪，安捷伦公司； METTLER AE240型电子天平，梅特勒仪器上海有限公司；TG