β-七叶皂苷钠在脑缺血再灌注大鼠体内药代动力学的研究  

Pharmacokinetics of sodium β-aescinate induced by ischemia-reperfusion in cerebral damage rats

作　　者：胡霞敏[1] 曾繁典[2] 

机构地区：[1]武汉科技大学医学院药理教研室 [2]华中科技大学同济医学院基础医学院药理系

出　　处：《中国临床药理学与治疗学》2005年第7期828-831,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:研究β-七叶皂苷钠在脑缺血再灌注大鼠体内的药代动力学规律。方法:应用酶联免疫吸附分析(ELISA,enzyme-linked immunosorbent assay)检测方法,测定正常大鼠及脑缺血大鼠经静脉注射β-七叶皂苷钠5 mg.kg-1后β-七叶皂苷钠的血药浓度,并对其药物代谢动力学参数进行研究。结果:脑缺血再灌注及正常大鼠静脉注射β-七叶皂苷钠5mg.kg-1后,其药代动力学模型符合二室模型。正常大鼠在静脉注射β-七叶皂苷钠后,血药浓度迅速下降,大约20 min后,其血浆药物浓度已下降50%,T1/2α=0.343 h,T1/2β=23.325 h。约2 h后,血浆药物浓度下降速率减慢。而脑缺血再灌注大鼠脑缺血30 min后,静脉注射β-七叶皂苷钠后,其体内药物代谢规律与正常大鼠不同,药物的代谢速率减慢,且在3 h出现一个较低的血药浓度峰,随后血浓下降。结论:β-七叶皂苷钠在脑缺血再灌注大鼠体内的消除较正常大鼠慢,在体内停留的时间较长。提示β-七叶皂苷钠在临床的对症治疗时应考虑其药代动力学的特点。AIM： To investigate the pharmacokinetics of sodium β-aescinate in cerebral damage rats induced by ischemia-reperfusion by the developed method of ELISA （ enzyme-linked immunosorbent assay ）. METHODS： After iv injection of sodium β-aescinate （ 5 mg· kg^-1 ）, the plasma concentration was determined. The pharmacokinetic parameters were accessed by the DAS. RESULTS： The profile of the plasma concentration-time was fitted with two-compartment model either in normal or in cerebral ischemia-reperfusion rats. In normal rats, T1/2α =0. 343 h, and T1/2β = 23. 325 h. In cerebral ischemiareperfusion, T1/2α = 0. 854 h, and T1/2β = 34.283 h. CONCLUSION： The clearance of sodium β-aescinate in cerebral ischemia-reperfusion rats is obviously slower than that in normal rats. The phannacokinetics of sodium β-aeseinate is necessary to consider under the pathologic condition when it is used in treatment of patients of cerebral ischemic disease.

关 键 词：Β-七叶皂苷钠 药代动力学 酶联免疫吸附分析 脑缺血 

分 类 号：R965.1[医药卫生—药理学]