灯盏花乙素大鼠口服给药的药动学与药效学研究  

Study on Pharmacokinetics and Pharmacodynamics of Scutellarin Administered by Orally Routes

作　　者：叶赏和[1] 石森林[2] 储利胜[2] 张晓东[2] 李昌煜[2] 沈伟[2] 葛卫红[2] 金玉婷[2] 

机构地区：[1]金华市人民医院,浙江金华321000 [2]浙江中医药大学药学院,浙江杭州310053

出　　处：《中华中医药学刊》2010年第7期1387-1389,F0003,共4页Chinese Archives of Traditional Chinese Medicine

基　　金：国家中医药管理局科研项目(06-07ZP24);浙江省教育厅重点项目(Z200805647);浙江省实验动物科技计划项目(2009F80016);杭州市科技局重点课题(200432358)

摘　　要：目的：以静脉给药为对照,研究灯盏花乙素口服给药在大鼠中的药代动力学及对大鼠实验性脑缺血的药效作用,探讨灯盏花乙素口服给药治疗脑梗死的可行性。方法：采用125I标记法测定SD大鼠尾静脉注射和灌胃0.4mg.kg-1灯盏花乙素后不同时间血浆中灯盏花乙素的浓度,3P87软件拟合房室模型,计算药动学参数;采用Longa线栓法制作SD大鼠局部脑缺血模型,脑缺血1h,再灌注24h,随机分为假手术组、模型组、灯盏花乙素口服给药与静脉给药组,每组6只,分别给予相应药物,观察各组对脑缺血大鼠神经功能、脑梗死面积的影响。结果：口服给药组Tmax、Cmax分别为42.70 min、0.28μg/mL,绝对生物利用度为30.54%。脑缺血1h,再灌注24h时模型组大鼠神经功能缺损严重,平均达4~5级;模型组梗死体积平均为21.82%,口服组给药组与静脉给药组分别为16.76%与14.01%,与模型组比较有显著性差异。结论：灯盏花乙素口服给药治疗脑梗死具有一定的可行性。Objective：To study the pharmacokinetics and protective effect on experimental cerebral ischemia of Scutellarin in rats by orally routes compare with intravenously routes,and to discuss the feasibility of taking Scutellarin orally.Method：Scutellarin concentrations of plasma samples were obtained after 0.4mg·kg-1 Scutellarin given to rats by intravenously and orally.They were determined by 125I marked method.The pharmacokinetic profiles and parameters were calculated by 3P87 software;The right side cerebral ischemia models,established by suture-occluded method of Longa,were treated with 1h in cerebral ischemia,24h in reperfusion.The rats were randomly and equally divided into 4 groups： sham operation group,model group,breviscapine oral and injection administration groups.There were 6 rats in every group.Each group was given corresponding drugs respectively.Observation on the influence on the nerve function and cerebral infarction area of ischemia rats of each group.Result：The main pharmacokinetic parameters of oral group,such as Tmax were 42.7 min,Cmax were 0.28μg/mL and the Absolute bioavailability were 30.54%.Moreover there were significant difference of bioavailability between the groups.Conclusion： It＇s feasible and meaningful to develop an orally dosage form of Scutellarin.

关 键 词：灯盏花乙素 口服给药 药动学 生物利用度 

分 类 号：R959.1[医药卫生—药学]