柴胡皂苷经不同给药途径血药和脑药动力学的比较研究  

Comparison of different administration routes of saikosaponin in plasma pharmacokinetics and brain pharmacokinetics

作　　者：戴雅洁 陈晓兰[1] 唐红艳[1] 邓显仪 谢浪 DAI Ya-jie CHEN Xiao-lan TANG Hong-yan DENG Xian-yi XIE Lang(School of Pharmarcy , Guiyang College of Traditional Chinese Medicine, Guiyang 550002, Chin)

机构地区：[1]贵阳中医学院药学院,贵州贵阳550002

出　　处：《中国中药杂志》2017年第14期2767-2772,共6页China Journal of Chinese Materia Medica

基　　金：贵州省科学技术厅中药现代化攻关项目(黔科合ZY字[2013]3017);苗族医药协同创新中心(黔教合协同创新字[2015]05);中药民族药药剂学专业学位研究生工作站(黔教研合YJSZ字[2013]05)

摘　　要：通过比较柴胡皂苷经不同途径给药后血药及脑药动力学,评价柴胡皂苷治疗癫痫的最佳给药途径。柴胡皂苷经不同途径给予小鼠后于不同时间点取血和全脑,以乙腈-甲醇(9∶1)沉淀血浆蛋白质,采用UPLC-MS/MS测定SSa在小鼠血浆和脑组织中的浓度,用Kinetica程序软件计算药代动力学参数和生物利用度,并计算脑靶向系数(Re)和药物脑靶向指数(DTI)。鼻腔给药后脑药Re为142.17%,DTI为3.06,要显著高于注射组。灌胃组DTI为1.25。柴胡皂苷鼻腔给药后脑靶向性要高于注射组和灌胃给药组,显示出鼻腔给药"引药入脑"的优势。To evaluate the optimum administration routes of saikosaponin in the treatment of epilepsy by comparing the plasma phar- macokinetics and the brain pharmacokinetics after different administration routes of saikosaponin. After receiving saikosaponin in differ- ent administration routes, the mice were sacrificed to collect the blood and brain tissues. The acetonitrile and methanol （9：1 ） were used to precipitate the plasma protein. The concentration of the SSa in mice plasma and brain was determined by UPLC-MS/MS, and the pharmacokinetic parameters, bioavailability, the brain targeting coefficient （Re） and the brain drug targeting index （DTI） were calculated with Kinetica software. The relative brain Re was 142. 17% by intranasal administration, with DTI of 3.06, significantly higher than those by the injections ; in addition, the brain DTI was 1.25 by garage administration. The brain drug targeting of saikosa- ponin by intranasal administration was higher than that by injection and gavage administration, indicating the advantages of the in- tranasal administration on medicine absorption into the brain.

关 键 词：柴胡皂苷 药代动力学 脑靶向系数 药物靶向指数 

分 类 号：R285.5[医药卫生—中药学]