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马钱子总碱脂质液晶纳米粒的制备和体外评价研究
引用本文:金晨,陈家乐,徐玲霞,管咏梅,刘丽丽,朱卫丰,吴璐,张凌,陈丽华.马钱子总碱脂质液晶纳米粒的制备和体外评价研究[J].中草药,2018,49(22):5305-5312.
作者姓名:金晨  陈家乐  徐玲霞  管咏梅  刘丽丽  朱卫丰  吴璐  张凌  陈丽华
作者单位:江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004,江西中医药大学 现代中药制剂教育部重点实验室, 江西 南昌 330004
基金项目:国家自然科学基金资助项目(81460606);江西省卫生计生委中医药科研计划(2014A059)
摘    要:目的制备一种马钱子总碱(TASS)的新剂型,以期提高TASS的载药量和经皮渗透性能。方法采用热溶剂-高压均质法制备马钱子总碱脂质液晶纳米粒(TASS-LLCN),采用超滤离心法测定包封率,以包封率为指标采用星点设计-响应面法优化TASS-LLCN的处方,并对优化后制备的TASS-LLCN的基本性能进行评价。同时,采用Franz扩散池法比较TASS-LLCN凝胶和TASS普通凝胶的体外经皮渗透特性,初步考察TASS-LLCN凝胶的经皮渗透行为。结果 TASS-LLCN的最佳制备处方为甘油单油酸酯(GMO)1 403.19 mg、GMO-泊洛沙姆407(GMO-F127)质量比为7.25∶1、载药量为9.48%,预测包封率为64.01%;制剂质量评价显示制得的纳米粒平均粒径为186 nm左右,Zeta电位为-33.1 mV,pH值6.83,稳定性良好;透皮实验显示,TASS-LLCN的24 h累积透过量和渗透速率均大于TASS普通凝胶,具有显著性差异(P0.05),可以促进有效成分的吸收;TASS-LLCN的皮肤滞留量大于TASS普通凝胶,说明药物在皮下形成储库,有利于药物的持续释放。结论 TASS-LLCN可显著提高TASS的载药量和经皮渗透性能,是一种潜在的具有缓释作用的新型药物。

关 键 词:脂质液晶纳米粒  马钱子总碱  包封率  星点设计-响应面法  Franz扩散池法  马钱子碱  士的宁
收稿时间:2018/6/21 0:00:00

Study on preparation and evaluation in vitro of TASS-LLCN
JIN Chen,CHEN Jia-le,XU Ling-xi,GUAN Yong-mei,LIU Li-li,ZHU Wei-feng,WU Lu,ZHANG Ling and CHEN Li-hua.Study on preparation and evaluation in vitro of TASS-LLCN[J].Chinese Traditional and Herbal Drugs,2018,49(22):5305-5312.
Authors:JIN Chen  CHEN Jia-le  XU Ling-xi  GUAN Yong-mei  LIU Li-li  ZHU Wei-feng  WU Lu  ZHANG Ling and CHEN Li-hua
Institution:Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China,Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China and Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM), Ministry of Education, Jiangxi University of TCM, Nanchang 330004, China
Abstract:
Keywords:lipid liquid crystalline nanoparticl (LLCN)  total alkaloids from seed of Strychni Semen  encapsulation efficiency  response surface methodology with central composite design  Franz diffuser method  brucine  strychnine
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