水飞蓟宾纳米粒的制备及其理化性质研究  

Preparation and physicochemical characterization of silibinin nanoparticles

作　　者：胡霓霓[1] 谭群友[2] 魏农农[3] 杨帆[2] 张景勍[1] 

机构地区：[1]重庆医科大学生物化学与分子药理学重点实验室、药物高校工程研究中心,重庆400016 [2]第三军医大学大坪医院野战外科研究所,重庆400042 [3]国家食品药品监督管理局国家新药评审中心,北京400010

出　　处：《中草药》2009年第9期1384-1387,共4页Chinese Traditional and Herbal Drugs

基　　金：重庆市首批高等学校优秀人才资助计划项目;重庆医科大学创新基金项目

摘　　要：目的制备水飞蓟宾纳米粒并对其进行质量评价。方法采用乳化-蒸发-固化法制备水飞蓟宾纳米粒,以包封率、多分散指数、载药量等为评价指标优化制备工艺。考察体外释药规律,考察3～5℃、15～25℃、37℃(相对湿度为75%)条件下纳米粒的稳定性。结果以硬脂酸和表面活性剂为载体材料,优化工艺制备的水飞蓟宾纳米粒包封率为96.88%,多分散指数为0.168,载药量为7.55%。差示量热分析确证形成了纳米粒,水飞蓟宾以无定形态分散在纳米粒内。纳米粒体外释放缓慢,可用Higuchi方程拟合。纳米粒静置观察具有良好的稳定性。结论采用乳化-蒸发-固化法可制备得到水飞蓟宾纳米粒,工艺简便,粒径和分散度小,包封率和载药量高,体外释药缓慢,稳定性好。Objective To prepare silibinin nanoparticles and investigate their properties. Methods Silibinin nanoparticles were prepared by the emulsion evaporation-solidification method at low temperature. The entrapment efficiency, polydispersity index, drug loading were set as evaluation indexes to optimize the preparation processing. Drug release from nanopartieles and the stability of nanopartieles were investigated at the different temperatures of 3--5 ℃, 15--25 ℃, and 37℃, respectively, and with the relative humidity of 75%. Results Taking stearie acid and surfaetant Brij 78 as carrier, the entrapment efficiency of silibinin nanoparticles prepared by optimized technology was up to 96.88%, the dispersion index of the smallest was 0. 168, and durg loading was 7.55%. Analysis by using differential scanning calorimetry showed that silibinin was dispersed in the nanoparticles at an amorphous state. The in vitro silibinin released slowly from nanoparticles and the release profile fitted well into Higuehi equation. Nanoaparticles were stable under storage conditions. Conclusion Silibinin nanoparticles could be prepared by the emulsion evaporationsolidification method, with the advantages of techniques simple, diameter and dispersion small, entrapment efficiency and drug loading high, in vitro release slow, and stability good.

关 键 词：水飞蓟宾纳米粒 差示量热扫描仪 稳定性 

分 类 号：R286.02[医药卫生—中药学]