改良溶剂挥发/萃取法制备曲尼司特聚乳酸微球及体外表征  

Study on Preparation and in vitro Characterization of Tranilast Poly(D,L-lactide) Microspheres by a Modified Solvent Evaporation/Extraction Method

作　　者：姚帮新[1] 邹烨[1] 阙俐[2] 吴伟[2] 

机构地区：[1]复旦大学附属中山医院药剂科,上海200032 [2]复旦大学药学院,上海200032

出　　处：《中国药学杂志》2006年第8期608-612,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30100204)

摘　　要：目的改良溶剂挥发/萃取法制备曲尼司特聚乳酸微球,并对其体外特性进行表征。方法O/W型溶剂挥发/萃取法制备曲尼司特聚乳酸微球,4%聚乙烯醇溶液为乳化剂,通过改变内相或外相溶剂,加快萃取速度,促进微球快速形成。对微球的粒径、表面形态、载药量、包封率、释放特性进行考察。结果内相中加入一定比例的极性溶剂可提高曲尼司特的包封率,微球粒径相应减小。外相中加入一定量有机溶剂进行萃取,并不能明显提高包封率,但微球粒径减小。优选条件制备的微球表面光滑圆整,药物具有一定的突释效应,7 d时释放约68%。结论经改良的溶剂挥发/萃取法可较好地用来制备曲尼司特聚乳酸微球,并能提高药物的包封率。OBJECTIVE To prepare tranilast poly（ D, L-lactide） microspheres by a modified solvent evaporation/extraction method and investigate in vitro properties.METHODS Tranilast microspheres were prepared by O/W type solvent evaporation/extraction method, with 4% polyvinyl alcohol solution as emulsifier. Organic solvent was added to inner and outer phase to accelerate solvent extraction and the formation of microspheres. In vitro characteristics, such as size and size distribution, morphology, drug loading, loading efficiency and drug release, were investigated. RESULTS Adding polar organic solvent in inner phase improved the loading efficiency of tranilast in microspheres, meanwhile reduce microsphere diameter greatly. Loading efficiency did not increase after adding organic solvent in outer phase, however reduced diameters. Microspheres prepared under optimum conditions were smooth and spherical. A burst release was observed and followed by sustained release, releasing 65 % of total tranilast after 7 days. CONCLUSION The modified solvent evaporation/extraction method can be used for the preparation of tranilast poly（ D, L-lactide） micraspheres with high drug loading efficiency.

关 键 词：微球 曲尼司特 聚乳酸 溶剂挥发/萃取法 

分 类 号：R943.4[医药卫生—药剂学]