伊曲康唑Pluronic P123聚合物胶束的制备工艺研究  

Preparation and Formulation of Itraconazole Loaded Pluronic P123 Polymeric Micelles

作　　者：关延彬[1] 左岚[1] 饶子超[1] 斯陆勤[1] 李高[1] 

机构地区：[1]华中科技大学同济医学院药学院,武汉430030

出　　处：《中国药学杂志》2011年第6期434-439,共6页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30873171)

摘　　要：目的制备Pluronic P123为载体的伊曲康唑胶束给药系统。方法采用薄膜水化法制备载药胶束,考察处方因素及工艺条件对载药共聚物胶束的包封率及载药量的影响,并采用三因素、五水平的星点设计-效应面法优化处方。动态光散射法测定胶束粒径,并对载药胶束的体外溶出度进行了测定,HPLC法测定胶束的载药量和包封率。结果制得的载药胶束包封率为60.23%,载药量为1.12%,粒径为30～40 nm。载药胶束在模拟的人工胃液和人工肠液中都可以快速溶出,但市售Sporan-oxTM胶囊的溶出行为却与溶出介质相关。结论本实验制备以Pluronic P123为载体的伊曲康唑胶束给药系统工艺简单可行,为其进一步研究奠定了基础。OBJECTIVE To prepare Pluronic P123 polymeric micelles system loaded with itraconazole（ITZ）. METHODS ITZ loaded Pluronic P123 micelles were prepared by thin-film hydration method. The main factors affecting the drug -loading coefficient and encapsulation ratio were studied by single factor analysis and central composite design. The mean particle size was determined by dynamic light scattering （DIS）. Dissolution in vitro of ITZ in mieelles were determined. The drug-loading coefficient and entrapment effi- ciency of ITZ in micelles were investigated by HPLC. RESULTS The encapsulation efficiency and drug-loading coefficient were 60. 23% and 1.12% ,respectively. The diameter was in the range of 30 -40 nm . Itraconazole in mieelles rapidly dissolved both in simulated gastric fluid （ pH 1.2） and simulated intestinal fluid （ pH 6. 8 ） whereas the SporanoxTM showed different dissolution patterns according to the dissolution media. CONCLUSION The formulation and preparation process were practical and simple for the preparation of ITZ loaded Pluronic P123 mieelles. It was valuable to be further studied.

关 键 词：伊曲康唑 Pluronie P123共聚物胶束 星点设计 效应面 

分 类 号：R944[医药卫生—药剂学]