摘要
目的以聚乳酸-羟基乙酸共聚物(PLGA)为载体材料,制备伊潘立酮长效缓释微球,并考察微球的体外释放度。方法采用O/W型乳化-溶剂挥发法制备伊潘立酮PLGA微球,运用正交实验设计优化处方组成和制备工艺,并对微球的外观形态、粒径、包封率、载药量和体外释放等理化性质进行了考察。结果优化得到的最佳处方工艺为油相PLGA的浓度为80 g/L,油相-水相体积比为1∶30,聚乙烯醇(PVA)浓度为1%,乳化剪切速度为10 000 r/min。以优化处方制备的伊潘立酮PLGA微球为圆球形,粒径为(24.56±0.46)μm,包封率为(81.94±1.48)%,载药量为(7.50±0.13)%。药物体外释放30 d累计释放度达86.33%。结论采用O/W型乳化-溶剂挥发法制备的伊潘立酮PLGA微球的包封率和载药量高,具有较好的缓释效果。
Objective To prepare iloperidone sustained-release microspheres using polylactic-co- glycolic acid （PLGA） as sustained-release carrier and to study their release in vitro. Methods Iloperidone- containing PLGA microspheres were prepared by O/W emulsion-solvent evaporation method. The formulation and the preparation conditions were optimized by orthogonal tests. The morphology was evaluated by light microscopy. The particle size distribution was measured by Mastersizer 2000 （Malvern）. The encapsulation efficiency and the drug load were assessed. The in vitro release characteristics of the microspheres were also assayed. Results The optimized preparation conditions were as follows： PLGA concentration 80 g/L, the volume ratio of oil to water 1 ： 30, polyvinyl alcohol concentration 1%, and speed of mechanical stirring 10 000 r/min. The results showed that iloperidone-containing PLGA microspheres were spherical in shape, with mean diameter of （24.56 ±0. 46 ） μm, average encapsulation efficiency of （ 81. 94 ±1.48 ） %, drug load of （ 7. 50 ±0. 13 ）% , and cumulative release of iloperidone from microspheres of 86. 33% for 30 d. Conclusion Iloperidone-containing PLGA microspheres are prepared successfully by O/W emulsion-solvent evaporation method with high encapsulation efficiency, high drug load and good sustained release characteristics.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2014年第3期274-277,共4页
Journal of Third Military Medical University
基金
重庆医药工业研究院有限责任公司
重庆市化学制药工程技术研究中心提供科研经费资助和指导
