星点设计-效应面法优化缓释微丸型片剂中填充辅料颗粒处方  

Optimization of Filling Particles with Three Excipients in Sustained-release Pellets-type Tablets by CCD-RSM

作　　者：刘岐[1] 姜立群[1] 郑春丽[1] 朱家壁[1] 刘建平[1] 

机构地区：[1]中国药科大学药物制剂研究所,江苏南京210009

出　　处：《中国医药工业杂志》2013年第12期1240-1244,共5页Chinese Journal of Pharmaceuticals

基　　金：江苏省普通高校研究生科研创新计划(CXLX12_0313)

摘　　要：采用挤出-滚圆法和流化床包衣法,以Eudragit?NE30D为包衣材料制备单硝酸异山梨酯缓释微丸,然后与填充辅料颗粒混合后压制微丸型片剂。利用星点设计-效应面法对填充辅料颗粒中3种辅料(微晶纤维素PH 200、KG-802和预胶化淀粉PC-10)的含量进行优化并对预测结果进行验证。优化后颗粒中PH 200与KG-802比例为1.01,含PC-10 23%,具有良好的可压性与成型性,可在压缩过程中有效地保护微丸衣膜不被破坏。相似因子法比较结果表明微丸压片前后的释药行为相似,扫描电镜观察可见压片前后微丸形态未发生明显变化。The isosorbide mononitrate sustained-release pellets were prepared by extrusion-spheronization and fluid-bed coating method with Eudragit？ NE30D as coating material. Then these pellets were mixed with filling particles containing microcrystalline cellulose （MCC） PH 200, MCC KG-802 and pregelatinized starch PC-10 to prepare pelletstype tablets. The ratios of three excipients in filling particles were optimized by central composite design-response surface methodology （CCD-RSM） and the results were validated. The optimal particles with the ratio of MCC PH 200 to MCC KG-802 of 1.01 and PC-10 content of 23% had good compressibility and formability so that they could effectively protect the multi-unit coating pellets. The release behaviors and microstructures of the pellets prior to and after compression were not significantly changed according to the results of similarity factor method and scanning electron microscope observation.

关 键 词：单硝酸异山梨酯 缓释微丸 缓释微丸型片剂 填充辅料颗粒 星点设计-效应面法 优化 

分 类 号：R944.9[医药卫生—药剂学]