正交试验法优化西咪替丁中空微球的处方工艺及微球体外释药模式研究  

Orthogonal experiments for optimizing the formulation and preparation conditions of cimetidine hollow microspheres and study on the release profile of microspheres in vitro

作　　者：朱澄云[1] 郑佳妮[1] 周名扬 佟立今[1] 阎心丽[3] 杨思广[4] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]南开大学化学院,天津300071 [3]沈阳药科大学医疗器械学院,辽宁沈阳110016 [4]吉林市食品药品检验所,吉林吉林132011

出　　处：《沈阳药科大学学报》2014年第9期669-672,共4页Journal of Shenyang Pharmaceutical University

摘　　要：目的优化西咪替丁中空微球的制备条件并对其释药模式进行研究。方法采用溶剂扩散-挥发法制备西咪替丁中空微球。以微球包封率、收率及漂浮率为指标,采用正交试验法优化处方工艺,最终得到分散性良好的微球。以优化处方制备的中空微球进行体外溶出实验,进行释放机理的探讨。结果采用正交试验法优化了西咪替丁中空微球的处方工艺,在最优处方下制得的微球外观圆整,微球的粒径较均匀,载药量与包封率分别为19.48%与65.37%,在人工胃液中12 h漂浮率可达99%。结论该方法制备工艺简单、重现性好,制得的中空微球在人工胃液中具有良好的漂浮及缓释特性,体外释药符合Higuchi模型。Objective To optimize the formulation and preparation conditions of cimetidine hollow microspheres by orthogonal test and to study the release profile of microspheres. Methods Cimetidine hollow microspheres were prepared by the solvent diffusion-evaporation method. Formulation and process factors including the encapsulation efficiency, yield and rate of floatage were fully investigated using orthogonal test to obtain microspheres with good dispersion. The dissolution experiments of the hollow microspheres prepared under the optimized conditions proceeded in vitro to analyze the mechanism of drug release behavior. Results The prepared microspheres were spherical and smooth in appearance. The particle size distribution was uni- form. The drug loading and encapsulation efficiency were 19.48% and 65.37%, respectively. More than 99% of the microspheres tended to float over simulated gastric fluid for 12 h. Conclusions This preparation method of microspheres is simple and reproducible. These microspheres show excellent floatability and con- tinuous release performance. The accumulative release profile in vitro can be described by the Higuchi equation.

关 键 词：正交试验 中空微球 溶剂扩散-挥发法 西咪替丁 

分 类 号：R94[医药卫生—药剂学]