摘要
目的:优化罗红霉素微球的制备工艺。方法:以乙基纤维素为囊材,采用乳化-溶剂扩散法制备罗红霉素微球,以药物与囊材用量比(A)、囊材的浓度(B)、水相与油相的比例(C)为因素,包封率为指标设计正交试验优选制备工艺,并对所得微球的外观、粒径分布、载药量、包封率、体外释放度及苦味进行研究。结果:优化后的最佳工艺:A为1∶1,B为30mg.mL-1,C为4∶1。所得的微球外观圆整,平均粒径(75.0~90.0)μm,且分布均匀,载药量约45%~46%,包封率可达90%以上,可持续释药13h以上,多数试验者服药后感觉不苦。结论:优化工艺后所制罗红霉素微球具有明显掩味和缓释效果。
OBJECTIVE: To optimize the preparation technology of roxithromycin microspheres. METHODS: The microspheres of roxithromycin were prepared by the emulsion- solvent diffusion method with ethylcellulose used as capsule wall material. The preparation technology of microspheres was optimized by orthogonal experiment taking encapsulation efficiency as index with the ratio of roxithromycin to ethylcellulose (A), the concentration of ethylcellulose (B) and the ratio of water phase to oil phase (C) as factors. The appearance, particle diameter, drug- loading amount, encapsulation efficiency, in vitro release and bitter smell were studied. RESULTS: The optimal preparation conditions were as follows: A was 1 : 1, B was 30 ug · mL^-1 and C was 4 : 1. The microspheres obtained were round and well- distributed with mean diameter of 75.0-90.0 um, drug-loading amount of 45%-46%, encapsulation efficiency of over 90% and sustained release for over 13 hours. No bitter taste of the roxithromycin- ethylcellulose microspheres was felt by the majority of subjects. CONCLUSION: The roxithromycin microspheres made by optimization technology was bitter- masked and sustained release.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第16期1230-1232,共3页
China Pharmacy
基金
河北大学引进人才资助项目(y2005064)
关键词
罗红霉素
乙基纤维素
微球
制备工艺
正交试验
Roxithromycin
Ethyl cellulose
Microspheres
Preparation technology
Orthogonal experiment