高萍,张啸,邹梅娟,韩佳容,安跃,程刚
GAO Ping,ZHANG Xiao,ZOU Mei-juan,HAN Jia-rong,AN Yue,CHENG Gang(School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的采用O/O型乳化溶剂挥发法制备瑞舒伐他汀钙肠溶缓释微球,评价各因素对微球性质的影响。方法以微球的粒径、收率、包封率和释放度作为微球的质量评价指标,研究Eudragit类型、乙基纤维素黏度、两种囊材的质量比、搅拌速度、理论载药量和乳化剂用量对微球性质的影响。结果 Eudragit L100-55制得的微球在酸中突释严重,Eudragit L100能很好地抑制药物在酸中的释放;乙基纤维素(20 cp)制得的微球能在pH值6.8的磷酸盐缓冲液中持续释药10 h;Eudragit L100和乙基纤维素(20 cp)的质量比为70∶30时能得到理想的释放曲线;搅拌速度为600 r.min-1、理论载药量为10%和乳化剂Span 80的质量占液体石蜡质量的2%时能得到较好的微球。结论联合应用pH敏感型材料Eudragit L100和缓释材料乙基纤维素,应用乳化溶剂挥发法可以制备瑞舒伐他汀钙肠溶缓释微球。
Objective To prepare enteric,extended-release rosuvastatin calcium microspheres by the oil-in-oil(O/O)emulsification solvent evaporation method and evaluate factors influencing characteristics of the microspheres. Methods Particle size,yield,entrapment efficiency and in vitro release were used as criteria to evaluate the effects of type of Eudragit and ethyl cellulose,the ratio of the two wall materials,stirring speed,theoretical drug loading and emulsifier concentration on the characteristics of the microspheres. Results The microspheres prepared with Eudragit L100-55 showed burst release in the acidic medium while Eudragit L100 exhibited good control of drug release.Ethyl cellulose(20 cp)achieved a constant release of rosuvastatin calcium in pH 6.8 phosphate buffer within 10 hours.The ideal release profile could be obtained when Eudragit L100-55 and ethyl cellulose(20 cp)are in the ratio of 70∶30.Microspheres with good physical properties could be prepared at the stirring speed of 600 r·min-1,10% theoretical drug loading and 2% Span 80. Conclusions Combining Eudragit L100 and ethyl cellulose(20 cp),microspheres which continuously release rosuvastatin calcium in intestine can be achieved by emulsification solvent evaporation method.

关键词(KeyWords)： 微球;Eudragit L100;乙基纤维素;瑞舒伐他汀钙;乳化溶剂挥发法
microspheres;Eudragit L100;ethyl cellulose;rosuvastatin calcium;emulsification solvent evaporation method

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 高萍,张啸,邹梅娟,韩佳容,安跃,程刚
GAO Ping,ZHANG Xiao,ZOU Mei-juan,HAN Jia-rong,AN Yue,CHENG Gang(School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2012.09.011

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