克拉霉素生物黏附微球的体外释药及黏附性研究  

In vitro drug release profiles and mucoadhesive property of bioadhesive microspheres of clarithromycin

作　　者：孙明辉[1] 陈莉[1] 斯陆勤[2] 张伟[2] 

机构地区：[1]华中科技大学同济医学院附属同济医院药学部,湖北武汉430030 [2]华中科技大学医学院药学院,湖北武汉430030

出　　处：《中国医院药学杂志》2009年第14期1183-1186,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研制具有较好生物黏附性能和药物缓释效果的克拉霉素(Cla)-乙基纤维素(EC)-卡波姆(Cb)微球。方法:使用乳化-溶剂挥发法制备克拉霉素生物黏附微球(Cla-EC-Cb),以高效液相色谱法测定Cla-EC-Cb微球中克拉霉素的含量;以体外释药速率评价EC与Cb不同配比、不同EC黏度对微球缓释效果的影响;以大鼠体内胃黏膜表面滞留程度,考察EC与Cb不同配比、不同EC黏度对微球生物黏附能力的影响。结果:黏附材料Cb的加入有助于提高微球的载药量;EC(20cp)与Cb配比为2∶1的微球体外药物释放度明显高于同EC黏度其他比例组和EC组;EC与Cb配比为4∶1时,EC(10cp)组体外释放参数明显高于EC(20cp)与EC(45cp)组;不同比例、不同EC黏度的Cla-EC-Cb微球在大鼠胃黏膜的滞留率均明显高于Cla-EC微球,Cla-EC(20cp)-Cb微球的胃黏膜滞留率随着Cb比例的提高有增大的趋势,但差异无显著性。结论:处方配比为EC(10cp)-Cb为4∶1,粒径为450～1 000μm的Cla-EC-Cb微球具有较好的体外药物缓释效果和胃黏膜黏附特性。OBJECTIVE To prepare bioadhesive microspheres of clarithromycin （Cla） with prolonging resident time in the stomach and sustaining drug release. METHODS The microspheres were prepared using emulsification/evaporation method. The bioadhesion was evaluated via counting the number of mierospheres retaining at the surface of gastric mueosa. In vitro drug release was also studied. The factors influencing bioadhesive property and drug release, such as ethyl cellulose（EC）/carbopol 934P（Ch） ratio, viscosity of EC were investigated. RESULTS The addition of Cb to microspheres can improve the Cla content. While the EC（20 cp）/Cb ratio was 2：1, the drug release rate of microspheres was significantly different from EC micropheres and mieropheres with other high ratio of EC（20 cp）/Cb. When the EC/Cb ratio was 4： 1, the drug release rate of Cla-EC （10 cp）-Cb was faster than EC（20 cp） and EC（45 cp）. The retention percentage of EC/Cb micropheres with various ratio and different EC viscosity were significantly higher than EC micropheres. Moreover, with the increase of Cb content, the retention percentage of microspheres increased, but it had no significant difference（P〉0. 05）. CONCLUSION The Cla-EC Cb microspheres have a sound mucoadhesive and sustained drug release property when the ratio of EC（10 cp） and Cb was 4：1.

关 键 词：克拉霉素 生物黏附微球 乙基纤维素 卡波姆934P 

分 类 号：R944.9[医药卫生—药剂学]