阿昔洛韦生物粘附微球的动物胃粘膜表面粘附能力和体外缓释效果  

The bioadhesive property of aciclovir microspheres on animals gastric mucin and its in vitro effect of sustained drug release

作　　者：陆伟跃[1] 潘俊[1] 刘敏[1] 

机构地区：[1]上海医科大学药学研究所药物靶向制剂研究室,上海200032

出　　处：《中国药学杂志》2000年第5期313-317,共5页Chinese Pharmaceutical Journal

摘　　要：目的 :研制一种具有较好生物粘附能力和药物缓释效果的阿昔洛韦 (Acv) 卡波姆 (Cb) 乙基纤维素 (Ec)微球。方法 :通过油包水乳剂的溶媒蒸发法制备Acv Cb Ec微球 ;以动物体内外胃粘膜表面滞留程度 ,考察Cb与Ec不同配比、Acv含量、微球粒径对Acv Cb Ec微球生物粘附能力的影响 ;以体外释药速率评价Cb与Ec不同配比、Acv含量、微球粒径和介质 pH对Acv Cb Ec微球缓释效果影响。结果 :Cb配比增加 ,Acv Cb Ec微球生物粘附能力增强 ,药物缓释效果降低 ,表现为负相关性 ;Acv含量增加 ,Acv Cb Ec微球生物粘附能力和药物缓释效果均降低 ,但Acv含量≤ 2 0 %时 ,缓释效果基本接近 ;粒径增大 ,Acv Cb Ec微球生物粘附能力有所减小 ,但在 5 0 0～ 12 0 0 μm时 ,药物缓释效果显著提高 (12h) ,而粘附性变化不明显 ;Acv Cb Ec微球在酸性介质中的释药速率明显快于中性或近中性介质。结论 :载药量≤ 2 0 % ,粒径为 5 0 0～ 12 0 0 μm ,Cb与Ec配比为1∶9的Acv Cb Ec微球在胃粘膜表面具有良好粘附特性 ,且药物缓释可达 12h ,近中性pH条件下的缓释效果更佳。OBJECTIVE:To prepare aciclovir (Acv) carbomer(Cb) ethylcellulose(Ec)microspheres with good bioadhesion and sustained drug release.METHODS:The microspheres were prepared using a w/o emulsion solvent evaporation technique.The bioadhesion was evaluated via counting the microspheres retaining at the surface of gastric mucin. In vitro drug release was also studied.The factors influencing the bioadhesion and drug release,such as Cb/Ec ratios,Acv content,particle size as well as the pH of media were studied,respeitively.RESULTS:While Cb/Ec ratio being increased,the bioadhesion of Acv Cb Ec microspheres increased,but teh drug release rate slowed down,which showed a negative correlation.The more the Acv content was,the worse the bioadhesion was and the faster Acv released.When the Acv content was ≤20%,the drug release rate slightly changed.The bioadhesion of the microspheres was also reduced when the particle size was increased.However when the particle sizes were between 500～1200 μm,the drug release rate was significantly retarded (12 h).In acedic media,the drug release rate was faster than that in neutral media.CONCLUSION:The Acv Cb Ec microspheres had a good bioadhesion and sustained drug release when Acv content was ≤20%,the particle size was between 500～1200 μm and the Cb/Ec ratio was 1∶9.The drug released even slower in neutral media.

关 键 词：阿昔洛韦 生物粘附 药物缓释 ACV-Cb-Ec微球 

分 类 号：R978.7[医药卫生—药品]