氧氟沙星掩味微囊的制备及优化筛选  

Optimized screening method for preparation of taste-masked ofloxacin microcapsules

作　　者：鲍光明[1] 刘宝生[1] 王小莺[1] 罗军荣[1] 邹欣[1] 袁厚群[2] 张路捷 胡弯弯[1] 陈书鹏[1] 

机构地区：[1]江西农业大学动物科学技术学院,江西南昌330045 [2]江西农业大学理学院,江西南昌330045

出　　处：《中国兽医学报》2017年第1期92-96,共5页Chinese Journal of Veterinary Science

基　　金：国家自然科学基金资助项目(31560712;21461011);江西省自然科学基金资助项目(20151BAB204014;20142BAB214017;20132BAB213002;20144BDH80006);教育部高校博士点专项基金资助项目(20113603120006)

摘　　要：为了屏蔽药物的不良味道,本试验以聚丙烯酸树脂IV为囊材,采用液中干燥法制备了氧氟沙星掩味微囊。试验以包封率及载药量为指标,通过考察溶剂、囊材、乳化剂、抗黏剂的用量对微囊的影响来筛选处方工艺。应用最佳工艺制备的氧氟沙星掩味微囊,载药量为57.4%,包封率为48.6%。该微囊在模拟口腔环境(pH值为7.0)介质中释放极其缓慢,60min仅释放总药量的2.1%;随着释放介质的酸度提高,药物的释放速率显著加快;除此之外,在胃酸酸度(pH值为1.0~3.0)范围内,氧氟沙星的释放还呈现缓释特征,可持续近10h。体外试验显示,采用液中干燥法制备得的氧氟沙星微囊,既可掩味又能实现持续释药,而且制备工艺简便,具有很好的应用前景。In order to cover the unpleasant taste of oflxacin, taste-masked oflxacin microcapsules were prepared by in-liquid drying method using acrylic resin IV. The various factors of procedures （such as solvent, capsules shell material, emulsifier and antiadherent） were optimized based on en- capsulation efficiency and drug loadings. The best procedure for the preparation of taste-masked oflxacin microcapsules was decided,in which the concentration of oflxacin reached 57.4% while the encapsulation rate was 48.6%. The result of drug release in vitro showed that the drug was hardly any release from the oflxacin microcapsules in neutral medium. The release rate of oflxacin was accelerated accompanied by the acidity of release medium. The release of drug could be kept for about 10 hours in simulated gastric fluid. The oflxacin microcapsules with taste-masked and sustained-release have high encapsulation efficiency and drug loadings. The preparation technolo- gy of oflxacin microcapsules is simple and maneuverable.

关 键 词：氧氟沙星 微囊 掩味 缓释 

分 类 号：S859.5[农业科学—临床兽医学]