氧氟沙星掩味微囊的制备及优化筛选

发布时间：2019-05-17 01:17

【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。
[Abstract]:In order to shield the bad taste of drugs, ofloxacin mask microcapsules were prepared by liquid drying with polyacrylic resin IV as capsule material. Taking the entrapment efficiency and drug loading as the index, the prescription process was screened by investigating the effects of solvent, capsule, emulsifier and antisticker on the microcapsules. The ofloxacin mask microcapsules were prepared by the best process. The drug loading was 57.4% and the entrapment efficiency was 48.6%. The release of the microcapsule in simulated oral environment (pH 7. 0) was very slow, and the release rate of 60min was only 2.1% of the total drug content, and the drug release rate increased significantly with the increase of acidity of the release medium. In addition, the release of ofloxacin showed sustained release in the range of gastric acid acidity (pH 1.0 鈮，

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