氧氟沙星掩味微囊的制备及优化筛选
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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 encapsulation 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 technology of oflxacin microcapsules is simple and maneuverable.
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 encapsulation 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 technology of oflxacin microcapsules is simple and maneuverable.
引文
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[2]雷连成,陈伟,韩文瑜,等.氧氟沙星脂质体的制备及其抑菌试验的观察[J].中国兽药杂志,2002(5):32-33.
[3]鲍光明,梅天笑,袁厚群,等.淀粉支载氧氟沙星前药的合成及其体外释放研究[J].江西农业大学学报,2014(2):413-417.
[4]刘锦光,许岸高.氧氟沙星的临床安全使用[J].临床荟萃,2001(5):237.
[5]余春芳,肖秀兰,田建平,等.左氧氟沙星的毒副反应及其防范[J].中国当代医药,2010(14):13-15.
[6]MARYER I,NAGY E.Evaluation of post-antibiotic effects of antipseudomonal antibiotics using an automated system[J].APMIS,2000,108(4):261-266.
[7]陆伟根,陈亭亭.药物制剂掩味技术研究进展[J].中成药,2008(1):113-116.
[8]GUO B L,GAO Q Y.Preparation and properties of a pH/temperature-responsive carboxymethyl chitosan/poly(N-isopropylacrylamide)semi-IPN hydrogel for oral delivery of drugs[J].Carbohydr Res,2007,342(16):2416-2422.
[9]APS J K,MARTENS L C.Review:The physiology of saliva and transfer of drugs into saliva[J].Forensic Sci Int,2005,150(2/3):119-131.
[10]裴志强,尹莉芳,周建平,等.氧氟沙星缓释微丸的研制[J].中国医院药学杂志,2008(7):543-546.