阿维拉霉素自微乳制剂的研制及质量评价

发布时间：2018-06-28 04:49

本文选题：阿维拉霉素 + 自微乳化　；参考：《中国药学杂志》2017年20期

【摘要】：目的采用星点设计-效应面法优化阿维拉霉素自微乳化给药系统(SMEDDS),并进行质量评定。方法测定阿维拉霉素在各辅料中的溶解度,通过三相配伍实验筛选自微乳化基质;以微乳粒径、Zeta电位和分散系数(PDI)作为效应值,应用Design Expert进行处方优化,并对阿维拉霉素自微乳制剂进行稳定性、释放度及抑菌活性考察。结果通过星点效应面优化获得阿维拉霉素自微乳的处方:丙二醇月桂酸酯(36.67%)、聚氧乙烯氢化蓖麻油(42.83%)、二乙二醇乙醚(20.50%),载药量为2%。将自微乳浓缩液加水乳化后粒径为(28.34±0.06)nm,Zeta电位为(-1.98±0.24)mV,PDI为(0.15±0.005),并具有较好的体外抑菌活性。结论成功制备了阿维拉霉素SMEDDS,质量稳定,可显著改善阿维拉霉素的溶出度,有望提高阿维拉霉素动物体内口服生物利用度。
[Abstract]:Objective to optimize the self-emulsifying drug delivery system (SMEDs) of Avila mycin by star design-effect surface method and evaluate its quality. Methods the solubility of Avila in various excipients was determined, the self-emulsified matrix was selected by three-phase compatibility experiment, and the formulation was optimized by using the particle size, Zeta potential and dispersion coefficient of microemulsion as effect values. The stability, release and bacteriostatic activity of Avila-mycin self-emulsion were investigated. Results the formulation of Avila mycin self-microemulsion was obtained by star effect surface optimization: propanediol lauric acid ester (36.67%), polyoxyethylene hydrogenated castor oil (42.83%), diethylene glycol ether (20.50%). The particle size of self-microemulsion concentrate was (28.34 卤0.06) nm Zeta potential (-1.98 卤0.24) MV, PDI was (0.15 卤0.005), and it had better bacteriostatic activity in vitro. Conclusion the Avila mycin SMEDDSs were prepared successfully, and the quality was stable, the dissolution of Avila was improved significantly, and the bioavailability of Avila mycin was expected to be increased in vivo.
【作者单位】：浙江工商大学食品与生物工程学院;
【基金】：浙江省新苗人才计划资助项目(2014R408085)
【分类号】：R943

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