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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Microspheres with pH modulated release: Design and characterization of formulation variables for colonic delivery
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Microspheres with pH modulated release: Design and characterization of formulation variables for colonic delivery

机译:pH调节释放的微球:用于结肠递送的配方变量的设计和表征

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The aim of this study was to design and develop microspheres of indomethacin with pH and transit time dependent release properties for achieving targeted delivery to the colon. Microspheres containing varying proportions of ethyl cellulose and Eudragit (L100 or S100) either alone or in combination were prepared using an oil-in-oil emulsion-based solvent evaporation technique. System comprising of acetone (internal phase) and liquid paraffin (external phase) in the ratio of 1:1 and 1:9 yielded microspheres with good physical properties (spherical and discrete), high drug loading (70-80%) and entrapment efficiency (70-85%). The lag time in the initial release depended on the proportion of pH-sensitive polymer Eudragit, while the duration of indomethacin release from microspheres was found to be directly proportional to proportion of the total polymer. Thus, a pH- and time-modulated sigmoidal release pattern could be observed in optimized formulations with less than 10% drug release in 4-6 h followed by controlled release extending up to 14-16 h.
机译:这项研究的目的是设计和开发吲哚美辛微球,其pH和转运时间依赖于释放特性,以实现向结肠的靶向递送。使用基于油包油乳液的溶剂蒸发技术制备单独或组合包含不同比例的乙基纤维素和Eudragit(L100或S100)的微球。由比例为1:1和1:9的丙酮(内相)和液体石蜡(外相)组成的系统产生的微球具有良好的物理性质(球形和离散),高载药量(70-80%)和包封效率(70-85%)。初始释放的滞后时间取决于pH敏感聚合物Eudragit的比例,而吲哚美辛从微球中释放的持续时间则与总聚合物的比例成正比。因此,在优化的制剂中可以观察到pH和时间调节的乙状结肠释放模式,其中在4-6小时内药物释放少于10%,随后是控制释放直至14-16小时。

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