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载有特布他林的多孔 PCL/Eudragit RS 微胶囊的特性及释放行为。

Characterization and release behaviors of porous PCL/Eudragit RS microcapsules containing tulobuterol.

机构信息

Department of Chemistry, Inha University, Nam-gu, 253, Incheon 402-751, South Korea.

出版信息

Colloids Surf B Biointerfaces. 2010 Apr 1;76(2):404-9. doi: 10.1016/j.colsurfb.2009.11.015. Epub 2009 Nov 26.

Abstract

In this work, porous poly(epsilon-caprolactone) (PCL)/Eudragit RS 100 (ERS-100) microcapsules containing tulobuterol base as a model drug were prepared by a solvent evaporation method and the effect of the quaternary ammonium groups of ERS-100 on the release behaviors of the microcapsules was investigated. The microcapsules prepared with PCL alone showed a stable and smooth surface, whereas porous microcapsules were formed with the addition of ERS-100. Drug loading and encapsulation efficiency of the microcapsules were slightly decreased with an increase of ERS-100 content, resulting from an increase in the porosity of the microcapsules. In an acidic release medium, PCL microcapsules showed slow drug release, whereas PCL/ERS-100 microcapsules showed a faster release rate with an increasing ERS-100 content. These behaviors are likely due to an increase in the diffusion rate of the drugs stemming from an increased hydration of the microcapsules, which results from the interaction between the carboxyl group of the release medium and the quaternary ammonium group of ERS-100.

摘要

在这项工作中,通过溶剂蒸发法制备了含有作为模型药物的特布他林碱的多孔聚己内酯(PCL)/Eudragit RS 100(ERS-100)微胶囊,并研究了 ERS-100 的季铵基团对微胶囊释放行为的影响。单独使用 PCL 制备的微胶囊表面稳定光滑,而加入 ERS-100 则形成多孔微胶囊。随着 ERS-100 含量的增加,微胶囊的载药量和包封效率略有下降,这是由于微胶囊的孔隙率增加所致。在酸性释放介质中,PCL 微胶囊表现出缓慢的药物释放,而随着 ERS-100 含量的增加,PCL/ERS-100 微胶囊表现出更快的释放速率。这些行为可能是由于药物的扩散速率增加,这是由于释放介质的羧基与 ERS-100 的季铵基团之间的相互作用导致微胶囊的水合作用增加所致。

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