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由流化床包衣机制备的聚合物薄膜包衣微粒的不完善导致的突发药物释放。

A burst drug release caused by imperfection of polymeric film-coated microparticles prepared by a fluidized bed coater.

作者信息

Sriamornsak P, Casallas-Hernández G L, Manchun S, Kumpugdee-Vollrath M

机构信息

Department of Pharmaceutical Technology, Faculty of Mathematics-Physics-Chemistry, Beuth Hochschule für Technik Berlin-University of Applied Sciences, Berlin, Germany.

出版信息

Pharmazie. 2011 Aug;66(8):576-83.

PMID:21901979
Abstract

The aim of this study was to investigate the drug release from microparticles coated with various polymeric films. Ibuprofen-loaded microparticles with diameter of 250 and 300 microm were prepared by a fluidized bed granulator. Five polymers were used as coating materials, i.e., ethylene vinyl acetate, ethyl cellulose, ethyl cellulose aqueous dispersion, polyethacrylate or Eudragit NE 30D, and carnauba wax. The coating was performed with a fluidized bed coater. Afterwards the coated microparticles were characterized in terms of particle size, morphology, and drug content. The drug dissolution was also investigated in pH 7.4 phosphate buffer. In our attempts for production of extended release ibuprofen microparticles coated with polymeric films, it was shown that the coating process had a significant effect on drug release. The undesired burst release of ibuprofen was observed in all film-coated microparticulate formulations, resulting from the imperfection of coating films.

摘要

本研究的目的是研究药物从涂覆有各种聚合物薄膜的微粒中的释放情况。通过流化床制粒机制备了直径为250和300微米的载布洛芬微粒。使用了五种聚合物作为包衣材料,即乙烯-醋酸乙烯共聚物、乙基纤维素、乙基纤维素水分散体、聚丙烯酸酯或Eudragit NE 30D以及巴西棕榈蜡。采用流化床包衣机进行包衣。之后,对包衣微粒的粒径、形态和药物含量进行了表征。还在pH 7.4的磷酸盐缓冲液中研究了药物溶出度。在我们制备聚合物薄膜包衣的布洛芬缓释微粒的过程中,结果表明包衣过程对药物释放有显著影响。在所有薄膜包衣微粒制剂中均观察到布洛芬意外的突释现象,这是由包衣膜的不完善所致。

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