Kawashima Y, Niwa T, Handa T, Takeuchi H, Iwamoto T, Itoh K
Gifu Pharmaceutical University, Japan.
J Pharm Sci. 1989 Jan;78(1):68-72. doi: 10.1002/jps.2600780118.
A novel quasi-emulsion solvent diffusion method to prepare the controlled-release microspheres of ibuprofen with acrylic polymers has been developed. An ethanol solution of ibuprofen and acrylic resin was poured into aqueous medium with stirring. The finely dispersed ethanolic droplet-like coacervates formed in aqueous medium were gradually solidified and transformed into microspheres during agitation. The size of microspheres was determined by the concentrations of drug and polymer and the agitation speed of the system. The flowability, the packability, and the compressibility of the resultant microspheres were much improved compared with the raw crystals of the drug. The drug release rate from the microspheres could be controlled by the type and the concentration of polymer formulated. A unique principle of the present method and the resultant microspheres, having a matrix- or sponge-like texture, can provide characteristic advantages compared with a conventional reservoir-type device drug, like a microcapsule.
已开发出一种新型的准乳液溶剂扩散法,用于制备含丙烯酸聚合物的布洛芬控释微球。将布洛芬和丙烯酸树脂的乙醇溶液在搅拌下倒入水介质中。在水介质中形成的精细分散的乙醇液滴状凝聚层在搅拌过程中逐渐固化并转化为微球。微球的大小由药物和聚合物的浓度以及体系的搅拌速度决定。与药物的原始晶体相比,所得微球的流动性、填充性和可压缩性有了很大提高。微球的药物释放速率可通过所配制聚合物的类型和浓度来控制。本方法以及所得具有基质状或海绵状结构的微球的独特原理,与传统的储库型装置药物(如微胶囊)相比,具有独特的优势。