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采用乳液-溶剂扩散法制备含丙烯酸聚合物的布洛芬长效释放球形微基质以提高生物利用度。

Preparation of prolonged-release spherical micro-matrix of ibuprofen with acrylic polymer by the emulsion-solvent diffusion method for improving bioavailability.

作者信息

Kawashima Y, Niwa T, Handa T, Takeuchi H, Iwamoto T, Itoh Y

出版信息

Chem Pharm Bull (Tokyo). 1989 Feb;37(2):425-9. doi: 10.1248/cpb.37.425.

Abstract

Prolonged-release spherical micro-matrices of ibuprofen with acrylic polymer (Eudragit RS) were prepared using a novel emulsion-solvent diffusion method. It was found by examining cross sections of the spherical matrix before and after dissolution tests with a scanning electron microscope and a porosimeter that the resultant micro-matrix had a sponge-like internal structure. The spherical matrices were successfully recovered with a relatively high concentration of the drug in ethanol (0.4-0.6 g/ml) and over a wide range of temperatures (5-35 degrees C). The size of the spherical matrix could be easily controlled by varying the agitation speed of the system and the concentration of emulsifier added to the aqueous medium. The drug release rate from the spherical matrix decreased with increasing concentration of polymer formulated due to the reduced diffusion path and increased tortuosity in the matrix. Spherical matrices with ibuprofen:Eudragit RS = 3:1 improved the bioavailability of the drug and prolonged the drug action in beagle dogs.

摘要

采用一种新型乳液-溶剂扩散法制备了含丙烯酸聚合物(Eudragit RS)的布洛芬缓释球形微基质。通过扫描电子显微镜和孔隙率仪对球形基质在溶出试验前后的横截面进行检查发现,所得微基质具有海绵状内部结构。球形基质在乙醇中药物浓度相对较高(0.4 - 0.6 g/ml)且在较宽温度范围(5 - 35℃)内均能成功回收。通过改变体系的搅拌速度和添加到水相介质中的乳化剂浓度,可以轻松控制球形基质的大小。由于基质中扩散路径缩短和曲折度增加,球形基质中药物的释放速率随聚合物配方浓度的增加而降低。布洛芬与Eudragit RS比例为3:1的球形基质提高了药物在比格犬体内的生物利用度并延长了药物作用时间。

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