Kawashima Y, Handa T, Kasai A, Takenaka H, Lin S Y, Ando Y
J Pharm Sci. 1985 Mar;74(3):264-8. doi: 10.1002/jps.2600740308.
A novel method for the preparation of theophylline granules coated with a polyelectrolyte complex of sodium tripolyphosphate and chitosan was developed. The theophylline granules containing sodium tripolyphosphate were stirred in an HCl solution of chitosan. During the mixing, the dissolved sodium tripolyphosphate in the granule moved to the surface and reacted with the chitosan, resulting in the formation of the polyelectrolyte complex film. The factors affecting the drug content, the particle size, and the coating-film thickness of the resultant coated granules were determined. The theophylline content in the coated granule decreased with increasing content ratio of sodium tripolyphosphate to theophylline in the original granule and with increasing chitosan concentration in the coating solution. The coated granule size increased with increasing chitosan concentration in the coating solution and with decreasing agitation speed. The coating-film thickness increased with an increase in the chitosan concentration, the pH of the coating solution, and the sodium tripolyphosphate to theophylline content ratio in the original granule. The drug-release pattern of the coated granules followed zero-order kinetics and the release rates were significantly reduced compared with that of the original granule.
开发了一种制备用三聚磷酸钠和壳聚糖的聚电解质复合物包衣的茶碱颗粒的新方法。将含有三聚磷酸钠的茶碱颗粒在壳聚糖的盐酸溶液中搅拌。在混合过程中，颗粒中溶解的三聚磷酸钠迁移到表面并与壳聚糖反应，从而形成聚电解质复合膜。确定了影响所得包衣颗粒的药物含量、粒径和包衣膜厚度的因素。包衣颗粒中的茶碱含量随着原始颗粒中三聚磷酸钠与茶碱的含量比增加以及包衣溶液中壳聚糖浓度的增加而降低。包衣颗粒尺寸随着包衣溶液中壳聚糖浓度的增加和搅拌速度的降低而增大。包衣膜厚度随着壳聚糖浓度、包衣溶液的pH值以及原始颗粒中三聚磷酸钠与茶碱的含量比的增加而增加。包衣颗粒的药物释放模式遵循零级动力学，与原始颗粒相比，释放速率显著降低。
