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目的研究多索茶碱脉冲控释微丸的制备工艺,并考察其释药性能。方法以微晶纤维素为骨架材料采用挤出滚圆法制备载药丸芯,通过流化床包衣法分别覆上交联羧甲基纤维素钠作为溶胀层、乙基纤维素和羟丙甲纤维素作为控释层制备多索茶碱脉冲微丸,通过单因素考察筛选丸芯、溶胀层、控释层的处方组成对体外释药性能的影响。结果以微晶纤维素、羧甲基淀粉钠和乳糖为添加剂可制得性能良好的高载药微丸。随着溶胀层厚度的增加,药物释放时滞变短,速率显著增加;随着控释层包衣厚度的增加,时滞延长,释药减慢;控释层中羟丙甲纤维素用量或分子量增加,时滞缩短;控释层中增塑剂用量增加,时滞延长。结论所得包衣微丸具有良好的脉冲释药性能,有广阔的应用前景。
Objective To study the preparation process of doxofylline pulse controlled release pellets and study its drug release properties. Methods microcrystalline cellulose as the skeleton material was prepared by extrusion spheronization pellets loaded with fluidized bed coating were coated with sodium croscarmellose as the swelling layer, ethyl cellulose and hypromellose Doxofylline pulsed pellets as the controlled release layer were prepared. The effects of prescription composition of the cores, swollen layer and controlled release layer on drug release in vitro were investigated by single factor test. Results Microcapsules, sodium carboxymethyl starch and lactose were used as additives to prepare highly loaded drug-loaded pellets. With the increase of the thickness of the swelling layer, the drug release delay becomes shorter and the rate increases significantly. With the increase of the thickness of the controlled release coating, the time delay is prolonged and the drug release slows down. The dosage of hypromellose or Molecular weight increases, the time delay shortened; controlled release layer plasticizer dosage increases, the delay prolongation. Conclusion The obtained coated pellets have good properties of pulsed release and have broad application prospects.