目的研究影响盐酸青藤碱κ-卡拉胶/魔芋胶骨架片体外释药机制的处方和工艺因素。方法采用粉末直接压片和湿法制粒压片制备盐酸青藤碱κ-卡拉胶/魔芋胶骨架片,考察κ-卡拉胶与魔芋胶配比,骨架材料用量,填充剂种类,片剂大小,压片工艺,压片压力对骨架片体外释药机制的影响。结果盐酸青藤碱κ-卡拉胶/魔芋胶骨架片的释药机制为药物扩散和骨架溶蚀协同作用;随κ-卡拉胶与魔芋胶配比中κ-卡拉胶用量降低,骨架材料用量降低,填充剂水溶性降低,片剂直径增加,压片压力降低,骨架片释药机制中扩散释放所占比重增加;压片工艺对骨架片药物释放机理影响不大。结论κ-卡拉胶与魔芋胶复配可作为载体材料使用延缓盐酸青藤碱κ-卡拉胶/魔芋胶骨架片中药物释放;κ-卡拉胶与魔芋胶配比,骨架材料用量,填充剂种类,片剂直径和压片力为影响骨架片释药机制的主要因素。

Objective To study the formulation and preparation factors influencing in vitro release mechanism of drug from κ-carrageenan/konjac glucomannan hydrophilic matrix tablets.Methods The matrix tablets containing sinomenine hydrochloride as a model drug were obtained by direct compression method or wet granulation technique.The effects of the ratios of ,κ-carrageenan/konjac glucomannan, the amount of matrix materials,the kinds of diluent agent，tablet size，preparation method，and compressing pressure on release mechanism of the matrix tablets were studied by evaluating the n value in the Peppas equation.Results The release mechanism of the matrix tablets was non-Fickian release that coupled diffusion and erosion modle.With a decrease in the ratio of κ-carrageenan/konjac glucomannan，a decrease in the amount of matrix materials,a decrease in the water-solubility of diluent agents，an increase in tablet size，and a decrease in compressing pressure, the ratio of drug diffusion was increased. Preparation method had little influence on drug release mechanism. Conclusion Drug could be slowly released from the matrix tablets containing -carrageenan/konjac glucomannan as matrix material，the main factors influencing drug release mechanism are the ratio of κ-carrageenan/konjac glucomannan, the amount of matrix materials，the kinds of diluent agent，tablet size, and compressing pressure.