氨茶碱魔芋胶骨架片的体外释放研究

目的：通过体外释放试验对氨茶碱魔芋胶骨架片的体外释药特性及影响因素进行研究。方法：以氨茶碱为模型药物,采用粉末直接压片法制备氨茶碱骨架片,通过体外释放试验研究释放度测定方法,释放介质的pH、离子强度及转速对魔芋胶骨架片体外释药的影响。结果：桨法测得药物的平均释放时间(MDT)明显低于转篮法(P＜0.05)；在不同pH的释放介质中,药物的释放以在蒸馏水中最快,pH 6.8的PBS中次之,0.1 mol·L^-1盐酸液中最慢；药物释放随释放介质离子强度增加而减慢(P＜0.05)；药物释放随搅拌转速增加而加快,但增加至100 r·min^-1后,转速对药物释放影响不大(P＞0.1)；药物释放为扩散和溶蚀机制协同作用。结论：魔芋胶可有效控制骨架片中药物的缓慢释放,可作为一种新型的亲水骨架材料使用。

Studies on drug release from aminophylline konjac glucomannan matrix tablet

OBJECTIVE: In vitro aminophylline release from matrix tablets with konjac glucomannan (KGM) were studied to elevate the feasibility of KGM used as carrier materials to prepare matrix tablets. METHOD: KGM hydrophilic matrix tablets were prepared by direct compression method with aminophylline as the model drug. The effects of test methods, pH values, ionic strength of dissolution media and rotation speeds on drug release were studied by in vitro dissolution experiment. RESULT: The MDT value tested by Paddle method was less than that tested by Basket method (P < 0.05). Among the rate of drug release in different dissolution media, distillded water is the fastest, pH 6. 8 PBS is the second, 0.1 mol x L(-1) HCL is the slowest. MDT increased with increasing the ionic strength of dissolution media (P < 0.05). MDT decreased with increasing the rotation speed, but the rate of drug release did not increase when the rotation speed was more than 100 r x min(-1) (P > 0.1). The mechanism of drug release were diffusion and erosion. CONCLUSION: KGM can be used in sustained delivery systems as a good candidate of hydrophilic polymer.