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处方和工艺因素对氨茶碱魔芋胶骨架片体外释放度的影响
Effect of formulation and preparation process on in vitro release of aminophylline from konjac glucomannan matrix tablets
【摘要】 目的:考察处方和工艺因素对魔芋胶骨架片体外释放度的影响,评价魔芋胶作为新型载体材料用于缓释骨架片制备的可行性。方法:以氨茶碱为模型药物,采用粉末直接压片法和湿法制粒压片法制备魔芋胶骨架片,考察魔芋胶粒度、黏度和用量,填充剂种类,主药粒度,压片工艺,压片压力等对其体外药物释放的影响。结果:氨茶碱魔芋胶骨架片可缓慢释放药物;随魔芋胶粒度降低,骨架材料用量或主药粒度增加,药物释放减慢;与淀粉、微晶纤维素和乳糖相比,Eudragit L100作为填充剂,可明显延缓药物释放;压片工艺,压片压力和魔芋胶黏度对药物释放影响不大。结论:魔芋胶可作为一种新型载体材料用于缓释骨架片的制备,魔芋胶粒度、用量,主药粒度和填充剂种类是影响骨架片体外药物释放的主要因素。
【Abstract】 OBJECTIVE The effects of formulation and preparation process on in vitro drug release of aminaphyline from konjac glucomannan(KGM)hydrophilic matrix tablets were studied to evaluate the feasibility of KGM used as new carrier material to prepare sustained-release matrix tablets.METHODS The KGM matrix tablets containing aminophylline as model drug were prepared by direct compression method or wet granulation technique.The effect of the amount,viscosity and particle size of KGM,the kinds of diluent agent,preparation method,particle size of drug,compressing pressure on in vitro drug release from the matrix tablets were studied.RESULTS Drug could be released slowly from the matrix tablets.With a decrease in the particle size of KGM,an increase in the amount of KGM or the particle size of drug,the drug release rate was decreased significantly.Compared with starch,microcrystalline cellulose or lactose used as diluent,the drug release rate was decreased significantly with Eudragit L100.KGM viscosity grades,preparation method and compressing pressure had little influence on drug release rate.CONCLUSION KGM could be used as a new carrier material to prepare sustained-release matrix preparations.The main factors influencing drug release are the amount and particle size of KGM,particle size of drug,the kinds of diluent.
【Key words】 aminophylline; konjac glucomannan; matrix tablets; in vitro drug release;
- 【文献出处】 中国医院药学杂志 ,Chinese Journal of Hospital Pharmacy , 编辑部邮箱 ,2008年23期
- 【分类号】TQ461
- 【被引频次】1
- 【下载频次】170