影响羧甲基魔芋胶骨架片体外释药的处方和工艺因素  

Formulation and preparation factors of drug release from carboxymethyl konjac glucomannan matrix tablet

作　　者：刘蔚[1] 张瑜[2] 杨磊[2] 宋卫中[2] 

机构地区：[1]河南大学第一附属医院药剂科,河南开封475001 [2]河南大学中药研究所,河南开封475004

出　　处：《河南大学学报（医学版）》2012年第4期277-280,共4页Journal of Henan University:Medical Science

基　　金：河南省2010年政府招标项目(B087)

摘　　要：目的考察影响羧甲基魔芋胶骨架片体外释药的因素。方法以羧甲基魔芋胶(CMKGM)为骨架材料,用湿法制粒压片和粉末直接压片法制备缓释骨架片,并考察CMKGM粒径、骨架材料的用量、填充剂种类、制备工艺和压片压力对羧甲基魔芋胶骨架片体外释放速率的影响。结果氨茶碱羧甲基魔芋胶骨架片的释药均符合Peppas方程,释药机制为药物扩散和骨架溶蚀协同作用;填充剂种类、骨架材料用量对氨茶碱的释放速率有显著影响;骨架片的释药速率随骨架材料用量的增加而减慢;聚丙烯酸树脂L100减慢药物释放,而乳糖则加快药物的释放;CMKGM粒径、制备工艺和压片压力对药物释放无显著影响。结论羧甲基魔芋胶骨架片具有缓慢释药特性,其释药机理为溶蚀释放和扩散释放协同作用;影响氨茶碱CMKGM骨架片释药速率的主要因素为骨架材料用量和填充剂种类。Objective To study the influencing factors of aminophylline release from carboxymethyl konjac glucomannan（CMKGM） hydrophilic matrix tablets.Methods The CMKGM matrix tablets containing aminophylline as a model drug were obtained by direct compression or wet granulation.The effects of the amount of the matrix materials,particle size of CMKGM,the kinds of diluent agent,preparation method,compressing pressure on drug release in vitro were studied.Results To all case,the release behavior of the matrix tablets follows the Peppas equation,and the mechanism is non-Fickian coupling diffusion and erosion model.With an increase of CMKGM,the drug release rate was decreased significantly.Compared with starch as diluent agent,the rate of drug release was decreased with Eudragit L100,and the rate of drug release was increased with lactose.Conclusion The release mechanism of aminophylline from CMKGM matrix tablets is non-Fickian release coupling diffusion and erosion modle.The main factors influencing drug release are the amount of the matrix materials and the kind of diluent agent.

关 键 词：氨茶碱 羧甲基魔芋胶 骨架片 体外释药 

分 类 号：R962[医药卫生—药理学]