结肠定位魔芋胶-羟丙甲纤维素包衣片的制备及体外释药研究  

Study on preparation of konjac glucomannan-hydroxypropyl methyl cellulose compression coated tablets for colonic delivery and in vitro release

作　　者：张瑜[1] 侯世祥[1] 卢懿[1] 陈钢[1] 鞠静红[1] 

机构地区：[1]四川大学华西药学院

出　　处：《中国中药杂志》2006年第8期642-645,共4页China Journal of Chinese Materia Medica

摘　　要：目的:制备魔芋胶-羟丙甲纤维素包衣片,并研究处方工艺及体外释放条件对制剂药物释放的影响,以评价其结肠定位释药效果。方法:湿法制粒压片得到盐酸小檗碱片芯,以魔芋胶与羟丙甲纤维素为包衣材料,制备干法压制包衣片;通过体外释放试验,对影响制剂释药的处方工艺因素进行考察;研究体外释放过程中衣膜的溶蚀情况。结果:在模拟胃肠道上端介质中包衣片几乎不释放药物,在模拟结肠环境的介质中,通过酶降解溶蚀造成衣膜破裂而完全释放药物;处方工艺中,随魔芋胶占衣膜总量的比例减少及衣膜用量增加,药物释放减慢(P<0.05),压力对药物释放无影响(P>0.05);体外释放时,随释放介质中酶含量增加,药物释放加快(P<0.05),而搅拌转速对药物释放无影响(P>0.05);药物释放机制为扩散和溶蚀释药。结论:魔芋胶-羟丙甲纤维素包衣片可达到结肠定位给药的目的。Objective： Prepare konjac glucomaunan-hydmxypropyl methyl ceUulose（HPMC） compression coated tablets and study the effects of the formulation, technics and in vitro dissolution condition on drug release behavior to elevate the colon-specific effects of preparation. Method： Berberine hydrochloride core tablets were prepared by wet granulation technique and konjac glucomannan-HPMC mixture as the coating layer were used with compression coated technique. The effects of the formulation and technics on drug release behavior were investigated by dissolution test. The erosion of coat layer during dissolution test was investigated. Result： Drug almost not released in dissolution medium stimulating gastric and intestinal condition, and released completely by coating layer erosion and rupture by enzyme in stimulating colonic condition. Drug release decreased with decreasing the ratio of konjac glucomannan-HPMC and increasing coat weight（ P 〈 0.05）, compression force was not found to be a significant factor on drug release. Drug release increased with increasing the concentration of β-mannase in dissolution medium（P 〈 0.05）, rotation speed has no effect on drug release. The release of drug was correlative with erosion of coat layer. The mechanism of drug release were diffusion and erosion. Conclusion： The konjac glucomannan-HPMC compression coated tablets was a promising delivery system for drugs to be delivered to the colon.

关 键 词：魔芋胶 压制包衣 酶降解 溶蚀 结肠定位给药系统 

分 类 号：TQ460.1[化学工程—制药化工]