果胶-壳聚糖-卵磷脂复合凝胶球结肠给药的性能考察  

Properties of Pectin-chitosan-lecithin Composite Microspheres for Targeted Drug Delivery to Colon

作　　者：郭春静 谭丽珠 李倩 高雅 武文洁 

机构地区：[1]天津科技大学化工与材料学院,天津300457

出　　处：《中国医药工业杂志》2017年第9期1332-1338,共7页Chinese Journal of Pharmaceuticals

摘　　要：探讨壳聚糖和卵磷脂对果胶凝胶球的改性作用,以酮洛芬(KTP)为药物模型,对比不同交联剂(Ca^(2+)和Zn^(2+))形成的果胶-壳聚糖-卵磷脂复合凝胶球的性能。通过改变处方的壳聚糖浓度、卵磷脂浓度、交联剂p H值等进行单因素试验,考察各因素对凝胶球粒径、粒重、载药量、包封率和体外释药的影响。结果表明,壳聚糖的加入对钙体系和锌体系的凝胶球载药量影响不大;随着卵磷脂的加入,2种凝胶球的载药量都呈现降低趋势;2种凝胶球的包封率都在一定范围内随着壳聚糖和卵磷脂浓度的增加而升高。载KTP的钙体系果胶-壳聚糖-卵磷脂复合凝胶球在模拟小肠(SIF)阶段释药90%以上,达不到结肠给药的目的 ;锌体系果胶-壳聚糖-卵磷脂复合凝胶球在SIF阶段释药10%,在模拟结肠液(SCF)阶段释药83.21%,提示壳聚糖、卵磷脂共同改性的果胶锌凝胶球有一定的结肠给药效果。In this paper, pectin-chitosan-lecithin composite microspheres with Ca2＋ or Zn^2＋ as the crosslinking agent, which were used to load ketoprofen （KTP） for oral colon-specific drug delivery, were prepared and investigated. By a single factor analysis for chitosan concentration, lecithin concentration, pH value of crosslinking solution, the effects of above factors on size, bead weight, encapsulation efficiency, drug loading and in vitro release were investigated. The results showed that chitosan had no significant influence on drug loading of both calcium and zinc pectinate composite microspheres; while the drug loading of both gel beads decreased with the increasing of the lecithin amount. In a certain extent, the encapsulation efficiency of both gel beads increased with the increasing of the amounts of chitosan and lecithin. The release of KTP from the calcium pectinate composite microspheres was above 90% in simulated intestinal fluid （SIF）, which was not suitable for colon targeted drug delivery. However, the release form zinc pectinate composite microspheres in SIF was about 10% and in simulated colonic fluid （SCF） was 83.21%. These findings indicated that the zinc-pectin- chitosan-lecithin composite microspheres had a potential for colon-targeted drug delivery.

关 键 词：果胶 结肠给药系统 壳聚糖 卵磷脂 酮洛芬 交联剂 

分 类 号：R944.9[医药卫生—药剂学]