药物肠吸收机制在胰岛素口服制剂设计中的应用  

The Absorption Mechanism for Intestinal Drugs and its Application in the Oral Dosage-Form Design for Insulin

作　　者：李益[1] 魏振平[1] Li Yi;Wei Zhenping(School of Chemical Engineering and Technology,Tianjin University,Tianjin 300072,China)

机构地区：[1]天津大学化工学院,天津300072

出　　处：《化学工业与工程》2019年第2期73-79,共7页Chemical Industry and Engineering

基　　金：天津市自然科学基金(14JCYBJC29100)

摘　　要：提高口服胰岛素的生物利用度一直是药学工作者研究的热点内容。介绍了药物在肠内经细胞间和跨细胞转运吸收的一般机制,详述了胰岛素在胃肠道中所面临的物理和化学屏障、酶屏障以及对此采取的相应措施,建议:在胰岛素制剂加工过程中,采用温和的pH值和温度环境并尽量避免使用有机溶剂,以最大限度保留药物的生物活性;对胰岛素采用微囊包衣以降低胃肠道的化学屏障或酶屏障对其稳定性的影响;开发广谱酶抑制剂并用于胰岛素口服制剂,以对抗肠道内的蛋白酶对其降解。Improving the bioavailability of insulin after oral delivery has long been one of the hot topics for pharmaceutical scientists. In this review, we summarized the general mechanism for intestinal drug absorption by transcellular and paracellular routes with the details on the physical, chemical and enzyme barriers for intestinal insulin, as well as the corresponding measures that should be taken to overcome these obstacles. Those measures are : Establishment of mild conditions of pH and temperature as well as avoiding the use of organic solvents during the preparation of oral insulin so that its biological activity could be maximally retained;encapsulation of insulin into carrier to prevent it from chemical or enzymatic degradation in intestinal tract;development of broad spectrum enzyme inhibitors and their application in the manufacture of oral insulin preparations to resist the enzymatic degradation.

关 键 词：胰岛素 口服给药系统 细胞间及跨细胞转运 生物利用度 

分 类 号：R914[医药卫生—药物化学]