口服胰岛素制剂的研究进展  

Research progress of oral insulin preparations

作　　者：张艺卓[1,2] 张俊伟[3] 尹东东[2] 王杏林[2] 宋艳宁 

机构地区：[1]河南大学药学院,开封475001 [2]天津药物研究院有限公司释药技术与药动学国家重点实验室,天津300193 [3]国家食品药品监督管理总局药品审评中心,北京100038

出　　处：《中国新药杂志》2015年第22期2560-2566,2571,共8页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2014ZX09507005-001)

摘　　要：胰岛素是治疗糖尿病最有效的药物之一,主要以注射给药方式应用于临床。口服胰岛素经胃肠吸收后,由门静脉直接进入肝脏,在一定程度上模拟了人体正常生理途径,同时口服给药可提高患者依从性,具有明显的临床应用优势。但由于口服胰岛素制剂生物利用度较低,血糖控制仍不稳定,使其临床应用受限。本文主要从提高口服生物利用度,改善血糖控制两个方面,综述了提高口服胰岛素临床疗效的方法,并简单介绍了进入临床阶段口服制剂的研究现状。Insulin is one of the most effective therapeutic drugs for the treatment of diabetes mellitus. Sub- cutaneous administration of insulin remains to be the preferred approach in clinic. When oral insulin is absorbed by the gastrointestinal tract, it directly enters into the liver through portal vein circulation. The mechanism is very sim- ilar to the absorption of endogenous insulin to a certain extent. At the same time, administration via the oral route has good patient compliance. Thus, this delivery mode has significant clinical advantage. However, the clinical ap- plication of oral insulin preparations is restricted because of its low bioavailability and unstable glycemic control. In this review, approaches to improve clinical effect of oral insulin were summarized mainly in aspects of enhancing o- ral bioavailability and improving glycemic control. We also briefly introduced the research progress of oral insulin formulations in clinical stage.

关 键 词：口服胰岛素 糖尿病 生物利用度 血糖控制 研究进展 

分 类 号：R977.15[医药卫生—药品]