蛋白多肽类药物口服微球给药系统的研究进展  

Research Progresses in Microspheres Containing Protein and Peptide Drugs for Oral Delivery

作　　者：冯地桑 陈龙楷 权桂兰[1] 潘昕[1] 吴传斌[1,2] 

机构地区：[1]中山大学药学院,广东广州510006 [2]广东省高校创新药物制剂工程技术研究中心,广东广州510006

出　　处：《中国医药工业杂志》2016年第11期1464-1469,共6页Chinese Journal of Pharmaceuticals

摘　　要：由于胃肠道消化酶的降解作用和肠道上皮组织的低通透性,蛋白多肽类药物的口服生物利用度一直偏低。本文介绍了微粒在人体胃肠道的转运机制,并概述了蛋白多肽类药物口服微球给药系统的研究进展。口服微球进入胃肠道后可靶向到派尔集合淋巴结,通过跨膜转运等方式被吸收进入体循环。提高蛋白多肽类药物微球给药系统口服生物利用度的策略有以下几种:利用特定的载体材料制备结肠靶向、生物黏附等功能性微球;加入酶抑制剂或吸收促进剂;制备具有多重功能的组合型口服微球系统。The bioavailability of oral administration for protein and peptide drugs is always poor due to the enzymatic degradation in the gastrointestinal tract and the low permeability of epithelial cellular membrane. In this paper, the transport mechanisms of particulates in gastrointestinal tract are introduced and the research progresses in oral delivery system of microspheres containing protein and peptide drugs are reviewed. Microspheres after oral administration can be absorbed by the Peyer＇s patches and passed to the systemic circulation through several transport ways such as transmembrane transport. There are several strategies to enhance the oral bioavailability of microspheres containing protein and peptide drugs, such as preparing colon-specific targeting or bioadhesive microspheres with special carriers, adding enzyme inhibitors or absorption enhancers, as well as preparing multi-functional microspheres.

关 键 词：蛋白多肽类药物 微球 口服给药 转运机制 结肠靶向 生物黏附 口服生物利用度 综述 

分 类 号：R944.9[医药卫生—药剂学]