环糊精及其衍生物在多肽/蛋白质类药物非注射给药体系中的应用  

The Applications of Cyclodextrins and Their Derivatives in Non-injection Administration Systems of Peptide/Protein Drugs

作　　者：陈星羽[1] 辛剑宇[1] 李建树[1] 

机构地区：[1]四川大学高分子科学与工程学院,成都610065

出　　处：《中国生物工程杂志》2010年第12期111-115,共5页China Biotechnology

基　　金：国家自然科学基金(51073102);教育部留学回国人员科研启动基金(2008890-19-7)资助项目

摘　　要：目前,多肽/蛋白质类药物多数需要采用注射剂型给药以确保其生物利用度。开发易于给药、病人顺应性高以及治疗费用更低的非注射剂型是非常有意义的。然而,多肽/蛋白质类药物直接进行非注射给药的生物利用度通常非常低,需要制备具有设计功能的载药系统,例如加入不同比例的酶抑制剂、吸收促进剂等以提高生物利用度。环糊精及其衍生物由于其能与客体分子形成包合物的特性,以及对粘膜的促渗透作用等,在多肽/蛋白质药物的非注射给药系统中获得了日益广泛的应用。综述了近年来环糊精及其衍生物在多肽/蛋白质类药物非注射给药体系中的应用情况。Nowadays,peptide/protein drugs are administrated by injective formulations to ensure their bioavailability.While non-injection formulations,particularly oral delivery method,are desiderata because they exhibit great advantages such as easier administration,better patient compliance and lower cost.However,the bioavailability is usually very low if the peptide/protein drugs are used directly in the non-injection systems.And it is necessary to develop drug delivery systems with designed functions,such as adding different proportions of the protease inhibitors and/or absorption enhancers to improve drug bioavailability.Cyclodextrins（CDs）and their derivatives can form complexes with various molecules and have the capability to facilitate mucosa permeability,thus are widely applied in the non-injection administration systems of peptide/protein drugs.recent applications of CDs and their derivatives in non-injection administration systems of peptide/protein drugs were reviewed.

关 键 词：环糊精 多肽 蛋白质 非注射给药 

分 类 号：Q819[生物学—生物工程]