摘要
胰高血糖素样肽-1受体激动剂(Glucagon-like peptide-1receptor agonists,GLP-1RAs)是近年来进入2型糖尿病治疗领域的新型多肽类药物,因其具有良好的心血管收益、体重控制效果且不产生低血糖危险等特性,受到越来越多的关注。然而目前已上市的7种GLP-1RAs类药物均为注射剂型,长期注射给药会降低患者的依从性,因此口服剂型的开发一直受到广泛关注。文章对口服递送GLP-1RAs的解决方案进行综述,重点介绍用于改善GLP-1及其类似物口服生物利用度的策略,包括研制含有吸收促进剂、细胞穿透肽、黏膜粘附剂和药物递送系统的新型制剂。
Glucagon-like peptide-1 receptor-1 receptor agonists( GLP-1 RAs) are novel peptide drugs for the treatment of type 2 diabetes in recent years. They have gained increasing attention because of their good cardiovascular benefits and weight control effects without the risk of hypoglycemia. However,the seven GLP-1 RAs currently listed are all injected subcutaneously and the long-term administration of injections will reduce the patient’s compliance. Therefore,the development of oral dosage forms has received widespread attention. This article reviews the solutions for oral delivery of GLP-1 RAs and focuses on current strategies for improving the oral bioavailability of GLP-1 and its analogues,including development of new formulations with absorption enhancers,cell penetrating peptides,mucoadhesive polymers and drug delivery systems.
作者
葛阳
赛文博
田浤
唐道琪
姚文兵
GE Yang;SAI Wen-bo;TIAN Hong;TANG Dao-qi;YAO Wen-bing(Jiangsu Key Laboratory of Drug Gability of Biopharmaceuticals ,China Pharmaceutical University,Nanjing 210009,China;School of Life Science and Technology,China Pharmaceutical University ,Nanjing 210009,China)
出处
《药物生物技术》
CAS
2018年第6期533-536,共4页
Pharmaceutical Biotechnology
基金
国家自然科学基金资助项目(No.81430082
81573335)
国家重大新药创制课题(No.2018ZX09301034001)
关键词
胰高血糖素样肽-1
吸收促进剂
细胞穿透肽
黏膜粘附剂
口服递送
生物利用度
2型糖尿病
Glucagon-kike peptide-1 receptor-1
Absorption enhancers
Cell penetrating peptides
Mucoadhesive polymers
Oral delivery
Bioavailability
Type 2 diabetes
