多肽药物口服递送技术研究进展  

Research progress in oral delivery technology of therapeutic peptides

作　　者：黄侃 孙敏捷[1] HUANG Kan;SUN Min-jie(Department of Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学药剂教研室,南京211198

出　　处：《中国新药杂志》2022年第14期1380-1386,共7页Chinese Journal of New Drugs

摘　　要：多肽高效低毒,作为治疗药物具有巨大的潜力,但患者常因无法忍受长期注射给药而不得不放弃治疗,严重影响生存质量。相比之下,口服给药具有高顺应性、自助给药、低成本的优势,但也受到胃肠道生化环境、黏液、上皮渗透和肝脏消除的限制,因此开发多肽口服递送系统面临巨大挑战。本文介绍克服多肽口服给药障碍所采用的技术,包括结构修饰与环化、促渗透技术、纳米技术和药械组合技术,并重点介绍已上市产品和具有巨大临床突破的技术。Peptides have a great potential as therapeutic agents,with advantages of potent effects and low toxicity.However,a large number of patients cannot be able to bear long-term injection and have to give up treatment,seriously affecting the quality of life.In contrast,oral administration has the advantages of high compliance,self-delivery and low cost.However,oral peptides are limited by gastrointestinal biochemical environment,mucus,epithelial infiltration and liver elimination.Thus,it is a great challenge to develop drug delivery systems for oral administration of peptides.This article highlighted strategies designed to overcome these barriers,including conjugation and cyclization of peptides,permeation enhancers,nanotechnology,nanoparticles,and combination products.It then focused on the technologies of approved oral peptides and products with great clinical breakthroughs.

关 键 词：多肽药物 口服递送 渗透促进剂 药械组合 纳米技术 

分 类 号：R944.[医药卫生—药剂学]