摘要
与小分子药物相比,多肽药物因其高选择性与高效性已在医药领域得到广泛应用。但由于较差的药代动力学与有限的生物屏障渗透性等问题,多肽药物的口服生物利用度较低,其通常通过胃肠外途径给药。主要为多肽药物的口服给药进行综述、介绍了多肽类药物面临的挑战及改善其口服稳定性的策略,如酸碱度调节、酶抑制剂、渗透促进剂及化学法修饰,并对纳米粒载体给药系统进行阐述,以期为未来开发设计临床多肽类口服药物提供参考。
Compared with small molecule drugs,peptide drugs had been widely used in the pharmaceutical field because of their high selectivity and efficiency.However,due to their poor kinetics and limited biological barrier permeability,peptide drugs had low oral bioavailability and were usually administered by the parenteral route.This review focused on the oral administration of peptide drugs,introduced the challenges faced by peptide drugs and strategies to improve their oral stability,such as pH regulation,enzyme inhibitors,penetration enhancers and chemical modifications,and elaborated on the nanoparticle carrier delivery system,to provide a reference for the future development and design of clinical peptide oral drugs.
作者
王彬
段丛雪
王珊珊
陈旺
冯自立
WANG Bin;DUAN Cong-xue;WANG Shan-shan;CHEN Wang;FENG Zi-li(School of Biological Science and Engineering,Shaanxi University of Technology,Hanzhong 723000,China;Key Laboratory of resource biology of Shaanxi Province,Shaanxi University of Technology,Hanzhong 723000,China)
出处
《化学试剂》
CAS
北大核心
2023年第1期24-32,共9页
Chemical Reagents
基金
陕西理工大学博士启动基金项目(SLGQD2017-11)
陕南秦巴山区生物资源综合开发协同创新中心产业化培育项目(QBXT-18-1)。
关键词
多肽药物
口服给药
稳定性
纳米粒子
吸收机制
peptide drugs
oral administration
stability
nanoparticles
absorption mechanism
