胆盐促进药物口服吸收的作用及机制研究进展  

Research Progress on Effect and Mechanism of Bile Salts in Promoting Oral Absorption of Drugs

作　　者：蔡毅范 张子辰 卢懿[1] 戚建平[1] 吴伟[1] CAI Yifan;ZHANG Zichen;LU Yi;QI Jianping;WU Wei(Key Lab.of Smart Drug Delivery of MOE and PLA,School of Pharmacy,Fudan University,Shanghai 201203)

机构地区：[1]复旦大学药学院智能化递药教育部及全军重点实验室,上海201203

出　　处：《中国医药工业杂志》2020年第12期1529-1540,共12页Chinese Journal of Pharmaceuticals

摘　　要：胆盐是具有甾体骨架的生理表面活性剂,能以混合胶束的形式增加亲脂性药物的溶解度,协助极性药物透过肠上皮屏障,从而改善低水溶性和低渗透性药物的口服生物利用度。近年来,胆盐制剂在口服药物递送领域受到了广泛关注,磷脂/胆盐混合胶束、胆盐脂质体、胆盐修饰纳米粒和药物-胆盐缀合物等都是具潜力的载药体系。为此,本文综述了胆盐及其制剂促进药物口服吸收的作用和机制、胆盐载药体系的制备方法,探讨不同体系的优势和不足,以期为高口服生物利用度胆盐制剂的发展提供参考。Bile salts are physiological surfactants with a steroidal core,which can increase the solubility of lipophilic drugs in the form of mixed micelles,assisting polar drugs to overcome intestinal epithelial barrier,thus improving the oral bioavailability of drugs with poor solubility and permeability.Recently,preparations containing bile salts have received widespread attention in the field of oral drug delivery.Phospholipid/bile salt mixed micelles,bilosomes,bile salt modified nanoparticles,drug-bile salt conjugates are all promising drug delivery systems.We review the effect and mechanism of bile salts and their preparations in promoting oral absorption of drugs,as well as the preparation methods of bile salt drug delivery systems.The advantages and disadvantages of these delivery systems are discussed in order to provide some references for the development of bile salt preparations with high oral bioavailability.

关 键 词：胆盐 口服吸收 胶束 脂质体 纳米粒 作用机制 制备方法 

分 类 号：R944.9[医药卫生—药剂学]