蛋白质和多肽类药物具有良好的选择性和生物活性,已成为治疗众多疾病的首选药物。由于胃肠道内酶的降解作用以及肠道粘膜的低通透性,蛋白质和多肽类药物口服生物利用度极低,其常规给药一直以注射为主。为了使蛋白质和多肽类药物能够广泛应用于临床,研究人员对蛋白质和多肽类药物口服给药系统做了大量研究。目前用于提高蛋白质和多肽类药物口服生物利用度的方法主要有微粒给药系统、内源性细胞转运系统、应用酶抑制剂和黏附给药系统等。文章就这些方法在蛋白质和多肽类药物口服给药中的应用进行了综述。 Proteins and peptide drugs with good selectivity and biological activity, has become the drug of choice for the treatment of many diseases. Due to the degradation of enzymes in the gastrointestinal tract and the low permeability of intestinal mucosa, the oral bioavailability of protein and peptide drugs is extremely low, and their routine administration has been mainly injection. To make proteins and peptides widely available for clinical use, researchers have done a lot of research on oral delivery systems of proteins and peptides. Currently used to improve the oral bioavailability of protein and peptide drugs are the main methods of particle delivery system, endogenous cell transport system, the application of enzyme inhibitors and adhesive delivery systems. The article reviewed the application of these methods in oral administration of protein and peptide drugs.