浅析多肽类药物的口服递送策略

Analysis on the oral delivery strategy of polypeptide drugs

关键词:  多肽  口服吸收障碍  口服递送策略

Key words:  polypeptide  oral malabsorption  oral delivery strategy  

摘要:

与传统的小分子药物相比，多肽具有高效低毒，合成修饰容易、溶解性强等优点。通常，非胃肠道给药是多肽药物最常用的给药途径，然而口服是一种更经济便利的给药途径，不仅可以提高患者的顺应性还可以降低成本。但胃肠道的生理环境造成吸收障碍是多肽类药物在口服递送中面临的主要难题。国内外对多肽类药物的口服递送技术进行了多种探索，取得了一定研究成果。现将对近20年的多肽药物的口服递送技术进行分析总结，包括化学策略、自乳化药物递送技术、微粒给药技术等，这些技术都致力于克服多肽口服给药的胃肠道pH以及酶降解等障碍，促进多肽类药物的口服吸收，延长半衰期，减少给药次数，提高生物利用度，降低药物的毒副作用。这些技术已经在很大程度上提高了多肽类药物口服给药的有效性和安全性，通过以索马鲁肽、奥曲肽等为例深入分析多肽类药物口服给药成功的原因，为进一步提高多肽的口服吸收和临床疗效的研究提供有价值的参考。 关键词：多肽；口服吸收障碍；口服递送策略

Abstract:

Compared with traditional small molecule drugs, polypeptides have the advantages of high efficiency, low toxicity, easy synthesis and modification, and strong solubility. In general, non-gastrointestinal administration is the most commonly used route for peptide drugs, but oral administration is a more economical and convenient route to improve patient compliance and reduce costs. However, the physiological environment of the gastrointestinal tract causes absorption disorders, which is the main problem in the oral delivery of polypeptide drugs. The oral delivery technology of polypeptide drugs has been explored at home and abroad, and some research results have been achieved. The oral delivery technologies of polypeptide drugs in the past 20 years will be analyzed and summarized, including chemical strategies, self-emulsifying drug delivery technologies, and particulate drug delivery technologies.. All these technologies are committed to overcoming the gastrointestinal pH and enzyme degradation obstacles of oral peptide administration, promoting the oral absorption of polypeptide drugs, extending half-life, reducing administration times, and improving bioavailability. Reduce the toxic side effects of drugs. These technologies have greatly improved the effectiveness and safety of oral administration of polypeptide drugs. Through taking somarutide and octreotide as examples, in-depth analysis of the reasons for the success of oral administration of polypeptide drugs provides a valuable reference for further improving the oral absorption and clinical efficacy of polypeptide drugs.