Hamza A, Șaramet G
"Carol Davila" University of Medicine and Pharmacy - Faculty of Pharmacy, Dept. of Pharmaceutical Technology and Biopharmacy, Bucharest, Romania.
Acta Endocrinol (Buchar). 2020 Jul-Sep;16(3):383-387. doi: 10.4183/aeb.2020.383.
As the medical utility of injectable therapeutic peptides is expanding, so is the challenge of developing technologies that allow the administration of such molecules via alternative routes, considering that chronic patients requiring treatment with parenteral formulations are less adherent and compliant to the therapeutic regimens. Hence, substantial efforts have been made to develop technologies that allow the oral formulation of peptides. Due to their importance in the field of pharmaceutical technology, we describe the latest advancements made in the development of oral salmon calcitonin and oral semaglutide, in co-formulation with absorption enhancers such as 8-[(5-chloro-2-hydroxybenzoyl) amino] octanoic acid (or 5-CNAC) and N-[8-(2-hydroxybenzoyl) amino] caprylate (or SNAC). Oral semaglutide is considered to be a landmark for oral peptide delivery technology, as it is one of the very few successful examples of peptides that can be administered orally. Unlike semaglutide, oral calcitonin is still not approved by the regulatory authorities because it failed to demonstrate the anticipated effects in phase III clinical trials conducted so far. However, the efforts for obtaining an oral form of calcitonin have significantly contributed to the development of technologies that facilitate the absorption of peptide-structure macromolecules.
随着注射用治疗性肽的医学应用不断扩大，开发能够通过替代途径给药此类分子的技术面临的挑战也在增加，因为需要肠胃外制剂治疗的慢性病患者对治疗方案的依从性较差。因此，人们已做出大量努力来开发能够实现肽口服制剂的技术。鉴于它们在制药技术领域的重要性，我们描述了口服鲑鱼降钙素和口服司美格鲁肽与吸收促进剂（如8-[(5-氯-2-羟基苯甲酰基)氨基]辛酸（或5-CNAC）和N-[8-(2-羟基苯甲酰基)氨基]辛酸酯（或SNAC））共同制剂开发方面的最新进展。口服司美格鲁肽被认为是口服肽递送技术的一个里程碑，因为它是极少数能够口服给药的成功肽类例子之一。与司美格鲁肽不同，口服降钙素尚未获得监管机构的批准，因为在迄今为止进行的III期临床试验中，它未能证明预期效果。然而，获得降钙素口服剂型的努力对促进肽结构大分子吸收的技术发展做出了重大贡献。
