A NEW APPROACH TO THE ORAL-ADMINISTRATION OF INSULIN AND OTHER PEPTIDE DRUGS
A NEW APPROACH TO THE ORAL-ADMINISTRATION OF INSULIN AND OTHER PEPTIDE DRUGS
复制标题
DOI：
10.1126/science.3526553
复制
发表时间：
1986-09-05
期刊：
影响因子：
56.9
通讯作者：
NECKERS, DC
中科院分区：
文献类型：
--
作者：
SAFFRAN, M;KUMAR, GS;NECKERS, DC
众所周知，肽类药物的口服给药会因其在胃和小肠中的消化而受阻。作为一种新的口服给药方法，肽类药物被偶氮芳香基团交联的聚合物包衣，形成一种不渗透的膜，以保护口服给药的药物在胃和小肠中的消化。当偶氮聚合物包衣的药物到达大肠时，固有的微生物菌群减少偶氮键，破坏交联，并降解聚合物膜，从而将药物释放到结肠腔中以进行局部作用或吸收。偶氮聚合物涂层保护和递送口服给药的肽类药物的能力在具有肽类激素血管加压素和胰岛素的大鼠中得到证实。
The oral administration of peptide drugs is well known to be precluded by their digestion in the stomach and small intestine. As a new approach to oral delivery, peptide drugs were coated with polymers cross-linked with azoaromatic groups to form an impervious film to protect orally administered drugs from digestion in the stomach and small intestine. When the azopolymer-coated drug reached the large intestine, the indigenous microflora reduced the azo bonds, broke the cross-links, and degraded the polymer film, thereby releasing the drug into the lumen of the colon for local action orfor absorption. The ability of the azopolymer coating to protect and deliver orally administered peptide drugs was demonstrated in rats with the peptide hormones vasopressin and insulin.