[Improvement of transmucosal absorption of biologically active peptide drugs].
[Improvement of transmucosal absorption of biologically active peptide drugs].
复制标题
[改善生物活性肽药物的经粘膜吸收]。
DOI：
--
复制
发表时间：
2001
期刊：
影响因子：
--
通讯作者：
A. Yamamoto
中科院分区：
文献类型：
--
作者：
A. Yamamoto
多肽和蛋白质类药物正成为一类非常重要的治疗药物。然而，多肽和蛋白质药物的口服生物利用度普遍较差，因为它们在胃肠道中被蛋白酶广泛降解或不能通过肠粘膜。对于多肽和蛋白质药物的全身给药，目前需要肠外给药来实现它们的治疗活性。然而，这种用法被患者接受程度较低，可能会引起过敏反应和严重的副作用。因此，当这些多肽进入胃肠道和其他粘膜部位时，人们已经研究了各种方法来克服它们的递送问题。这些方法包括(1)使用吸收促进剂和蛋白酶抑制剂等添加剂，(2)开发可替代口服和注射给药的多肽给药方法，(3)改变多肽和蛋白质药物的分子结构以生产前药和类似物，以及(4)使用这些多肽药物的剂型。在这项研究中，我们证明了通过使用这些方法可以改善胰岛素、降钙素、胃泌素和促甲状腺激素释放激素(TRH)等多种多肽的跨粘膜吸收。因此，这些方法可能为我们改善多肽和蛋白质药物的经粘膜吸收提供基础信息。
Peptide and protein drugs are becoming a very important class of therapeutic agents. However, the oral bioavailability of peptide and protein drugs is generally poor because they are extensively degraded by proteases in the gastrointestinal tract or impermeable through the intestinal mucosa. For the systemic delivery of the peptide and protein drugs, parenteral administration is currently required to achieve their therapeutic activities. However, this administration is poorly accepted by patients and may cause allergic reactions and serious side effects. Therefore, various approaches have been examined to overcome the delivery problems of these peptides when they are administered into the gastrointestinal tract and other mucosal sites. These approaches include (1) to use additives such as absorption enhancers and protease inhibitors, (2) to develop an administration method for peptides that can serve as an alternative to oral and injection administration, (3) to modify the molecular structure of peptide and protein drugs to produce prodrugs and analogues, and (4) to use the dosage forms to these peptide drugs. In this study, we demonstrated that the transmucosal absorption of various peptides including insulin, calcitonin, tetragastrin and thyrotropin releasing hormone (TRH) could be improved by the use of these approaches. Therefore, these approaches may give us basic information to improve the transmucosal absorption of peptide and protein drugs.
白化兔直肠胰岛素通透性增强的机制研究。
DOI：
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发表时间：
1992
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Yamamoto,A;Hayakawa,E;Kato,Y;Nishiura,A;Lee,VH
通讯作者：
Lee,VH
影响因子：
56.9
作者：
SAFFRAN, M;KUMAR, GS;NECKERS, DC
通讯作者：
NECKERS, DC