Abstract:
:In order to estimate the intestinal stability of ebiratide [H-Met(O2)-Glu-His-Phe-D-Lys-Phe-NH(CH2)8-NH2], a novel adrenocorticotropic hormone (ACTH) analogue, after oral administration, the hydrolytic properties of ebiratide were determined in the rat small intestinal fluid and mucosal homogenates. Ebiratide was extremely stable in the rat small intestinal fluid, while it was degraded in various intestinal mucosal homogenates. Regional differences were observed in its proteolytic properties; e.g., the hydrolytic rates of ebiratide in jejunal and ileal mucosal homogenates were 2-3 times faster than that in duodenal and colonic homogenates. Degradation of ebiratide was markedly inhibited by aminoprotease inhibitors such as sodium glycocholate, puromycin, bestatin and bacitracin. These results suggest that co-administration of certain protease inhibitors are useful to improve the stability of ebiratide in the intestine.
journal_name
Life Scijournal_title
Life sciencesauthors
Okagawa T,Fujita T,Murakami M,Yamamoto A,Shimura T,Tabata S,Kondo S,Muranishi Sdoi
10.1016/0024-3205(94)00674-1subject
Has Abstractpub_date
1994-01-01 00:00:00pages
677-83issue
9eissn
0024-3205issn
1879-0631pii
0024-3205(94)00674-1journal_volume
55pub_type
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