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Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes.
J Pharm Pharmacol. 1997 Nov; 49(11):1057-61.JP

Abstract

The permeation of ebiratide (H-Met(O2)-Glu-His-Phe-D-Lys-Phe-NH(CH2)8NH2), a novel ACTH analogue, across the intestinal mucosae has been examined by use of isolated intestinal membranes from rats in a modified Ussing chamber. Regional differences were observed in the permeation of ebiratide across intestinal membranes; the order of membrane permeability was jejunum > ileum > duodenum > colon. Overall, the permeation of ebiratide was relatively poor. The effects of various absorption enhancers were examined to increase the intestinal permeability to ebiratide. Sodium glycocholate and sodium caprate had no significant enhancing effect on the permeability of the jejunal membrane, but significantly enhanced the permeation of ebiratide through the colonic membrane. On the other hand, N-dodecyl-beta-D-maltopyramoside (LM) significantly enhanced the permeation of ebiratide through both jejunal and colonic membranes. In general, the absorption-enhancing effects of these agents were more predominant in the colon than in the jejunum. Membrane damage by the absorption enhancers was evaluated by measuring the amount of protein released from the intestinal membrane. It was found that all the absorption enhancers slightly increased the amount of protein released, but that the amounts of protein released in the presence of these enhancers were much less than in the presence of ethylenediaminetetraacetic acid (EDTA), used as a positive control. These findings suggest that the absorption enhancers, especially LM might be useful adjuvants for improving the intestinal absorption of peptide and protein drugs, including ebiratide.

Authors+Show Affiliations

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

9401937

Citation

Yamamoto, A, et al. "Effects of Different Absorption Enhancers On the Permeation of Ebiratide, an ACTH Analogue, Across Intestinal Membranes." The Journal of Pharmacy and Pharmacology, vol. 49, no. 11, 1997, pp. 1057-61.
Yamamoto A, Okagawa T, Kotani A, et al. Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes. J Pharm Pharmacol. 1997;49(11):1057-61.
Yamamoto, A., Okagawa, T., Kotani, A., Uchiyama, T., Shimura, T., Tabata, S., Kondo, S., & Muranishi, S. (1997). Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes. The Journal of Pharmacy and Pharmacology, 49(11), 1057-61.
Yamamoto A, et al. Effects of Different Absorption Enhancers On the Permeation of Ebiratide, an ACTH Analogue, Across Intestinal Membranes. J Pharm Pharmacol. 1997;49(11):1057-61. PubMed PMID: 9401937.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes. AU - Yamamoto,A, AU - Okagawa,T, AU - Kotani,A, AU - Uchiyama,T, AU - Shimura,T, AU - Tabata,S, AU - Kondo,S, AU - Muranishi,S, PY - 1997/12/24/pubmed PY - 1997/12/24/medline PY - 1997/12/24/entrez SP - 1057 EP - 61 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 49 IS - 11 N2 - The permeation of ebiratide (H-Met(O2)-Glu-His-Phe-D-Lys-Phe-NH(CH2)8NH2), a novel ACTH analogue, across the intestinal mucosae has been examined by use of isolated intestinal membranes from rats in a modified Ussing chamber. Regional differences were observed in the permeation of ebiratide across intestinal membranes; the order of membrane permeability was jejunum > ileum > duodenum > colon. Overall, the permeation of ebiratide was relatively poor. The effects of various absorption enhancers were examined to increase the intestinal permeability to ebiratide. Sodium glycocholate and sodium caprate had no significant enhancing effect on the permeability of the jejunal membrane, but significantly enhanced the permeation of ebiratide through the colonic membrane. On the other hand, N-dodecyl-beta-D-maltopyramoside (LM) significantly enhanced the permeation of ebiratide through both jejunal and colonic membranes. In general, the absorption-enhancing effects of these agents were more predominant in the colon than in the jejunum. Membrane damage by the absorption enhancers was evaluated by measuring the amount of protein released from the intestinal membrane. It was found that all the absorption enhancers slightly increased the amount of protein released, but that the amounts of protein released in the presence of these enhancers were much less than in the presence of ethylenediaminetetraacetic acid (EDTA), used as a positive control. These findings suggest that the absorption enhancers, especially LM might be useful adjuvants for improving the intestinal absorption of peptide and protein drugs, including ebiratide. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/9401937/Effects_of_different_absorption_enhancers_on_the_permeation_of_ebiratide_an_ACTH_analogue_across_intestinal_membranes_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0022-3573&date=1997&volume=49&issue=11&spage=1057 DB - PRIME DP - Unbound Medicine ER -