Abstract |
Bioavailability and metabolism of a peptide drug Dalargin with a chemical structure Tyr-D-Ala-Gly-Phe- Leu-Arg have been examined. Dalargin is applied for the treatment of gastric and duodenal ulcers. Bioavailability was estimated following intramuscular (i/m) and intranasal (i/n) routes of administration of 3H-dalargin in anesthetized dogs. The highest dalargin concentration was achieved about 10 min after i/m and i/n administration. Absolute dalargin bioavailability was 15% and 8%, while its elimination half-life was 23.2 min and 21.3 min, respectively. Tyrosine, N-terminated tetra- and pentapeptides were the main metabolites detected in the blood. The intranasal route of dalargin administration is concluded to be possible in the clinical practice.
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Authors | V A Vinogradov, E I Kalenikova, A S Sokolov |
Journal | Biulleten' eksperimental'noi biologii i meditsiny
(Biull Eksp Biol Med)
Vol. 106
Issue 7
Pg. 48-50
(Jul 1988)
ISSN: 0365-9615 [Print] Russia (Federation) |
Vernacular Title | Biodostupnost' dalargina i ego metabolizm pri intranazal'nom vvedenii krysam. |
PMID | 3401577
(Publication Type: Journal Article)
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Chemical References |
- Anti-Ulcer Agents
- Enkephalin, Leucine
- Enkephalin, Leucine-2-Alanine
- enkephalin-Leu, Ala(2)-Arg(6)-
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Topics |
- Administration, Intranasal
- Animals
- Anti-Ulcer Agents
(administration & dosage, metabolism, pharmacokinetics)
- Biological Availability
- Enkephalin, Leucine
(administration & dosage, analogs & derivatives, metabolism, pharmacokinetics)
- Enkephalin, Leucine-2-Alanine
(analogs & derivatives)
- Male
- Rats
- Rats, Inbred Strains
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