Bioavailability of dalargin and its metabolism during intranasal administration to rats
Vinogradov, V.A.; Kalenikova, E.I.; Sokolov, A.S.
Biulleten' Eksperimental'noi Biologii i Meditsiny 106(7): 48-50
1988
ISSN/ISBN: 0365-9615 PMID: 3401577 Document Number: 319471
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.