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[Bioavailability of dalargin and its metabolism during intranasal administration to rats].

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.
AuthorsV A Vinogradov, E I Kalenikova, A S Sokolov
JournalBiulleten' 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 TitleBiodostupnost' dalargina i ego metabolizm pri intranazal'nom vvedenii krysam.
PMID3401577 (Publication Type: Journal Article)
Chemical References
  • Anti-Ulcer Agents
  • Enkephalin, Leucine
  • Enkephalin, Leucine-2-Alanine
  • enkephalin-Leu, Ala(2)-Arg(6)-
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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