[Bioavailability of dalargin and its metabolism during intranasal administration to rats].
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.
Vinogradov
V A
VA
Kalenikova
E I
EI
Sokolov
A S
AS
D000281:Administration, Intranasal; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D001682:Biological Availability; D004743:Enkephalin, Leucine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D000897:Anti-Ulcer Agents; D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine; C040996:enkephalin-Leu, Ala(2)-Arg(6)-
Biodostupnost' dalargina i ego metabolizm pri intranazal'nom vvedenii krysam.