Vinogradov V A, Kalenikova E I, Sokolov A S
Biull Eksp Biol Med. 1988 Jul;106(7):48-50.
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.
已对化学结构为Tyr-D-Ala-Gly-Phe-Leu-Arg的肽类药物达乐argin的生物利用度和代谢情况进行了研究。达乐argin用于治疗胃和十二指肠溃疡。通过在麻醉犬身上经肌肉注射（i/m）和鼻内（i/n）途径给予³H-达乐argin来评估生物利用度。i/m和i/n给药后约10分钟达到最高达乐argin浓度。达乐argin的绝对生物利用度分别为15%和8%，而其消除半衰期分别为23.2分钟和21.3分钟。酪氨酸、N端四肽和五肽是血液中检测到的主要代谢产物。得出结论，达乐argin的鼻内给药途径在临床实践中是可行的。
