Pharmacokinetics of Morocromen in animals and man
Dell, H.D.; Jacobi, H.; Kamp, R.; Lorenz, D.
Arzneimittel-Forschung 32(5): 492-498
1982
ISSN/ISBN: 0004-4172 PMID: 7201825 Document Number: 191598
Investigations in animals (rat, rabbit, dog) and man show, that N-[3-(2-morpholinoethyl)-4-methyl-2-oxo-2H-1-benzopyran-7-yl]-4-morpholinocarboxamide (morocromen) is absorbed fast and is found as unchanged substance in organs (highest concentration in liver and kidneys, low concentration in brain), blood, bile, urine, saliva, sweat and feces. Extent of absorption, metabolisation and half-life are species-dependent. Five metabolites were found in rat, three in dogs and two in traces in man. After oral application unchanged morocromen is excreted renally by rat, dog and man (14, 18 and 54--64%, respectively). Renal elimination is pH-dependent, but not dependent on sex, dosis and urine volume. Oral bioavailability is approx. 60% in dogs, 67--79% in man. Elimination half-life (blood) is approx. 2 h in dogs, 3--4 hr in man. Organ distribution studies in animals and elimination studies in man (1 to 30 applications) give no hint for accumulation or enzyme induction. Morocromen is distinctly different from carbocromen by a longer biological half-life, by distribution and elimination as mostly unchanged drug and by a better bioavailability.