[Pharmacokinetics and metabolism of the antiinflammatory agents S-H 766 in man].
Blood and plasma levels as well as urinary and fecal excretion were measured in humans after oral administration of radioactively labelled 4-[j-(2'-fluorobiphenylyl)]-4-hydroxycrotonic acid (S-H 766 MO). The radioactivity in the plasma reaches maximum values of about 10 mug eq./ml 1 to 2 h after application with either form. After repeated administration good agreement is found between the plasma levels measured and those simulated according to the pharmacokinetic parameters obtained after single application. The S-H 766 metabolites were investigated in blood and urine. The substance was found to undergo considerable metabolism, only approximately 2% being excreted in the urine unchanged. The conjugates, which constitute over 60% of the radioactivity of the urine, consist mainly of glucuronides and sulfates. The structure of the aglycones shows that the metabolism occurs along two pathways, by beta-oxidation of the aliphatic side chain into aryl acetic acids and by hydroxylation of the aromatic nucleus to phenolic compounds. It must be assumed that these biotransformations take place both simultaneously and successively.
D000293:Adolescent; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000378:metabolism*; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000032:analysis / Q000378:metabolism*; D002250:Carbon Radioisotopes; D006207:Half-Life; D006801:Humans; D006885:Hydroxybutyrates / Q000008:administration & dosage / Q000032:analysis / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D009025:Morpholines / Q000008:administration & dosage / Q000032:analysis / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D001713:Biphenyl Compounds; D002250:Carbon Radioisotopes; D006885:Hydroxybutyrates; D009025:Morpholines
Pharmakokinetik und Metabolismus des Antiphlogistikums S-H 766 beim Menschen