Etofenamate [2-(2-hydroxyethoxy)ethyl-N-(alpha, alpha, alpha-trifluoro-m-tolyl)-anthranilate] was administered to dogs by the oral route. Minor amounts of etofenamate (Eto) and its glucuronide were found in urine and feces. The main portion of metabolites was eliminated as flufenamic acid (Flu) and hydroxy derivatives of Eto and Flu. Furthermore, a highly lipophilic fraction was isolated (extraction and TLC) and further separated into several compounds (HPLC, GLC). These metabolites were identified as Eto oleate, palmitate, linoleate, stearate, palmitoleate, myristate, and laurate by NMR and MS. The structures were confirmed by comparison with authentic material. The conjugation of etofenamate with fatty acids is an example of a new route of drug metabolism.

Administration, Oral↗

PubMedDate not supplied

[Tissue concentrations of non-steroidal anti-inflammatory agents in chronic polyarthritis patients].

Non-steroidal antiinflammatory drugs (NSAID) are indispensable for modern treatment of rheumatoid arthritis. Reports on drug concentration in rheumatoid human tissues are still lacking. We now report about steady-state concentrations of Indomethacin and Acemetacin in blood, synovial fluid, synovial membrane, muscle, bone and fat 6h after the last application of Acemetacin resp. Indomethacin. Levels in all tissues, except fat, were found to be significantly higher than in blood. Therefore, a noticeable accumulation of drug occurs in all rheumatoid tissues.

Arthritis, Rheumatoid↗