[Metabolism and pharmacokinetics of etofylline clofibrate, new antilipemic].
Upon investigations on metabolism and pharmacokinetics of 1-(theophyllin-7-yl)-ethyl-2-[2-(chlorophenoxy)-2-methylpropionate] (etofylline clofibrate, ML 1024, Duolip) is reported. As can be seen from in vivo tests in rats and dogs ML 1024 is cleaved to the metabolites clofibric acid and etofylline. This could be further demonstrated in vitro by incubation with lipases and human serum. The pharmacokinetic parameters of the metabolites after oral application of 2 capsules Duolip, corresponding to 500 mg etofylline clofibrate, were evaluated in 7 healthy volunteers. The serum fluctuations of the main metabolites could be adapted to an open two-compartment model (etofylline). The following mean values were found: the invasion half-life is 1 h 4 min for clofibric acid and 1 h 52 min for etofylline. The maximum concentration after approximately 4 h is 22.75 micrograms/ml for clofibric acid and 6.57 micrograms/ml for etofylline. The elimination half-life is 12.12 h for clofibric and 4.33 h for etofylline. Via urine 20 mg clofibric acid and 15.7 mg etofylline were excreted within 8 h. The elimination process after 8 h is not yet terminated.
D000818:Animals; D002994:Clofibrate / Q000031:analogs & derivatives* / Q000378:metabolism; D004285:Dogs; D000960:Hypolipidemic Agents / Q000378:metabolism*; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D007700:Kinetics; D008049:Lipase / Q000378:metabolism; D051381:Rats; D013045:Species Specificity
D000960:Hypolipidemic Agents; C028764:etofylline clofibrate; D008049:Lipase; D002994:Clofibrate
Metabolismus und Pharmakokinetik von Etofyllinclofibrat, einem neuen Antilipmikum.