[On pharacokinetics and metabolism of the choleretic agent febuprol (author's transl)].
The pharmacokinetic behaviour as well as metabolization of 3-butoxy - 1 - phenoxy-propanol-(2) (febuprol) in rats and mice were studied. In addition, binding on human protein and in vitro absorption were determined. The distribution of tritium labelled Febuprol in the body after oral administration was studied in rats and mice: the product was found to circulate in enterohepatic circulation, including the intestines, liver and kidney, and, in the case of mice, also the gall bladder, whereas other organs or tissues show no activity. Upon oral adminstration over 90% Febuprol are absorbed via gastro-intestinal tract and as metabolites 85% of the substance were eliminated via bile, 4% via urine. The rate of metabolisation is high. Via bile only 0.2%, via urine only 0.6% unaltered Febuprol are excreted. Mainly conjugated Febuprol and hydroxy-Febuprol are found as metabolites. By means of the Sartorius absorption model Febuprol yeilded a rate constant common to pharmaceutical substances which are absorbed at a medium rate. This constant does not depend on the pH-range. The buccal tests and the distribution coefficients show the same results.
D000433:1-Propanol / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001711:Biotransformation; D002756:Cholagogues and Choleretics / Q000378:metabolism*; D004764:Enterohepatic Circulation; D005260:Female; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D008567:Membranes, Artificial; D008954:Models, Biological; D020005:Propanols; D011485:Protein Binding; D051381:Rats; D012709:Serum Albumin / Q000378:metabolism
D002756:Cholagogues and Choleretics; D008567:Membranes, Artificial; D020005:Propanols; D012709:Serum Albumin; D000433:1-Propanol
Zu Pharmakokinetik und Metabolismus des Choleretikums Febuprol