Biliary excretion of furosemide glucoronide in rabbits

Article abstract of DOI:10.1248/bpb.18.447

Furosemide (F) was administered to rabbits intravenously and intraduodenaly and the biliary excretion was studied. The major metabolite excreted in bile was furosemide glucuronide (FG). P and acyl migration isomers of FG (FG-iso) were also excreted in bile. The biliary excretion rates of total F (F+ PG+FG-iso) following intraduodenal administration of F were much smaller than those following intravenous administration. The fraction of (F+PG-iso) in bile following intraduodenal administration of F were larger than those following intravenous administration. Stability of PG or FG-iso in bile and supernatant solution of the duodenum homogenate of rabbits was studied. FG was unstable in both media and its degradation followed apparent first-order kinetics in both media. In bile, PG degraded to produce several FG-iso and F, while in the supernatant solution of the duodenum homogenate, it hydrolyzed immediately to F. FG-iso were hardly detected in the supernatant solution. These results indicated that FG excreted in bile degraded easily to FG-iso and F. FG might easily hydrolyze to F enzymatically in the duodenum, and the resultant F might be reabsorbed from the intestinal tract. Unabsorbed PG-iso and P might be excreted in the feces.

Full text of DOI:10.1248/bpb.18.447

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