Evaluation of orally administered activated charcoal on intestinal dialysis of intravenously administered M79175, an aldose reductase inhibitor, in rats.
The effect of oral administration of activated charcoal on serum elimination of 14C-M79175 injected intravenously in rats was studied. In situ single-pass perfusion studies showed that M79175 and/or its metabolites was transported into the small intestinal lumen. Total radioactivity expressed as equivalents of M79175 exsorbed in the perfusate and excreted in the bile juice was 3.2% and 2.0%, respectively, of dose. Oral administration of multiple doses of activated charcoal significantly decreased the serum concentration and serum half-life of 14C-M79175. The fecal excretion of 14C-M79175 after treatment with activated charcoal was increased when compared to that in the control. On the other hand, urinary excretion of 14C-M79175 after treatment with activated charcoal was decreased. However, there was no significant difference in the cumulative amounts of total excretion (fecal plus urinary excretion) between rats with activated charcoal treatment and rats without charcoal treatment. These results suggest that intestinal dialysis by oral activated charcoal is a reasonable method to enhance the elimination of M79175 from the serum in case of overdose of the drug.
D000284:Administration, Oral; D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D001692:Biological Transport; D002606:Charcoal / Q000008:administration & dosage / Q000494:pharmacology*; D007093:Imidazoles / Q000493:pharmacokinetics*; D048289:Imidazolidines; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D008657:Metabolic Clearance Rate; D051381:Rats; D011919:Rats, Inbred Strains; D013401:Sugar Alcohol Dehydrogenases / Q000037:antagonists & inhibitors*
D007093:Imidazoles; D048289:Imidazolidines; D002606:Charcoal; C037070:M 79175; D013401:Sugar Alcohol Dehydrogenases; D000449:Aldehyde Reductase