PMID: 9172951Mar 1, 1997Paper

Metabolism and pharmacokinetics of 1-(2'-trimethylacetoxyethyl)-2-ethyl-3-hydroxypyridin-4-one (CP117) in the rat

Drug Metabolism and Disposition : the Biological Fate of Chemicals
R ChoudhuryS Singh

Abstract

Metabolism and pharmacokinetics of 1-(2'-trimethylacetoxyethyl]-2-ethyl-3-hydroxypyridin-4-one (CP117) were studied in the rat. Urinary recovery studies were conducted in normal (oral and intravenous) and iron-overloaded rats (500 mg Fe/kg body weight; oral only). In normal rats, the majority of the dose recovered in the urine was as the hydrophilic metabolite, CP102, accounting for 69.7 +/- 9.4% (oral) and 80.7 +/- 7.9% (intravenous) of the administered dose. There was, however, a dramatic decrease in the amount of CP102 recovered (47.7 +/- 5.9%) (p < or = 0.05) in the iron-loaded group of animals. The amount of CP102 glucuronide conjugate recovered in the normal and iron-overloaded rats after oral administration of CP117 did not differ significantly with values of 6.5 +/- 2.5% and 7.1 +/- 2.5%, respectively. There was, however, a significant increase in CP102 glucuronide conjugate (13.7 +/- 3.0%) (p < or = 0.05) after intravenous administration of CP117. Urinary iron content was determined in the iron-overloaded and normal (oral) animals. Negligible levels of the CP117 iron complex and only 0.6 +/- 0.2% was present as the corresponding CP102 complex in the urine of normal animals. Less than 0.1% of the administered dose was r...Continue Reading

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