Studies on the Metabolic Fate of Azuletil Sodium (IV):Absorption, Metabolism and Excretion after a Single and Repeated Administration to Dogs.

Abstract

The absorption, metabolism and excretion of ¹⁴C-KT1-32 were studied in dogs after a single oral, intravenous and repeated oral administrations of 1 mg/kg.
1. The radioactivity in the plasma reached a maximum level (3.46μg eq./ml) at 1.93hr after a single oral administration to male dogs.
2. The radioactivities in the plasma declined biexponentially with half-life times of 1.98hr and 39.6hr after a single intravenous administration to male dogs.
3. Within 96hr after a single oral administration, the excretions of radioactivity into urine and feces amounted to 74% and 25% of the administered dose, respectively.
4. In the study with repeated oral administration, the radioactivity in the blood reached the steady state within 24hr after the 3rd administration. The ratios of cumulative excretion into urine and feces were practically constant during the repeated administration. The ratios of the cumulative excreation were 59% in urine and 40% in feces, respectively.
5. The intact drug was found as the major component in plasma, urine and feces after a single oral or intravenous and repeated oral administrations.