1991 Volume 6 Issue 4 Pages 637-653
The absorption, distribution, metabolism and excretion of Oxiracetam (CT-848) were studied in rats after single administration of 14C-CT-848.
1. After oral administration of 10mg/kg of 14C-CT-848 to male rats, the plasma concentration of radioactivity reached Cmax 2hr after dosing and decreased rapidly with half-lives of 1.2hr (4 ?? 8 hr) and 3.6hr (8 ?? 12hr).
2. The plasma pharmacokinetics was not directly dose-proportional after oral administration with 10mg/kg, 50mg/kg and 250mg/kg. They were also slightly altered by food (Tmax : 1 hr, T1/2 : 2.5hr, 4.4hr) but did not differ between the sexes. μ3. Radioactivity was distributed in all tissues, especially in the gastroin testinal tract, bladder and kidney but only low levels were found in the cen tral nervous system.
4. Radioactivity was rapidly excreted predominantly via the kidney and elimination was almost completed within 24hr after dosing.
5. After oral administration to fasted male rats, only unchanged compound was observed in the plasma. In urine and feces up to 24hr the radioac tivity almost corresponded with unchanged compound and about 1 % of the radioactivity were unknown metabolites.
