TABLE 4

Radioactive plasma concentration of unchanged drug and its total metabolites after oral administration of[14C]TSU-68 with and without prior oral administration of unlabeled TSU-68 (200 mg/kg/dose)

Each value shown is mean with S.D. (n = 4).




Plasma Concentration (μg or μg-Eq/ml)a

Time
Prior Dosing
Total Metabolites
Unchanged Drug
Concentration Ratio (Metabolites/Unchanged Drug)
2 h (−) 3.3 ± 1.6 17.2 ± 5.5 0.18 ± 0.06
(+) 6.0 ± 2.3 2.8 ± 1.6* 2.41 ± 0.81*
4 h (−) 7.8 ± 1.7 18.5 ± 1.9 0.42 ± 0.07

(+)
9.2 ± 2.6
3.8 ± 2.1*
2.91 ± 1.33*
  • a The total amount of the radioactive metabolites in plasma was expressed as μg-Eq of TSU-68/ml.

  • * Significantly different from value without prior dosing (P < 0.05).