Table 2

Pharmacokinetic parameters of [3H]DGX after i.v. administration to rats

Dose of PSC 833
Control0.1 mg/kg0.3 mg/kg3 mg/kg
AUC0–360 min (Fd × min/ml)0.415  ± 0.0220.812  ± 0.0312-160 0.737  ± 0.0472-160 0.868  ± 0.0292-160
Xliver,360 min (Fd/g liver)0.00563  ± 0.001150.00918  ± 0.000990.011  ± 0.0032-150 0.013  ± 0.0022-160
Xbile,0–360 min (Fd)0.309  ± 0.0240.0986  ± 0.00852-160 0.109  ± 0.0172-160 0.108  ± 0.0132-160
Xurine,0–360 min (Fd)0.112  ± 0.0200.104  ± 0.0370.184  ± 0.0580.168  ± 0.043
CLbile (ml/min/kg)3.03  ± 0.350.486  ± 0.0382-160 0.595  ± 0.0852-160 0.506  ± 0.0812-160
CLR (ml/min/kg)1.12  ± 0.240.516  ± 0.1840.961  ± 0.2860.768  ± 0.188

[3H]DGX was administered i.v. to rats that had received an i.v. injection of PSC 833 (0, 0.1, 0.3, and 3 mg/kg) 30 min before the experiments. Amount of [3H]DGX in the plasma, bile, and urine specimens was determined with HPLC. The plasma concentration-time profiles of [3H]DGX are shown in Fig. 2. Kinetic parameters were calculated as described in the text. Xliver represents the fraction of administered dose (Fd) associated with 1 g liver at 6 h after administration. Results are given as the mean ± S.E. of four independent experiments.

  • 2-150P < .05, significantly different from control, using Fisher’s t test.

  • 2-160P < .01, significantly different from control, using Fisher’s t test.