Table 3

Prediction of intestinal and hepatic first-pass metabolism rate of indinavir in control and dexamethasone-treated rats (mean ± SD)

TreatmentIntestineLiver
Intrinsic Clearance (Vmax/KM) (ml/min/kg)Predicted Extraction RatioObserved Extraction Ratio3-aIntrinsic Clearance (Vmax/KM) (ml/min/kg)Predicted Extraction RatioObserved Extraction Ratio3-b
Control0.50  ± 0.140.0098  ± 0.00280.06  ± 0.09166  ± 750.45  ± 0.100.65  ± 0.19
Dexamethasone-treated1.87  ± 1.00.036  ± 0.020.34  ± 0.131403  ± 930.87  ± 0.0080.82  ± 0.18
  • 3-a The intestinal first-pass extraction ratio was determined using the in situ intestinal loop technique.

  • 3-b The hepatic first-pass extraction ratio was determined by comparing the drug concentrations in the systemic circulation during portal and femoral vein infusions of indinavir.