TABLE 5

Plasma and brain exposure of BIA 9-1079 and tolcapone after intravenous administration (10 mg/kg) to Wistar rats with or without coadministration of elacridar (2.5 mg/kg)

The AUC is expressed in micrograms.hour/gram in brain tissue.

Test CompoundAUC0-tKpKp,uu
VehicleElacridarVehicleElacridarVehicleElacridar
μg.h/mlμg.h/ml
BIA 9-1079
 Plasma32.7137.340.0010.0030.0070.017
 Brain0.0370.095
Tolcapone
 Plasma27.3128.590.0020.0040.0410.095
 Brain0.0500.119
  • AUC0-t, area under the concentration-time curve from time zero to the last measurable concentration; Kp, ratio of total brain-to-plasma AUC0-t; Kp,uu, unbound brain-to-plasma ratio.