TABLE 3

Pharmacokinetic parameters of BIA 9-1079 and tolcapone in plasma and brain after intravenous administration (10 mg/kg) to Wistar rats

The Cmax values are expressed in micrograms/gram and the AUC is expressed in micrograms.hour/gram in brain tissue.

Test CompoundtmaxCmaxAUC0-tAUC0-infAUCextrapKelt1/2elMRT
hμg/mlμg.h/mlμg.h/ml%/hhh
BIA 9-1079
 Plasma0.0352.7884.0884.941.020.135.392.46
 Brain0.080.0960.017NCNC0.661.050.23
Tolcapone
 Plasma0.0367.1236.2436.280.100.511.361.09
 Brain0.030.2050.0560.0571.791.530.450.38
  • AUCextrap, extrapolated area under the concentration-time curve; AUC0-inf, area under the concentration-time curve from time zero to infinite; AUC0-t, area under the concentration-time curve from time zero to the last measurable concentration; Kel, apparent elimination rate constant; MRT, mean residence time; NC, not calculated; t1/2el, apparent terminal elimination half-life; tmax, time to achieve the maximum concentration.