Table 4

Estimation of PBPK parameters in humans using the allometric scaling method and M1/P ratio calculation based on the static model.

ParametersDS-1971aM1SourceStatic modelPBPK model
Molecular weight465481XX
Plasma distribution volume at steady state: Vdssa (L/kg)0.15a0.10aAllometrya
DetailBlood-based extrahepatic distribution volume: V1pb or V1mb (L)13b9.8bCalculatedbX
Liver volume: Vh (L)1.7Reported (Davies and Morris, 1993)X
Liver to plasma ratio: Kp3.21.1MeasuredX
fCL,m (ratio)0.50Calculated (Table 3)XX
Total plasma clearance: cCLp,total or cCLm,total (ml/min/kg)4.4c2.6cAllometrycX
DetailMetabolic plasma clearance: CLmpc or CLmmc (ml/min/kg)4.3c0.0cXX
Biliary plasma clearance: CLbpc or CLbmc (ml/min/kg)0.059c1.0cXX
Renal plasma clearance: CLrpc or CLrmc (ml/min/kg)0.030c1.6cX
Hepatic availability: Fh,pd or Fh,me0.62d0.92eCalculatedd,eX
Plasma M1/P ratio f by static model1.3 fCalculated fX
  • X, used.

  • aEq. (9).

  • bEq. (31).

  • cEq. (8).

  • dEq. (10).

  • eEq. (11).

  • fEq. (13).