TABLE 1

Pharmacokinetic parameter estimates of S 55746 in all studies after single and repeated administration

Parameters (Unit)DefinitionEstimates (RSE%)IIV% (RSE%)
FBioavailability0.542 (7.27)31.3 (40.2)
VMA (mg⋅h−1⋅kg−1)Maximum rate of absorption41.7 (14.2)
KMA (mg⋅kg−1)Drug amount corresponding to 50% of maximum rate of absorption11.4 (31.8)
Vc (l⋅kg−1)Volume of distribution of the central compartment1.18 (7.97)24.9 (63.9)
Km (ng⋅ml−1)Drug concentration corresponding to 50% of maximum rate of elimination654 (28.9)75.8 (26.1)
Vm0 (mg⋅h−1⋅kg−1)Maximum rate of elimination3.79 (13.3)
k26 (h−1)First-order distribution rate constants0.470 (17.1)
k62 (h−1)First-order distribution rate constants0.480 (8.33)
kel (h−1)First-order enzyme degradation rate constant0.00789 (125)
EmaxMaximum capacity for enzyme production stimulation4.33 (66.5)
E50 (ng⋅ml−1)Drug concentration corresponding to 50% stimulation of enzyme production3745 (185)
εmultMultiplicative component of the residual error0.325 (5.75)
εadd (ng⋅ml−1)Additive component of the residual error0.674 (15.3)
  • IIV%, interindividual variability expressed in percentage; RSE%, relative standard error computed as the ratio between the S.E. and the parameter estimate multiplied by 100.