TABLE 2

Derived kinetic parameters for codeine glucuronidation by human liver microsomes determined in the absence and presence of 2% (w/v) bovine serum albumin

Without BSAa,bWith 2% BSAa,c
KmVmaxCLintdKmVmaxKsiCLintd
mMpmol/min·mgμl/min·mgmMpmol/min·mgmMμl/min·mg
H72.35 ± 0.01440 ± 1.20.190.32 ± 0.01430 ± 9.78.20 ± 1.041.34
H102.68 ± 0.02312 ± 0.90.120.34 ± 0.01303 ± 6.29.49 ± 1.190.89
H123.13 ± 0.18920 ± 20.80.290.28 ± 0.02848 ± 23.814.42 ± 2.783.03
H132.29 ± 0.12754 ± 13.20.330.26 ± 0.001680 ± 0.710.63 ± 0.122.62
H401.16 ± 0.01438 ± 0.50.380.24 ± 0.01447 ± 6.614.46 ± 1.501.86
Mean ± S.D.2.32 ± 0.73573 ± 2530.26 ± 0.110.29 ± 0.04541 ± 21811.44 ± 2.871.95 ± 0.88
Pooled HLM2.15 ± 0.13584 ± 160.270.23 ± 0.01436 ± 128.15 ± 1.031.90
  • a Data presented as mean ± standard error of parameter fit.

  • b Kinetic constants derived from fitting with the Michaelis Menten equation.

  • c Kinetic constants derived from fitting with the substrate inhibition equation.

  • d CLint calculated as Vmax/Km for both Michaelis-Menten and substrate inhibition kinetics.