TABLE 1

Kinetics of phenytoin hydroxylation by HLM- and E. coli-expressed CYP2C9 in the presence and absence of 2% albumin Units: HLM, Km, micromolar; Vmax, picomoles per minute per milligram; CLint, microliters per minute per milligram. E. coli-expressed CYP2C9: Km, micromolar; Vmax, picomoles per minute per picomole of P450; CLint, microliters per minute per milligram. CLint.liver, liters per hour.


Enzyme Source

Parameter

No Albumin

BSA

HSA-FAF

HSA
HLM K m 20.8 ± 1.5 4.7 ± 0.3* 4.7 ± 0.2* 26.5 ± 1.0*
V max 17.8 ± 0.3 20.2 ± 0.5* 20.7 ± 0.8* 17.4 ± 0.3
CLint 0.86 ± 0.05 4.3 ± 0.3* 4.5 ± 0.1* 0.66 ± 0.02*
CLint.liver 2.93 ± 0.16 14.85 ± 0.87* 15.39 ± 0.32* 2.25 ± 0.07*
CYP2C9 K m 14.4 ± 1.3 3.6 ± 0.2* 4.1 ± 0.2* 14.7 ± 0.1
V max 0.230 ± 0.006 0.246 ± 0.001* 0.249 ± 0.004* 0.236 ± 0.003
CLint 1.17 ± 0.07 4.99 ± 0.22* 4.49 ± 0.13* 1.17 ± 0.02

CLint.liver
4.01 ± 0.24
17.06 ± 0.75*
15.36 ± 0.43*
3.99 ± 0.06
  • * Significantly different (p < 0.05) from control value (determined in the absence of albumin)