TABLE 1

Derived kinetic parameters of R- and S-lorazepam glucuronidation by human liver microsomes

Data are modeled using the substrate inhibition equation.

R-LorazepamS-Lorazepam
LiverKm VmaxKsi CLinta Km Vmax Ksi CLinta
µMpmol/min/mg proteinµMµl/min/mgµMpmol/min/mg proteinµMµl/min/mg
H7325.94080.18395.04470.13
H10175.04240.29249.33810.39
H12389.93950.2643133030.30
H13407.12520.18518.72290.17
H40229.13580.4125163950.64
Mean ± S.D.29 ± 8.97.4 ± 1.9367 ± 620.26 ± 0.0836 ± 10*10 ± 3.8351 ± 760.33 ± 0.18
Pooled HLM377.62630.2137103540.27
  • a CLint calculated as Vmax/Km.

  • * P < 0.05.