TABLE 5

Concentration of oxycodone metabolites in human liver microsomal (Lot HK37) samples incubated with 200 μM oxycodone HCl at pH 7.4

Values are expressed as means ± S.D.

Human Liver Microsome HK37aTimeOxycodoneOxycodone N-OxideNoroxycodoneOxymorphoneNoroxymorphone
minnmol/ml(nmol/ml)/mg protein
No heat treatment0165.48 ± 13.540.21 ± 0.020.09 ± 0.010.01 ± 0.05ND
20153.48 ± 11.540.23 ± 0.041.47 ± 0.170.69 ± 0.04ND
Heat treated0160.28 ± 2.270.10 ± 0.020.04 ± 0.010.02 ± 0.01ND
20159.78 ± 5.500.15 ± 0.030.44 ± 0.040.26 ± 0.01ND
  • ND, not detected.

  • a CYP3A4 activity was 2.5 (nmol of product/min)/mg protein in the testosterone 6β-hydroxylase assay. FMO activity was 3.6 (nmol of product/min)/mg protein in the methyl p-tolyl sulfide oxidase assay.