Concentration of oxycodone HCl metabolites in human liver microsomal samples incubated with 200 µM oxycodone HCl at pH 10
Values are expressed as means ± S.D.
| Human Liver Microsome | Time | Oxycodone | Oxycodone N-Oxide | Noroxycodone | Oxymorphone | Noroxymorphone |
|---|---|---|---|---|---|---|
| min | nmol/ml | (nmol/ml)/mg protein | ||||
| HK37a | 0 | 210.50 ± 1.70 | 0.32 ± 0.001 | 0.42 ± 0.09 | 0.04 ± 0.01 | 0.013 ± 0.018 |
| 10 | 196.70 ± 10.61 | 0.63 ± 0.01 | 5.08 ± 0.18 | 0.97 ± 0.02 | ND | |
| 20 | 205.35 ± 0.64 | 0.70 ± 0.05 | 5.89 ± 0.11 | 1.12 ± 0.06 | 0.09 ± 0.08 | |
| HH18b | 0 | 166.03 ± 4.08 | 0.27 ± 0.05 | 0.45 ± 0.09 | 0.02 ± 0.004 | ND |
| 10 | 170.33 ± 9.08 | 0.37 ± 0.08 | 1.07 ± 0.12 | 0.07 ± 0.004 | ND | |
| 20 | 163.73 ± 6.25 | 0.32 ± 0.001 | 0.42 ± 0.09 | 0.14 ± 0.02 | ND | |
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.
↵b CYP3A4 activity was 12.0 (nmol of product/min)/mg protein in the testosterone 6β-hydroxylase assay. FMO activity was 2.8 (nmol of product/min)/mg protein in the methyl p-tolyl sulfide oxidase assay.