Concentration of oxycodone metabolites in human liver microsomal (Lot HH18) samples incubated with 200 µM oxycodone HCl at pH 7.4
Values are expressed as means ± S.D.
| Human Liver Microsome HH18a | Time | Oxycodone | Oxycodone N-Oxide | Noroxycodone | Oxymorphone | Noroxymorphone |
|---|---|---|---|---|---|---|
| min | nmol/ml | (nmol/ml)/mg protein | ||||
| No heat treatment | 0 | 176.90 ± 4.88 | 0.18 ± 0.009 | 0.45 ± 0.04 | 0.02 ± 0.001 | ND |
| 20 | 135.45 ± 4.32 | 0.87 ± 0.036 | 8.08 ± 0.36 | 0.28 ± 0.004 | ND | |
| Heat treated | 0 | 155.95 ± 7.04 | 0.11 ± 0.006 | 0.14 ± 0.01 | 0.01 ± 0.040 | ND |
| 20 | 16.21 ± 1.14 | 0.42 ± 0.033 | 4.17 ± 0.42 | 0.16 ± 0.012 | ND | |
ND, not detected.
↵a 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.