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 HK37a | Time | Oxycodone | Oxycodone N-Oxide | Noroxycodone | Oxymorphone | Noroxymorphone |
|---|---|---|---|---|---|---|
| min | nmol/ml | (nmol/ml)/mg protein | ||||
| No heat treatment | 0 | 165.48 ± 13.54 | 0.21 ± 0.02 | 0.09 ± 0.01 | 0.01 ± 0.05 | ND |
| 20 | 153.48 ± 11.54 | 0.23 ± 0.04 | 1.47 ± 0.17 | 0.69 ± 0.04 | ND | |
| Heat treated | 0 | 160.28 ± 2.27 | 0.10 ± 0.02 | 0.04 ± 0.01 | 0.02 ± 0.01 | ND |
| 20 | 159.78 ± 5.50 | 0.15 ± 0.03 | 0.44 ± 0.04 | 0.26 ± 0.01 | 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.