TABLE 1.
Depletion kinetics of THC and 11-OH-THC in pooled human intestinal microsomes.
Data presented are mean ± S.D. of independent experiments (n = 3–5), each conducted in duplicate or triplicate. CLint was calculated as depletion CL/fu,inc.
| THC | 11-OH-THC | |||||
|---|---|---|---|---|---|---|
| Vmax (nmol/min/mg) | Km (nM) | CLinta (ml/min/mg) | Fm | CLint (ml/min/mg) | Fm | |
| CYP2C9 | 1.1 ± 0.38 | 70 (fixed) | 15 ± 5.4 | 0.89 ± 0.31 | NS | NS |
| CYP3A | NA | NA | 2.0 ± 0.86 | 0.11 ± 0.050 | 0.26 ± 0.058 | 0.51 ± 0.11 |
| Total P450 | NA | NA | 17 ± 6.0 | 1.0 ± 0.32 | 0.34 ± 0.080 | 0.67 ± 0.16 |
| UGT2B7 | NA | NA | NS | NS | 0.13 ± 0.027 | 0.25 ± 0.053 |
| Total UGT | NA | NA | NS | NS | 0.17 ± 0.024 | 0.33 ± 0.046 |
NA, not applicable; NS, not significant.
aWhen CYP2C9 was not saturated.