Pharmacokinetic parameters of the inhibitors used for DDI simulations
| Inhibitor | Ka | Vd, ss | CLPO | Dose Regimen | Simulated [I]max, ss | Observed [I]max, ss | References |
|---|---|---|---|---|---|---|---|
| h−1 | l/kg | l/h | μg/ml | μg/ml | |||
| DIL | 1.69 | 3.09 | 175.8 | 120 mg t.i.d., 13 days | 0.15 | 0.18 | Abernethy et al., 1991 |
| CLAa | 1.7 | 2.0 | 58.1 | 500 mg b.i.d. 7 days | 1.07 | 2.27 | Calabresi et al., 2004 |
| ERY | 0.26 | 1.27 | 63.6 | 500 mg t.i.d., 7 days | 1.2 | 1.2 | Olkkola et al., 1993 |
| VER | 1.22 | 3.40 | 85.4 | 120 mg t.i.d., 7 days | 0.15 | 0.25 | Murdoch et al., 1991 |
| TAOa | 0.46 | 2.14 | 30.0 | 500 mg Sd | 1.08 | 1.77 | Genazzani, 1975 |
Sd, single dose.
↵a The PK parameters for CLA and TAO were obtained from Rodvold et al. (1999) and Genazzani (1975), respectively, and incorporated into Simcyp for PK simulation.