Table 1.
Midazolam and 1-hydroxy midazolam pharmacokinetic parametersa
| Pharmacokinetic parameters | Mean ± SD (n) |
|
|---|---|---|
| Treatment A (reference): midazolam alone | Treatment B (test): midazolam + PA-824 | |
| Midazolam | ||
| Cmax (ng/ml) | 11.9 ± 5.46 (14) | 9.64 ± 3.43 (14) |
| AUC0–t (ng · h/ml) | 30.7 ± 15.3 (14) | 25.3 ± 10.50 (14) |
| AUC0–∞ (ng · h/ml) | 32.1 ± 15.7 (14) | 25.0 ± 9.56 (13) |
| CL/F (liters/h) | 75.8 ± 32.0 (14) | 91.5 ± 36.2 |
| Tmax (h) | 0.505 (0.499–1.00) (14) | 1.00 (0.499–1.00) (14) |
| t1/2 (h) | 5.69 ± 2.14 (14) | 5.44 ± 2.4400 (13) |
| 1-Hydroxy midazolam | ||
| Cmax (ng/ml) | 5.32 ± 2.48 (14) | 5.42 ± 2.17 (14) |
| AUC0–t (ng · h/ml) | 12.0 ± 5.23 (14) | 13.7 ± 6.24 (14) |
| AUC0–∞ (ng · h/ml) | 12.9 ± 5.82 (13) | 14.6 ± 7.73 (10) |
| Tmax (h) | 0.505 (0.499–1.00) (14) | 1.00 (0.499–1.00) (14) |
| t1/2 (h) | 4.09 ± 2.16 (13) | 4.45 ± 2.87 (10) |
a
Tmax results are presented as the “median (range)”. Other values are arithmetic means ± the standard deviations. n, number of subjects contributing data; Cmax, maximum observed concentration; Tmax, time at which Cmax occurs; t1/2, elimination half-life; AUC0–t, area under the concentration-time curve during the dosing interval; AUC0–∞, area under the concentration-time curve extrapolated to infinity.