Table III.
Comparison of Predicted vs. Observed Mean Plasma PK Parameters
| Parameters | Suspension | IR tablet | XR tablet | XR capsule | |||||
|---|---|---|---|---|---|---|---|---|---|
| Obs. | Pred. | Obs. | Pred. | Obs. | Pred. | Obs. | Pred. | ||
| Dose (mg) | 200 | 400 | 400 | 300 | |||||
| C max (ng/mL) | Fasted | 3066.7 | 2914.6 | 3610.1 | 3713.7 | 3005.2 | 3105.2 | 2066.1 | 2120.8 |
| Fed | 2580.0 | 2506.9 | 5920.0 | 5501.2 | 3329.9 | 3786.6 | 2661.9 | 2798.5 | |
| AUCt (μg × h/mL) | Fasted | 166.6 | 163.3 | 279.8 | 301.6 | 270.4 | 263.7 | 194.3 | 190.2 |
| Fed | 165.2 | 152.9 | 401.3 | 348.6 | 286.1 | 288.6 | 221.1 | 222.2 | |
| AUCinf (μg × h/mL) | Fasted | 179.8 | 177.3 | 298.6 | 330.0 | 285.8 | 272.2 | 226.4 | 203.8 |
| Fed | 180.7 | 166.2 | 444.9 | 379.3 | 304.7 | 297.5 | 246.7 | 237.0 | |
| T max (hr) | Fasted | 1 | 1.45 | 24 | 16 | 24 | 28.9 | 26 | 20.98 |
| Fed | 4 | 3.66 | 12 | 4.8 | 24 | 16.4 | 15 | 17.8 | |
| POT20 (hr) | Fasted | [0.6,8.5] | [0.8,10] | [3.7,41] | [2.9,40] | [10,42] | [13,44] | [8.2,54] | [8.9,48] |
| Fed | [1.1,16] | [1.4,16] | [3.5,28] | [2.3,19] | [8.1,42] | [10,34] | [7.3,44] | [8.8, 39] | |
| F a (%) | Fasted | N.A. | 99.9 | N.A. | 93.0 | N.A. | 71.6 | N.A. | 76.6 |
| Fed | N.A. | 99.9 | N.A. | 99.8 | N.A. | 78.2 | N.A. | 89.0 | |
| Correlation coefficient (R 2) | Fasted | 0.956 | 0.975 | 0.974 | 0.977 | ||||
| Fed | 0.940 | 0.876 | 0.954 | 0.991 | |||||
POT 20 peak occupancy time, time span over which the concentration is within 20% of C max; F a fraction absorbed; N.A. not available