Table II.
Predicted Mean PK Parameters of Compound C from Tablets Manufactured Using API with Four Different Particle Size Distributions, Under Fasted Condition. The Ratio of the PK Parameters for Each Particle Size as Compared to the Phase I Suspension are Shown in Parenthesis
| 200 mg | 400 mg | 800 mg | |||||||
|---|---|---|---|---|---|---|---|---|---|
| AUC (μg×h/mL) | C max (μg/mL) | C 12 h (μg/mL) | AUC (μg×h/mL) | C max (μg/mL) | C 12 h (μg/mL) | AUC (μg×h/mL) | C max (μg/mL) | C 12 h (μg/mL) | |
| Phase I suspension (35 μm) | 2.12 | 0.87 | 0.011 | 6.26 | 1.49 | 0.018 | 9.32 | 2.79 | 0.026 |
| 23 μm | 3.18 (1.5) |
0.98 (1.1) |
0.012 (1.1) |
6.39 (1.0) |
1.67 (1.1) |
0.019 (1.1) |
12.00 (1.3) |
2.75 (0.9) |
0.028 (1.1) |
| 43 μm | 2.91 (1.4) |
0.90 (1.0) |
0.011 (1.0) |
5.76 (0.9) |
1.54 (1.0) |
0.019 (1.1) |
10.40 (1.1) |
2.39 (0.9) |
0.028 (1.1) |
| 57 μm | 2.83 (1.3) |
0.88 (1.0) |
0.010 (0.9) |
5.62 (0.9) |
1.50 (1.0) |
0.018 (1.0) |
9.72 (1.0) |
2.21 (0.8) |
0.027 (1.0) |
| 85 μm | 2.32 (1.1) |
0.76 (0.9) |
0.010 (0.9) |
4.97 (0.8) |
1.25 (0.8) |
0.016 (0.9) |
7.29 (0.8) |
1.64 (0.6) |
0.025 (0.9) |
AUC area under the curve