Table 3.
Pharmacokinetic parameters of sildenafil and UK-103,320 following administration of single oral doses of sildenafil ranging from 25 to 200 mg (dose-proportionality study). Geometric means are presented for AUC, AUCt and Cmax, arithmetic means are presented for tmax and kel and harmonic means are presented for t1/2. n = 32 per group.
| 25 mg | 50 mg | 100 mg | 200 mg | |
|---|---|---|---|---|
| Sildenafil | ||||
| AUC (ng ml−1 h) | 361* | 738 | 1685 | 3755 |
| AUCt (ng ml−1 h) | 334 | 727 | 1667 | 3702 |
| Cmax (ng ml−1) | 127 | 271 | 560 | 1150 |
| tmax (h) | 1.02 | 0.79 | 0.83 | 0.94 |
| kel (h−1) | 0.26* | 0.23 | 0.19 | 0.18 |
| t1/2 (h) | 2.62 | 2.96 | 3.73 | 3.84 |
| UK-103,320 | ||||
| AUC (ng ml−1 h) | 147* | 328 | 776 | 1822 |
| AUCt (ng ml−1 h) | 134 | 318 | 756 | 1772 |
| Cmax (ng ml−1) | 54 | 126 | 254 | 526 |
| tmax (h) | 0.97 | 0.78 | 0.77 | 0.88 |
| kel (h−1) | 0.24* | 0.20 | 0.15 | 0.14 |
| t1/2 (h) | 2.85* | 3.48 | 4.57 | 4.85 |
n = 30 per group.