TABLE 3.
Plasma pharmacokinetic parameters in the single-ascending-dose studya
| Dose (mg) | N | AUC0–t (h·ng/ml) | AUC0–∞ (h·ng/ml) | Cmax (ng/ml) | Tmax (h) | t1/2 (h) | CL/F (ml/h) | VZ/F (ml) |
|---|---|---|---|---|---|---|---|---|
| 50 | 8 | 1,620 ± 540 | 1,710 ± 557 | 124.4258 ± 27.8143 | 3.00 (1.5–6) | 13.096 ± 9.6354 | 32,000 ± 10,100 | 534,000 ± 217,000 |
| 100 | 8b | 2,400 ± 1,080 | 2,310 ± 1,050 | 146.8452 ± 54.1367 | 1.375 (0.50–3.00) | 16.247 ± 10.3146 | 46,200 ± 18,600 | 1,230,000 ± 722,000 |
| 200 | 8 | 4,160 ± 1,590 | 4,370 ± 1,700 | 190.4728 ± 38.8466 | 2.00 (1–4) | 17.146 ± 10.7704 | 52,800 ± 21,600 | 1,160,000 ± 501,000 |
| 300 (fasted) | 16 | 4,570 ± 1,380 | 4,720 ± 1,560 | 244.4718 ± 52.2741 | 1.75 (1.00, 6.00) | 21.927 ± 18.2576 | 69,200 ± 28,700 | 2,160,000 ± 1,430,000 |
| 300 (fed) | 16 | 10,400 ± 2,020 | 10,600 ± 2,280 | 968.2026 ± 143.8727 | 3.00 (1.00, 6.00) | 14.461 ± 13.4291 | 28,900 ± 6,050 | 790,000 ± 979,000 |
| 400 | 8 | 4,620 ± 1,870 | 4,780 ± 2,000 | 257.4554 ± 61.3238 | 1.25 (0.75–3) | 19.399 ± 12.0606 | 96,300 ± 35,200 | 2,540,000 ± 1,610,000 |
| 500 | 8 | 10,700 ± 3,160 | 10,800 ± 3,070 | 990.4379 ± 186.5262 | 2.50 (2–4) | 18.246 ± 14.6804 | 49,400 ± 12,300 | 1,340,000 ± 1,290,000 |
a
Data are expressed as mean ± SD unless otherwise specified. Tmax is expressed as median (range).
b
For subjects with AUC_%Extrap of >20%, AUC0–∞, t1/2, and AUC_%Extrap were not descriptively analyzed. PK parameters, including AUC0–∞, t1/2, and AUC_%Extrap, were descriptively analyzed for 7 subjects in the 100-mg group.