TABLE 9.
Pharmacokinetic parameters of bentysrepinine in a single oral dose (Study 01) and a randomised, open, crossover food-effect study (Study 03).
| Dose (mg) | Cmax (ng/ml) | Tmax (h) | t1/2 (h) | AUC0-t (ng·h/ml) | AUC0-∞ (ng·h/ml) | CL/F (l/h) | V/F (L) |
|---|---|---|---|---|---|---|---|
| Study 01 | |||||||
| 50 | 54.2 (24.5) | 1.50 (0.50–3.00) | 1.7 (1.1) | 106.1 (26.5) | 110.2 (25.1) | 481.1 (148.6) | 1,373.0 (1,441.8) |
| 100 | 127.3 (43.9) | 2.30 (0.50–5.00) | 1.7 (1.1) | 349.0 (83.4) | 354.1 (84.3) | 299.7 (85.8) | 726.2 (269.8) |
| 200 | 356.7 (162.3) | 0.90 (0.50–2.50) | 2.1 (0.7) | 864.2 (209.3) | 870.9 (208.9) | 241.1 (55.1) | 735.3 (344.9) |
| 400 | 921.3 (267.6) | 1.50 (0.50–2.00) | 4.2 (3.2) | 2,232.7 (494.7) | 2,246.0 (494.4) | 185.1 (37.7) | 1,097 (764.5) |
| 600 | 1,395.5 (766.1) | 2.00 (0.75–5.00) | 3.5 (1.4) | 4,002.9 (1,089.4) | 4,056.2 (1,055.2) | 157.6 (43.6) | 771.7 (301.5) |
| 900 | 1712.9 (602.5) | 1.50 (0.75–4.00) | 3.2 (1.4) | 5,115.4 (1,281.1) | 5,151.4 (1,276.8) | 182.8 (38.4) | 854.0 (472.9) |
| Study 03 | |||||||
| 600 (fasted) | 1,126.4 (391.1) | 1.50 (0.66–3.00) | 2.9 (2.0) | 3,312.6 (1,271.5) | 3,330.4 (1,271.8) | 208.4 (88.3) | 845.8 (556.1) |
| 600 (fed) | 1,258.6 (613.2) | 1.75 (1.00–4.00) | 2.6 (1.9) | 3,635.8 (923.8) | 3,652.6 (920.0) | 174.3 (46.0) | 690.0 (638.5) |
The data are expressed as mean (standard deviation, SD).