Table 3.
Pharmacokinetic parameters for P218 in healthy subjects following single oral doses
| Dose (mg) | C max (ng/mL) | T max (h) | AUClast (h.ng/mL) | AUCinf (h.ng/mL) | t 1/2 (h) | CL/F (L/h) | Vz/F (L) |
|---|---|---|---|---|---|---|---|
| 10 | 64.33 (58.4) | 1.0 (0.5‐2.0) | 125.97 (27.5) | 129.20 (28.8) | 3.14 (50.9) | 77.40 (28.8) | 350.35 (38.5) |
| 30 | 203.19 (24.2) | 1.0 (1.0‐2.0) | 435.84 (21.2) | 413.35 (16.4) | 6.87 (82.7) | 72.58 (16.4) | 718.98 (74.0) |
| 100 | 929.13 (45.8) | 0.75 (0.5‐2.0) | 1574.05 (24.8) | 1578.35 (27.3) | 17.17 (25.8) | 63.36 (27.3) | 1569.59 (44.2) |
| 250 | 2093.29 (17.5) | 1.0 (0.5‐2.0) | 3904.39 (25.3) | 3924.78 (25.1) | 8.91 (104.7) | 63.70 (25.1) | 818.99 (108.1) |
| 500 | 4158.80 (41.2) | 1.5 (0.5‐2.0) | 7731.40 (33.3) | 7757.98 (33.1) | 12.71 (58.9) | 64.45 (33.1) | 1181.52 (61.1) |
| 750 | 5979.78 (35.2) | 1.0 (0.5‐4.0) | 13403.09 (18.8) | 13568.48 (20.4) | 16.02 (60.3) | 55.28 (20.4) | 1277.11 (81.3) |
| 1000 | 8641.96 (31.1) | 1.0 (1.0‐2.0) | 17608.63 (29.7) | 17814.77 (28.3) | 19.61 (79.1) | 56.13 (28.3) | 1587.73 (89.5) |
C max, AUClast, AUCinf, t 1/2, CL/F and Vz/F are described as geometric mean (CV%); T max is described as median (range).
Abbreviations: AUClast, area under the concentration‐time curve for the sampling period; AUCinf, area under the concentration‐time curve extrapolated to infinity; CL/F, clearance; C max, maximum plasma concentration; CV%, percentage coefficient of variation; t 1/2, terminal half‐life; T max, time to C max; Vz/F, volume of distribution during the terminal phase.