Day 1 | Day 28 | |||||
---|---|---|---|---|---|---|
50 mg n = 8 | 100 mg n = 8 | 200 mg n = 8 | 50 mg n = 8 | 100 mg n = 8 | 200 mg n = 8 | |
aTmax (h) | 2.0 (2.0, 3.0) | 3.0 (2.0, 4.0) | 3.0 (2.0, 3.0) | 2.5 (2.0, 3.0) | 3.0 (2.0, 4.0) | 3.0 (2.0, 4.0) |
Cmax (ng/mL) | 1344.1 ± 498.2 | 2770.1 ± 652.5 | 4389.8 ± 1950.4 | 1752.3 ± 815.2 | 3398.7 ± 611.3 | 5330.6 ± 1656.4 |
t1/2 (h)b | 13.0 ± 1.9 | 12.1 ± 3.7 | 15.6 ± 2.3 | |||
AUC0-24 h (h·ng/mL) | 11,732.9 ± 4933.2 | 28,447.1 ± 9350.9 | 50,875.4 ± 25,750.5 | 18,134.1 ± 9665.9 | 42,115.1 ± 9863.1 | 73,897.0 ± 29,108.4 |
AUC0-t (h·ng/mL) | 11,701.1 ± 4915.6 | 28,356.5 ± 9307.9 | 50,671.4 ± 25,634.8 | 24,716.5 ± 15,157.2 | 57,807.0 ± 16,630.8 | 114,031.6 ± 51,939.3 |
AUC0-∞ (h·ng/mL)b | 25,625.6 ± 15,804.7 | 59,399.0 ± 18,159.0 | 120,090.0 ± 57,318.9 | |||
CL/F (L/h)b | 3.4 ± 1.5 | 2.5 ± 0.6 | 3.3 ± 2.0 | |||
Vz/F (L)b | 61.4 ± 23.0 | 42.3 ± 10.9 | 73.6 ± 43.4 | |||
Ctrough (ng/mL) | 289.8 ± 220.7 | 722.8 ± 256.6 | 1797.7 ± 933.9 | |||
degree of fluctuation (%) | 203.5 ± 34.2 | 155.8 ± 21.9 | 121.8 ± 33.0 | |||
RACAUC0-24 h | 1.65 ± 0.85 | 1.56 ± 0.45 | 1.99 ± 1.81 | |||
RACCmax | 1.44 ± 0.85 | 1.26 ± 0.29 | 1.52 ± 1.12 |