Table 3.
Dose (mg) | Day | Pharmacokinetic Parameters
|
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---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tmax (hours)
|
Cmax (ng/mL)
|
Vz/F (L)
|
Cls/F (L/h)
|
T1/2,z (hours)
|
AUC (ng · h/mL)
|
Css,min (ng/mL)
|
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Median | Range | No. | Mean | SD | No. | Mean | SD | No. | Mean | SD | No. | Mean | SD | No. | Mean | SD | No. | Mean | SD | No. | ||
2 | 1 | 2.02 | 1.98-3.00 | 4 | 7.0 | 2.7* | 4 | 354.7 | 371.5 | 2 | 29.0 | 30.6 | 2 | 11.13 | 3.15 | 4 | 65.3 | 69.1* | 2 | 6.6 | 6.6 | 4 |
2 | 28 | 2.00 | 1.07-4.05 | 3 | 9.2 | 1.8* | 3 | 277.5 | 473.2 | 2 | 16.3 | 0.8 | 3 | 11.23 | 1 | 122.7 | 5.6* | 3 | ||||
3 | 1 | 2.00 | 1.00-3.92 | 3 | 8.2 | 2.4* | 3 | 231.9 | 1 | 17.5 | 1 | 9.20 | 16.57 | 2 | 171.6* | 1 | 7.3 | 2.8 | 3 | |||
3 | 28 | 1.93 | 1.00-2.00 | 3 | 19.3 | 5.6* | 3 | 541.5 | 228.4 | 3 | 13.1 | 5.1 | 3 | 29.04 | 9.92 | 3 | 254.1 | 98.7* | 3 | |||
6 | 1 | 2.00 | 1.00-6.00 | 9 | 21.3 | 8.1* | 9 | 356.1 | 33.8 | 3 | 22.3 | 2.6 | 3 | 14.46 | 3.11 | 9 | 272.1 | 33.2* | 3 | 12.7 | 7.1 | 9 |
6 | 28 | 1.98 | 1.00-5.12 | 9 | 27.6 | 15.0* | 9 | 562.5 | 367.6 | 3 | 20.5 | 14.7 | 9 | 28.52 | 8.19 | 3 | 445.2 | 318.1* | 9 | |||
9 | 1 | 2.00 | 1.00-2.08 | 5 | 28.4 | 13.1* | 5 | 173.8 | 1 | 38.2 | 1 | 11.44 | 6.05 | 4 | 235.7* | 1 | 23.6 | 7.4 | 5 | |||
9 | 28 | 2.00 | 4.00 | 2 | 37.9 | 50.8* | 2 | 217.3 | 395.4 | 2 | 12.3 | 15.2 | 2 | 12.21 | 18.05 | 2 | 592.7 | 729.5* | 2 | |||
All | 1 | 2.00 | 1.00-6.00 | 21 | 314.3 | 80.6 | 7 | 26.0 | 7.1 | 7 | 12.95* | 3.99 | 19 | |||||||||
28 | 2.00 | 1.00-8.08 | 18 | 467.6 | 240.8 | 10 | 17.7 | 11.1 | 17 | 23.79* | 10.03 | 9 |
NOTE. When n ≤ 2, individual values are reported. AUCinf is reported for all dose levels for day 1; AUC0-24 hours is reported for all dose levels for day 28.
Abbreviations: AUC, area under the concentration-time curve; Cmax, maximal plasma concentration; Cls/F, apparent systemic clearance; Css,min, steady state plasma concentration at trough; NR, not reportable; Tmax, time of the maximal plasma concentration; T1/2,z, terminal half-life; Vz/F, apparent volume of distribution; SD, standard deviation.
P < .05 using a Wilcoxon matched pairs signed-rank test.