Table 2.
Pharmacokinetic parameters | Dose group (mg) | Relative deviation % | |||||||
---|---|---|---|---|---|---|---|---|---|
1 | 2.5 | 5 | 7.5 | 10 | 15 | 20 | |||
D (mg) | 0.089 | 0.223 | 0.446 | 0.670 | 0.893 | 1.339 | 1.786 | – | – |
t1/2Ka (h) | 5.24 | 4.71 | 4.66 | 5.63 | 5.16 | 5.80 | 5.58 | 5.25 | 6.18% |
t1/2Kel (h) | 40.18 | 44.25 | 43.11 | 41.37 | 41.99 | 39.75 | 39.92 | 41.51 | 3.08% |
Tmax (h) | 17.72 | 17.03 | 16.77 | 18.74 | 17.79 | 18.86 | 18.41 | 18.41 | 0.32% |
Cmax (µg/ml) | 0.11 | 0.29 | 0.60 | 0.98 | 1.29 | 1.84 | 2.67 | – | – |
VCentral (mL) | 574.95 | 584.19 | 563.50 | 500.08 | 515.99 | 487.29 | 485.34 | 530.19 | 6.04% |
R2 | 0.997 | 0.993 | 0.999 | 0.997 | 0.998 | 0.996 | 0.997 | – | – |
Relative deviation = (PK parameters in vitro/PK parameters in vivo—1) * 100%; –, no data.