Table I.
PK parameters | Oral administration | Intravenous administration | ||
---|---|---|---|---|
Male (n = 5) | Female (n = 5) | Male (n = 5) | Female (n = 5) | |
C max (ng/mL) | 51.1 ± 9.3 | 4.33 ± 1.37** | 8.81 ± 1.81 | 13.7 ± 5.7 |
AUC0–t (min μg/mL) | 52.6 ± 20.5 | 2.71 ± 0.86** | 0.460 ± 0.080 | 0.581 ± 0.179 |
AUC0–∞ (min μg/mL) | 53.5 ± 20.9 | 2.74 ± 0.91** | 0.594 ± 0.083 | 0.745 ± 0.339 |
t 1/2 (min) | 493 ± 130 | 219 ± 148* | 68.6 ± 15.5 | 53.2 ± 27.1 |
MRT (min) | 833 ± 214 | 494 ± 109** | 92.2 ± 20.4 | 72.8 ± 28.6 |
CL/F (mL/min) | 95.4 ± 3.0 | 1529 ± 425** | 19.8 ± 3.1 | 17.5 ± 5.8 |
CLrenal a (mL/min) | 0.343 ± 0.194 | 1.66 ± 0.39** | 0.158 ± 0.040 | 0.126 ± 0.032 |
*p < 0.05, significant difference; **p < 0.01, highly significant difference (vs. the same route of administration for male rats).
aCalculated by the cumulative amount of parent drug in urine (X u) vs. AUC0–∞ of parent drug.