TABLE 1.
Pharmacokinetic parameters of BAL4815 estimated after single oral administration or intravenous infusion of prodrug BAL8557a
| Parameter | Doseb
|
|||||
|---|---|---|---|---|---|---|
| Oral administration
|
Intravenous infusion
|
|||||
| 100 mg (n = 6) | 200 mg (n = 6) | 400 mg (n = 3) | 50 mg (n = 6) | 100 mg (n = 6) | 200 mg (n = 6) | |
| AUC0-∞ (μg·h/ml) | 37.0 (±6.75) | 78.5 (±10.8) | 215 (±42.0) | 11.3 (±4.43) | 26.6 (±6.25) | 73.2 (±12.4) |
| AUClast (μg·h/ml) | 36.5 (±6.70) | 77.7 (±11.0) | 214 (±41.9) | 10.5 (±4.04) | 24.9 (±5.92) | 72.2 (±12.1) |
| Cmax (μg/ml) | 1.45 (±0.177) | 2.59 (±0.449) | 5.57 (±0.212) | 0.446 (±0.076) | 1.03 (±0.184) | 2.47 (±0.374) |
| Tmax (h) | 2.0 (1.6-2.0) | 1.8 (1.5-3.0) | 3.0 (2.1-3.0) | 0.75 (0.5-1.0) | 1.0 (0.75-1.0) | 1.0 (0.75-1.0) |
| t1/2αc (h) | 1.70 (±0.34) | 2.05 (±0.53) | 2.06 (±0.59) | 1.57 (±0.52) | 1.53 (±0.59) | 0.42 (±0.31) |
| t1/2β (h) | 63.1 (±21.7) | 77.1 (±12.8) | 56.0 (±2.49) | 76.2 (±32.0) | 104 (±56.7) | 80.4 (±33.0) |
| Vd (liters) | 248 (±80.4) | 292 (±80.8) | 155 (±39.2) | 444 (±175) | 494 (±280) | 304 (±86.6) |
| CLSd (liters/h) | 2.80 (±0.548) | 2.59 (±0.363) | 1.91 (±0.418) | 5.03 (±1.99) | 3.96 (±1.04) | 2.80 (±0.519) |
a
Results are from a noncompartmental analysis except where indicated. Values are presented as arithmetic means plus or minus SD; median and range are listed for Tmax.
b
Dose corresponds to mg equivalents of BAL4815.
c
Obtained by two-compartmental analysis.
d
V corresponds to VZ/F after oral administration and to VSS after intravenous infusion; CLS corresponds to CLS/F after oral administration.