Parameter | Radioactivity in Blood | Radioactivity in Plasma | Linezolid | PNU-142586 | PNU-142300 |
---|---|---|---|---|---|
AUC0–∞ 5-a | 89.9 ± 33.6 | 117 ± 34.5 | 101 ± 41.4 | 21.0 ± 6.95 | 7.29 ± 0.64 |
C max 5-a | 10.4 ± 2.04 | 11.9 ± 2.40 | 12.7 ± 2.55 | 1.71 ± 0.75 | 0.76 ± 0.21 |
T max (h) | 0.893 ± 0.497 | 0.893 ± 0.497 | 0.93 ± 0.45 | 5.43 ± 0.98 | 2.71 ± 0.76 |
t 1/2 (h) | 5.37 ± 1.54 | 11.03 ± 7.27 | 6.13 ± 2.32 | 5.39 ± 1.36 | 8.07 ± 8.89 |
V z(liter) | 47.1 ± 16.4 | ||||
CL/F (ml/min)5-b | 96.4 ± 35.8 | ||||
CLw/F (ml/min/kg)5-b | 1.32 ± 0.42 | ||||
CLr/F (ml/min/kg)5-b 5-c | 0.51 ± 0.09 |
Male-female differences (p < 0.05) were observed with higher linezolid AUC and Cmax, and lower PNU-142586 AUC and Cmax in the single-dose female group. This difference was not present in the steady-state group. Accordingly, regimen based differences (p < 0.05) for females, showing relatively higher PNU-142586 and PNU-142300 AUC and Cmax and shorter linezolid t1/2 at steady-state were observed. The sample size in this study is not adequate to define sex-based differences in pharmacokinetic parameters.