Table 2.
Summary of the pharmacokinetic parameters for Lzd, PH027 and PH051 after IV and oral administration.
| Parameters | Linezolid | PH027 | PH051 |
|---|---|---|---|
| IV Administration (n = 4, 5 mg/kg) | |||
| AUC (μg h/L) | 4038 ± 1280 | 5670 ± 933 | 1950 ± 986 |
| CLT (L/h/kg) | 1.24 ± 0.43 | 0.882 ± 0.23 | 2.564 ± 1.212 |
| Elimination rate constant (min−1) | 0.0132 | 0.0101 | 0.00396 |
| Half life (min) | 52.4 ± 6.3 | 68.7 ± 12.1 | 175 ± 46.1 |
| Renal clearance (L/h/kg)# | 0.083 ± 0.016 | 0.00380 ± 0.0007 | - |
| Fraction excreted unchanged in urine | 5.70% | 0.402% | - |
| Oral Administration (n = 4, 20 mg/kg, as Suspension) | |||
| Cmax (μg/L) | 3910 ± 1010 | 1620 ± 820 | 69.7 ± 14.8 |
| tmax (min) | 60 | 60 | 60 |
| AUC (μg h/L) | 6250 ± 3620 | 5010 ± 2430 | 369 ± 378 |
| Bioavailability (%) | 38.7 % | 22.1%. | 4.73% |
| Oral Administration (n = 3, 20 mg/kg, as Microemulsion) | |||
| Cmax (μg/L) | 3413 ± 1800 | 2871 ± 392 | 731 ± 412 |
| tmax (min) | 45 | 120 | 30 |
| AUC (μg h/L) | 8350 ± 3340 | 16,550 ± 3460 | 1083 ± 426 |
| Bioavailability (%) | 51.7% | 72.9% | 13.9% |
| Increase in bioavailability | 33.6 % | 328 % | 293 % |
# Calculated from individual urine collection intervals, from renal excretion rate and plasma drug concentration.