TABLE 3.
Plasma and ELF concentrations of ceftaroline in healthy subjects
| Dosage regimen and time pointa (h) | Ceftaroline concn (mg/liter) |
Ratiob | |||
|---|---|---|---|---|---|
| Total plasma (n = 25 per treatment) |
ELF (n = 5 per time point, per treatment) |
||||
| Median | Min, max | Median | Min, max | ||
| 600 mg q12h | |||||
| 1 | 18.73 | 14.8, 25.7 | 3.38 | 2.08, 7.63 | 0.23 |
| 2 | 8.47 | 5.49, 11.4 | 1.60 | 1.08, 3.45 | 0.24 |
| 4 | 3.27 | 2.2, 4.9 | 0.54 | 0.36, 1.26 | 0.20 |
| 8 | 0.9 | 0.4, 1.2 | 0.18 | 0.00, 0.22 | 0.25 |
| 12 | 0.27 | 0.11, 0.43 | 0.00 | 0.00, 0.00 | 0.00 |
| 600 mg q8h | |||||
| 1 | 21.31 | 16.7, 28.9 | 3.56 | 2.69, 5.07 | 0.21 |
| 2 | 9.46 | 7.85, 12.0 | 2.57 | 0.61, 3.2 | 0.34 |
| 4 | 3.56 | 2.85, 5.49 | 0.58 | 0.39, 0.98 | 0.20 |
| 6 | 1.74 | 1.28, 3.29 | 0.27 | 0.17, 0.52 | 0.19 |
| 8 | 0.99 | 0.20, 1.74 | 0.26 | 0.00, 0.70 | 0.32 |
a
For subjects receiving 600 mg q12h, 4/5 subjects had measurable concentrations in ELF at 8 h. The same result was seen for subjects receiving 600 mg q8h, with 4/5 subjects having measureable concentrations of ceftaroline in ELF at 8 h. Ceftaroline was not measurable in the ELF of the five subjects who underwent BAL at 12 h.
b
Ratio of free drug assuming 20% protein binding in plasma and no protein binding in epithelial lining fluid.