TABLE 5.
PK/PD parameters of ciprofloxacin, sparfloxacin, and temafloxacin in the sera and lungs of immunocompetent mice infected with penicillin-susceptible strain P-4241 following s.c. administration of a single dosea
| Drug (dose [mg/kg]) and sample | Cmax (μg/ml or g) | t1/2 (h) | AUC0–24 (μg · h/ml or g) | Lung/serum AUC ratio | AUC/MIC ratio |
|---|---|---|---|---|---|
| Ciprofloxacin (100) | |||||
| Serum | 12.6 | 1.9 | 15 | 15 | |
| Lung tissue | 62.0 | 1.1 | 47 | 3.1 | 47 |
| Sparfloxacin (50) | |||||
| Serum | 9.4 | 4.2 | 25 | 100 | |
| Lung tissue | 27.0 | 5.7 | 64 | 2.6 | 256 |
| Temafloxacin (100) | |||||
| Serum | 14.7 | 3.8 | 142 | 142 | |
| Lung tissue | 124 | 2.8 | 490 | 3.4 | 490 |
a
Values are for six pooled serum and lung samples taken 0.5, 1, 3, 6, 8, and 24 h postdosing. The MICs and MBCs, respectively, for the challenge strain are as follows: ciprofloxacin, 1 and 2 μg/ml; sparfloxacin, 0.25 and 0.5 μg/ml; temafloxacin, 1 and 1 μg/ml.