TABLE 3.
Pharmacokinetic parameter | Amoxicillin
|
Clavulanic acid
|
||||||
---|---|---|---|---|---|---|---|---|
Total
|
Free
|
Total
|
Free
|
|||||
β pos | β neg | β pos | β neg | β pos | β neg | β pos | β neg | |
Mean Concn (μg/ml) ± SD at time (h) | ||||||||
1 | 11.6 ± 0.6 | 11.6 ± 0.5 | 9.9 ± 2.2 | 10.4 ± 0.5 | 1.2 ± 0.0 | 1.3 ± 0.1 | 0.9 ± 0.1 | 0.9 ± 0.1 |
1.5 | 17.4 ± 0.8 | 17.2 ± 0.6 | 13.3 ± 0.9 | 13.6 ± 0.7 | 2.1 ± 0.1 | 2.1 ± 0.2 | 1.4 ± 0.2 | 1.5 ± 0.1 |
2 | 14.1 ± 0.5 | 15.5 ± 0.2 | 7.8 ± 0.9* | 11.8 ± 0.6 | 1.5 ± 0.2 | 1.4 ± 0.2 | 1.0 ± 0.1 | 1.0 ± 0.1 |
3 | 10.5 ± 0.1 | 12.5 ± 0.9 | 2.9 ± 0.0* | 10.1 ± 0.8 | 0.7 ± 0.1 | 0.7 ± 0.1 | 0.4 ± 0.0 | 0.5 ± 0.1 |
4 | 5.5 ± 0.7* | 9.3 ± 0.6 | 0.8 ± 0.2* | 8.2 ± 0.9 | 0.4 ± 0.0 | 0.4 ± 0.0 | 0.1 ± 0.0 | 0.2 ± 0.1 |
6 | 2.1 ± 0.2* | 5.9 ± 0.5 | <0.03 | 5.0 ± 0.5 | 0.1 ± 0.0 | 0.1 ± 0.0 | 0.1 ± 0.0 | 0.1 ± 0.0 |
8 | <0.03 | 2.0 ± 0.3 | <0.03 | 1.7 ± 0.3 | 0.1 ± 0.0 | 0.1 ± 0.0 | <0.03 | <0.03 |
10 | <0.03 | 0.8 ± 0.0 | <0.03 | 0.6 ± 0.2 | <0.03 | <0.03 | <0.03 | <0.03 |
12 | <0.03 | 0.3 ± 0.1 | <0.03 | 0.3 ± 0.1 | <0.03 | <0.03 | <0.03 | <0.03 |
Mean Cmax (μg/ml) ± SD | 17.4 ± 0.6 | 17.2 ± 0.6 | 13.3 ± 0.9 | 13.6 ± 0.7 | 2.1 ± 0.0 | 2.1 ± 0.2 | 1.4 ± 0.1 | 1.5 ± 0.1 |
Mean AUC0-24 (μg/ml·h) ± SD | 48.7 ± 0.2* | 73.1 ± 1.2 | 22.5 ± 2.4* | 60.7 ± 3.3 | 4.5 ± 0.0 | 4.7 ± 0.0 | 2.8 ± 0.2 | 2.9 ± 0.1 |
Mean T>MIC (% dosing interval)b | 23.3 | 34.6 | 10.4 | 28.3 |
β pos, β-lactamase-positive simulations; β neg, β-lactamase-negative simulations. *, P ≤ 0.012 versus β-negative simulations.
For the BLPACR strain.