TABLE 3.
Pharmacokinetic (PK) parameters predicted for adult humans for determination of infusion rates for simulation of amoxicillin-clavulanate 16:1 twice a day in rats
| Species | PK modela | Parameter | Amoxicillin (2,000 mg) | Clavulanate (125 mg) |
|---|---|---|---|---|
| Human | C(t) = A(e−kelt − e−kat) + B(e−kel2(t − 2) − e−ka2(t − 2))b | A (μg/ml) | 95.0 | 9.0 |
| kel (h−1) | 1.0 | 1.3 | ||
| ka (h−1) | 0.65 | 0.78 | ||
| B (μg/ml) | 60.0 | |||
| kel2 (h−1) | 1.3 | |||
| ka2 (h−1) | 0.8 | |||
| Rat | C = Ae−λt | A (μg/ml) | 240 | 26.7 |
| λ (h−1) | 2.1 | 2.4 | ||
| Dose (mg/kg) | 44.0 | 4.4 |
a
C is the concentration in plasma at time t, A is the zero-time intercept assuming instantaneous absorption, e is the base of the natural log, kel is the elimination constant and ka is the absorption rate constant.
b
Sustained-release portion starting 2 h (t − 2) after immediate release. B is the zero-time intercept assuming instantaneous absorption for the second portion.