TABLE 3.
Mean (n = 16) pharmacokinetic parameters for total ertapenem in healthy volunteers receiving various single i.v. doses
| Pharmacokinetic parameter | Mean value (SD) at indicated dose
|
|||
|---|---|---|---|---|
| 0.5 g | 1 g | 2 g | 3 g | |
| AUC0-∞ (μg · h/ ml) | 305.6 (36.8) | 572.1 (68.6) | 1,011.4 (118.0) | 1,407.2 (230.1) |
| CLP (ml/min) | 27.6 (3.2) | 29.5 (3.4) | 33.4 (4.1) | 36.3 (5.2) |
| CLR (ml/min) | 12.7 (3.4)a | 12.9 (4.3)b | 14.9 (4.6) | 16.1 (4.9)b |
| CLNR (ml/min) | 15.0 (4.0)a | 16.1 (5.4)b | 18.5 (5.5) | 20.3 (5.9)b |
| VSS (liter) | 7.8 (1.3) | 8.2 (1.5) | 9.2 (1.4) | 9.4 (1.7) |
| Cmaxe (μg/ml) | 83.0 (12.1) | 154.9 (22.0) | 282.9 (41.4) | 274.3 (41.3) |
| C12 (μg/ml) | 5.2 (1.1) | 9.3 (2.8) | 16.4 (3.6) | 25.3 (8.3) |
| C24 (μg/ml) | 0.6 (0.3) | 1.2 (0.6) | 2.0 (1.0) | 3.0 (1.9) |
| fe (% dose)c | 45.6 (12.1)a | 44.4 (14.8)b | 44.3 (13.3) | 44.1 (12.5)b |
| t1/2β (h)d | 3.8 | 3.8 | 3.8 | 3.6 |
a
Based on 15 subjects; 1 subject whose urine collection during one of the intervals appeared incomplete was not included.
b
Based on 14 subjects; 2 subjects whose urine collections in one of the intervals appeared incomplete or missing were not included.
c
Percent excreted during 0 to 24 h.
d
Harmonic mean.
e
Cmax = concentration at end of infusion. The length of infusion was 0.5 h except for the 3-g dose, which was administered over 2 h.