TABLE 6.
Mean pharmacokinetic parameters for total ertapenem in men and women volunteers following various single i.v. doses (study 2)
| Pharmacokinetic parameter | Mean value (SD) for indicated dose
|
|||||||
|---|---|---|---|---|---|---|---|---|
| Men (n = 8)
|
Women (n = 8)
|
|||||||
| 0.5 ga | 1 g | 2 g | 3 gb | 0.5 g | 1 g | 2 g | 3 gb | |
| AUC0-∞ (μg · h/ml) | 298 (40.3) | 575.0 (83.7) | 986.3 (144.1) | 1,376.1 (302.3) | 312.3 (34.2) | 569.1 (55.3) | 1,036.5 (87.5) | 1,438.4 (140.9) |
| CLP (ml/min) | 28.3 (3.7) | 29.5 (4.1) | 34.4 (4.9) | 37.6 (6.5) | 27.0 (2.8) | 29.5 (2.8) | 32.4 (3.0) | 35.1 (3.5) |
| CLR (ml/min) | 10.9 (3.1) | 10.1 (3.4) | 12.2 (4.1) | 13.6 (5.8) | 14.3 (3.0) | 15.7 (3.1) | 17.6 (3.3) | 18.7 (2.2) |
| CLNR (ml/min) | 17.6 (3.2) | 18.8 (6.0) | 22.3 (5.1) | 23.7 (6.2) | 12.7 (3.2) | 13.3 (3.1) | 14.8 (2.6) | 16.9 (3.1) |
| Cmax (μg/ml) | 78.2 (13.2) | 144.2 (20.6) | 268.2 (48.1) | 253.0 (47.7) | 87.9 (9.4) | 165.5 (18.7) | 297.7 (29.2) | 295.7 (18.6) |
| C12 (μg/ml) | 5.5 (1.1) | 10.3 (2.1) | 17.5 (4.0) | 26.9 (9.5) | 4.8 (1.2) | 8.4 (3.2) | 15.4 (3.0) | 23.8 (7.3) |
| C24 (μg/ml) | 0.8 (0.2) | 1.5 (0.5) | 2.5 (1.1) | 3.8 (2.1) | 0.5 (0.2) | 1.0 (0.6) | 1.6 (0.6) | 2.2 (1.2) |
| fe(0-24) (% dose) | 37.5 (8.4) | 35.2 (13.2) | 34.8 (10.1) | 35.8 (12.1) | 52.7 (10.5) | 53.7 (9.9) | 53.8 (8.4) | 52.3 (5.7) |
| t1/2 (h) | 4.1 (0.3) | 4.2 (0.3) | 4.0 (0.5) | 3.9 (0.5) | 3.5 (0.3) | 3.5 (0.5) | 3.5 (0.3) | 3.3 (0.4) |
| VSS (liter) | 8.6 (1.3) | 8.9 (1.6) | 10.1 (1.5) | 10.4 (1.8) | 7.0 (0.8) | 7.5 (0.9) | 9.2 (1.4) | 9.4 (1.7) |
a
CLR, CLNR, and fe for the 0.5-g dose are based on 7 subjects (one subject's urine collection during one of the intervals appeared incomplete).
b
CLR, CLNR, and fe for the 3-g dose are based on seven out of eight subjects in each group (one subject's urine collection in one of the intervals appeared incomplete or missing).