Pharmacokinetic parameters of garenoxacin
Parameters were calculated from the plasma concentration-time profiles of garenoxacin and amounts excreted into urine following an administration of garenoxacin. Results were expressed as the mean ± S.D. (n = 3 or 4).
Parameter | Rat | Dog | Monkey | |
|---|---|---|---|---|
| Dose (mg/kg) | i.v. | 10 | 15 | 5 |
| p.o. | 10 | 25 | 5 | |
| CL (ml/min/kg) | 12.1 ± 6.1 | 2.43 ± 0.28 | 3.39 ± 0.30 | |
| Vss (l/kg) | 0.88 ± 0.26 | 1.29 ± 0.05 | 0.96 ± 0.05 | |
| MRT (h) | i.v. | 1.42 ± 0.61 | 8.93 ± 0.67 | 4.7 ± 0.4 |
| p.o. | 2.89 ± 1.43 | 11.6 ± 3.5 | 5.9 ± 1.2 | |
| t½ (h) | i.v. | 1.42 ± 0.51 | 7.64 ± 1.99 | 4.0 ± 0.4 |
| p.o. | 2.38 ± 0.90 | 7.81 ± 2.85 | 4.5 ± 0.2 | |
| Cmax (μg/ml) | p.o. | 6.25 ± 2.28 | 7.94 ± 3.12 | 2.98 ± 0.70 |
| tmax (h) | 0.25 ± 0.00 | 3.33 ± 1.16 | 1.2 ± 0.8 | |
| AUC (μg · h/ml) | i.v. | 13.6 ± 4.3 | 104 ± 12 | 24.7 ± 2.3 |
| p.o. | 10.5 ± 1.4 | 124 ± 31 | 18.7 ± 2.7 | |
| F | 0.772 | 0.716 | 0.757 | |
| Serum free fraction f | 0.131 ± 0.006 | 0.229 ± 0.007 | 0.186 ± 0.001 | |
| Ae | i.v. | 0.145 ± 0.044 | 0.134 ± 0.029 | 0.403 a |
| CLr (ml/min/kg) | 1.65 ± 0.21 | 0.368 ± 0.039 | 1.38 a | |
| CLer (ml/min/kg) |
| 10.4 ± 6.0 | 2.06 ± 0.31 | 2.01 a |
Cmax, maximum concentration; tmax, time to reach the maximum concentration; AUC, area under the curve extrapolated to infinity; F, availability; Ae, fraction excreted unchanged in urine.
↵ a The values of Ae, CLr, and CLer for monkeys were representative mean values (n = 3) because the extent of urinary excretion of garenoxacin was determined in pooled urine of three animals.