TABLE 1.
Serum pharmacokinetic parameters of benznidazole after a single oral dose of 100 mg/kg in healthy and chronically T. cruzi (Berenice-78 strain)-infected Swiss micea
| Parameter | Median value (IQ25–75) for group |
|
|---|---|---|
| Infected mice | Healthy mice | |
| Ka (h−1) | 3.92* (3.22–4.66) | 1.82 (1.73–1.88) |
| Cmax (μg/ml) | 44.24 (39.78–52.22) | 41.74 (40.86–42.87) |
| Tmax (h) | 0.67* (0.60–0.76) | 1.17 (1.16–1.18) |
| t1/2a (h) | 0.18* (0.15–0.23) | 0.38 (0.37–0.40) |
| AUC0–∞ (μg · h/ml) | 158.09 (141.34–181.98) | 199.67 (191.53–200.57) |
| t1/2el (h) | 1.92 (1.79–1.99) | 2.33 (2.10–2.43) |
| V/F (liters) | 0.089* (0.07–0.10) | 0.036 (0.03–0.04) |
| CL/F (liters/h) | 0.030* (0.02–0.04) | 0.011 (0.010–0.012) |
| Kel (h−1) | 0.36 (0.35–0.39) | 0.30 (0.29–0.33) |
a
Data are expressed as medians and interquartile ranges (IQ25–75). Cmax, maximum plasma concentration; AUC0–∞, area under the plasma concentration-versus-time curve from time zero to infinity; V, volume of distribution; CL, total clearance; t1/2el, elimination half-life; Kel, elimination rate constant; Ka, absorption rate constant; t1/2a, absorption half-life; Tmax, time to reach Cmax. *, P < 0.05 by a Mann-Whitney test.