TABLE 2.
Tissue 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 and tissue | Value for group |
|
|---|---|---|
| Infected mice | Healthy mice | |
| Median Cmax (μg/g) (IQ25–75) | ||
| Brain | 3.53* (2.92–4.47) | 2.53 (1.87–2.58) |
| Colon | 7.56* (6.34–11.12) | 3.73 (3.05–7.30) |
| Heart | 3.93* (3.77–7.12) | 3.00 (1.92–3.32) |
| Median Tmax (h) (IQ25–75) | ||
| Brain | 0.5 | 1.0 |
| Colon | 0.5 | 0.5 |
| Heart | 0.5 | 0.5 |
| Median AUC0–t (μg · h/g) (IQ25–75) | ||
| Brain | 7.97 (6.97–9.17) | 6.23 (5.08–7.27) |
| Colon | 21.21* (18.59–28.74) | 8.15 (6.71–13.76) |
| Heart | 13.58* (12.35–15.60) | 5.72 (4.90–8.63) |
| AUC0–t,tissue/AUC0–t,serum ratio (%) | ||
| Brain | 5 | 3 |
| Colon | 13 | 4 |
| Heart | 9 | 3 |
a
Data are expressed as medians and interquartile ranges (IQ25–75). Cmax, maximum plasma concentration; AUC0–t, area under the plasma concentration-versus-time curve from 0 h to time t; Tmax, time to reach Cmax; AUC0–t,tissue/AUC0–t,serum ratio, tissue penetration ratio. *, P < 0.05 by a Mann-Whitney test.