Table 2.
Pharmacokinetic parameters of MBZ-OS and MBZ-1% tragacanth in plasma and tissues of mice after oral administration at a single dose of 25 mg/kg
| Plasma, Parasite and Tissues | Mean value (SD) of pharmacokinetic parameters (MBZ-1% tragacanth/MBZ-OS) | |||||||
|---|---|---|---|---|---|---|---|---|
| T max a (h) | C max b (μg/ml or μg/g) | AUC 0-t c (μg/ml × h or μg/g × h) | F d | |||||
| Plasma | 2.6 (1.1) | 3.3 (1.1) | 0.7 (0.2) | 4.1 (1.7) | 3.8 (1.9) | 27.1 (0.9) | 7.1 | |
| Parasite | Cyst wall | 0.8 (0.3) | 6.7 (2.3) | 1.1 (0.7) | 0.7 (0.3) | 5.8 (2.0) | 13.4 (4.1) | 2.3 |
| Cyst fluid | 1.0 (0) | 8.0 (0) | 0.011 (0.002) | 0.031 (0.004) | 0.069 (0.011) | 0.50 (0.03) | 7.3 | |
| Tissues | Liver | 1.1 (0.9) | 3.1 (4.3) | 3.1 (2.7) | 4.1 (3.8) | 10.9 (11.1) | 19.4 (3.6) | 1.8 |
| Lung | 7.3 (7.5) | 4.0 (3.4) | 12.1 (12.0) | 50.2 (14.2) | 49.6 (47.6) | 459.7 (133.1) | 9.3 | |
| Spleen | 2.1 (1.8) | 11.3 (8.1) | 4.7 (2.1) | 10.6 (1.4) | 37.5 (28.0) | 135.3 (49.5) | 3.6 | |
| Kidney | 1.2 (0.8) | 9.2 (6.1) | 7.3 (2.1) | 7.6 (2.0) | 94.1 (24.4) | 137.8 (38.9) | 1.5 | |
| Intestine | 3.0 (1.7) | 1.1 (0.9) | 44.0 (39.2) | 7.8 (1.8) | 256.2 (233.9) | 28.2 (13.6) | 0.1 | |
| Heart | 13.4 (12.1) | 3.5 (4.0) | 2.4 (1.4) | 3.3 (0.6) | 28.2 (4.0) | 43.9 (4.1) | 1.6 | |
| brain | 8.7 (7.0) | 6.0 (3.5) | 0.2 (0.3) | 0.5 (0.1) | 0.7 (0.3) | 3.8 (0.06) | 5.4 | |
a: Tmax was time to the drug peak concentration.
b: Cmax was the peak concentration of the drug.
c: AUC0-t was the area under the drug concentration-time curve.
d: F (relative bioaviability) = AUC0-t of MBZ-1% tragacanth/AUC0-t of MBZ-OS.