TABLE 2.
Polyene pharmacokinetics in serum and tissue homogenates
| Tissue | Pharmacokinetic parameter | AMB (20)a | AMB (5) | L-AMB (80) | L-AMB (20) | ABLC (80) | ABLC (20) |
|---|---|---|---|---|---|---|---|
| Serum | Cmax (μg/ml) | 4.58 ± 1.20 | 218 ± 39.0 | 119 ± 7.00 | 13.3 ± 0.82 | 13.3 ± 0.82 | 0.90 ± 0.00 |
| t1/2b (h) | 16 | 14.3 | 10.1 | 12.5 | 12.5 | 16 | |
| AUC0-∞c (mg · h/liter) | 140 | 7,006 | 1,181 | 195 | 195 | 22 | |
| Kidney | Cmax (μg/ml) | 4.48 ± 0.40 | NDd | 14.4 ± 0.66 | 2.51 ± 0.00 | 29.1 ± 0.68 | ND |
| Mean ± SD Cmax (μg/ml) | 3.84 ± 0.70 | ND | 9.20 ± 3.22 | 0.93 ± 0.74 | 16.4 ± 8.32 | ND | |
| AUC0-48e (mg · h/liter) | 137 | ND | 351 | 26.5 | 761 | ND | |
| Liver | Cmax (μg/ml) | 42.1 ± 2.0 | 14.3 ± 0.52 | 12.9 ± 0.20 | 7.40 ± 0.50 | 46 ± 18 | 22 ± 2.8 |
| Mean ± SD Cmax (μg/ml) | 20.5 ± 11.4 | 9.47 ± 301 | 9.30 ± 3.11 | 4.95 ± 2.90 | 32 ± 14 | 16 ± 5.4 | |
| AUC0-48 (mg · h/liter) | 1,150 | 301 | 521 | 297 | 1,760 | 778 | |
| Lung | Cmax (μg/ml) | 3.33 ± 0.66 | ND | 7.90 ± 0.23 | 4.23 ± 0.54 | 218 ± 26 | ND |
| Mean ± SD Cmax (μg/ml) | 1.44 ± 1.00 | ND | 4.53 ± 2.20 | 1.35 ± 0.54 | 52 ± 81 | ND | |
| AUC0-48 (mg · h/liter) | 72 | ND | 181 | 33.1 | 2,739 | ND |
a
Values in parentheses are doses (milligram per kilogram).
b
t1/2, half-life.
c
AUC0-∞, AUC from time zero to infinity.
d
ND, not detected.
e
AUC0-48, AUC from time zero to 48 h.