TABLE 1.
Plasma creatinine and AMB concentrations after administration of a single i.v. dose of DOC-AMB and a single administration by oral gavage of DOC-AMB and various AMB lipid formulations to male Sprague-Dawley rats
| Treatment group and/or route of administration | Dose (mg/kg) | Plasma creatinine levela
|
Tmax (h) | Cmax (μg/ml) | AUC0-24 (μg · h/ml) | ||
|---|---|---|---|---|---|---|---|
| Concn prior to dose (mg/dl) | Concn 24 h after dose (mg/dl) | % Change from baseline | |||||
| DOC-AMB | |||||||
| i.v. | 1 | 0.38 ± 0.13 | 0.71 ± 0.10b | +87 | 4.3 ± 1.1 | ||
| Oral | 5 | 0.34 ± 0.07 | 0.29 ± 0.05 | −15 | NDc | ND | ND |
| Oral | 50 | 0.29 ± 0.07 | 0.42 ± 0.02b | +45 | 8 | 39.8 ± 22 | 519 ± 209d |
| AMB-lipid formulations | |||||||
| ABLC | 50 | 0.45 ± 0.01 | 0.24 ± 0.07b | −47 | 10 | 48.5 ± 26 | 542 ± 271 |
| Intralipid-AMB | 50 | 0.27 ± 0.02 | 0.38 ± 0.02b | +33 | 2 | 769 ± 213e | 5,984 ± 3,461e |
| Peceol AMB | 50 | 0.48 ± 0.10 | 0.65 ± 0.07 | +35 | 4 | 1,469 ± 891e | 11,407 ± 4,971e |
| 5 | 0.44 ± 0.06 | 0.39 ± 0.06 | −11 | 2 | 1,187 ± 409e | 4,415 ± 2,411e | |
Data presented as means ± standard deviations (n = 6).
Significantly difference from values prior to dose (P < 0.05).
ND, not determinable.
Significantly difference from DOC-AMB i.v. value (P < 0.05).
Significantly different from AUC0-24 value for ABLC (P < 0.05).