Study Type | Effect Studied | Model Used | Result | Reference |
---|---|---|---|---|
In vivo | Pharmacokinetics. | SPA-S-753 intravenously administered to rats (1.25, 2.5 and 5 mg/kg) and mice (1.25 and 2.5 mg/kg). |
In rats, the half-lives were approximately 21, 27, 39 h and the mean AUC values were 33, 53, 84 µg.h/ml, respectively. In mice, mean half-lives were 11 and 14 h, respectively. Compared with amphotericin B (1 mg/kg) the AUC0−∞ for SPA-S-753 was 2-fold higher in mice and 5-fold higher in rats. |
374244 |
In vivo | Pharmacokinetics. | Rats intravenously injected with SPK-843 (1.25 mg/kg) as single and multiple administrations (7 days). |
The half-life of SPK-843 was 22.15 h and AUC0−∞ was 35.52 µg.h/ml after a single administration. In multiple administrations the half-life was 41.4 h and the AUC0−∞ was 72.1 µg.h/ml. |
440534 |
In vivo | Pharmacokinetics. | Rats injected with three single dosage forms of SPK-843 (1.25 mg/kg in 5% glucose solution, 10% lipid emulsion at pH 5.3 and 10% lipid emulsion at pH 7.5). |
The half-lives of SPK-843 were 22.2 h in 5% glucose, 26.5 h in 10% lipid emulsion pH 5.3 and 23.2 h in lipid emulsion at pH 7.5. The AUC values were 35.5 µg.h/ml in 5% glucose, 40 µg.h/ml in 10% lipid emulsion pH 5.3 and 44.8 µg.h/ml in lipid emulsion at pH 7.5. |
440546 |
In vivo | Pharmacokinetics. | Phase I trial in healthy Japanese male individuals administered SPK-843 (0.0625, 0.125 or 0.25 mg/kg iv) as a 1 h infusion every day for 14 days. |
Blood Cmax values were 0.647, 1.180 and 2.030 µg/ml, respectively, and plasma Cmax values were 0.888, 1.185 and 1.250 µg/ml, respectively. |
568890 |