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. Author manuscript; available in PMC: 2016 Jun 30.
Published in final edited form as: Curr Opin Investig Drugs. 2005 Aug;6(8):845–853.
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.
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