Treatmenta | ||
---|---|---|
Parameter | CPX-POM | CPX-O |
Body weight (kg) | 9.65 ± 0.38 | 9.64 ± 0.34 |
CPX dose (mg/kg)b | 2.28 ± 0.01 | 3.10 ± 0.02 |
Test article dose (mg/kg)c | 5.40 ± 0.02 | 4.01 ± 0.02 |
C0 (ng/ml) | 2970 ± 969 | 5996 ± 1387 |
Kel (h−1) | 0.242 ± 0.030 | 0.185 ± 0.019 |
T1/2 (h) | 2.90 ± 0.329 | 3.77 ± 0.40 |
AUC0∫n (ng⋅h/ml) | 2571 ± 436 | 3314 ± 655 |
AUC0∫∞ (ng⋅h/ml) | 3075 ± 591 | 4009 ± 802 |
AUMC0∫n (ng⋅h2/ml) | 5485 ± 1293 | 7293 ± 1520 |
AUMC0∫∞ (ng⋅h2/ml) | 11,680 ± 3682 | 16,665 ± 3971 |
MRT (h) | 3.74 ± 0.58 | 2.20 ± 0.09 |
Cl (ml/h/kg) | 762 ± 158 | 804 ± 200 |
Vdz (ml/kg) | 4133 ± 363 | 4253 ± 1266 |
Vss (ml/kg) | 3686 ± 431 | 3218 ± 810 |
F (%) | 105.4 ± 11.9 |
AUC0∫n, area under the plasma CPX concentration versus time curve from time zero to the last measurable time point; AUC0∫∞, area under the plasma CPX concentration versus time curve from time zero to infinity; AUMC0∫n, CPX area under the first moment versus time curve from time zero to the last measurable time point; AUMC0∫∞, CPX area under the first moment versus time curve from time zero to infinity; C0, extrapolated plasma CPX concentration at time zero following intravenous bolus administration; Cl, CPX systemic drug clearance; CPX, ciclopirox; CPX-O, ciclopirox olamine; CPX-POM, fosciclopirox; F, CPX bioavailability; Kel, apparent first-order elimination rate constant; MRT, CPX mean residence time; T1/2, apparent elimination half-life; Vdz, CPX apparent volume of distribution; Vss, CPX apparent steady state volume of distribution.
↵a N = 4 dogs receiving both treatments in a complete, nonrandomized, cross-over study design.
↵b Ciclopirox free acid dose.
↵c CPX-POM disodium heptahydrate was formulated in 25 mM phosphate pH 7 with 50 mM Captisol at a strength of 2.61 mg/ml (1.11 mg/ml ciclopirox free acid), CPX-O was formulated in 25 mM phosphate pH 7 with 50 mM Captisol at a strength of 1.94 mg/ml (1.50 mg/ml ciclopirox free acid).