Table 3.
Pharmacokinetic parameters of ITZ and OH-ITZ after oral administration of the optimized formulation (F3), formulation of ITZ-HPMCAS (F1), and marketed product (Sporanox®) at a dose of 100 mg in beagle dogs (Mean ± S.D., n = 6).
| Pharmacokinetic Parameter | F3 | F1 | Sporanox® |
|---|---|---|---|
| Cmax (μg/mL), ITZ | 0.61 ± 0.08 * | 0.51 ± 0.12 | 0.45 ± 0.06 |
| Cmax (μg/mL), OH-ITZ | 0.18 ± 0.07 | 0.14 ± 0.03 | 0.12 ± 0.04 |
| Tmax (h), ITZ | 3.89 ± 0.41 * | 4.13 ± 0.57 | 2.92 ± 0.37 |
| Tmax (h), OH-ITZ | 5.64 ± 0.97 | 6.40 ± 0.59 * | 4.60 ± 0.63 |
| AUC0–24h (μg h/mL), ITZ | 8.98 ± 1.76 ** | 6.40 ± 1.12 * | 5.06 ± 1.43 |
| AUC0–24h (μg h/mL), OH-ITZ | 2.88 ± 0.76 * | 2.27± 0.94 * | 1.41± 0.37 |
* Significantly different from Sporanox® according to the ANOVA test (p < 0.05); ** Significantly different from Sporanox® according to the ANOVA test (p < 0.01).