The peak and trough concentrations of the two enantiomeric pairs of ITZ in the six healthy volunteers after a single dose administration (day 1) of a 100-mg oral solution of itraconazole and after multiple dose administration (100 mg/day) for 7 days
Peak (Day 1) | Trough (Day 1) | Trough (Day 6) | Peak (Day 7) | Trough (Day 7) | |||
|---|---|---|---|---|---|---|---|
| nM | nM | nM | |||||
| 2R,4S-ITZs | 91 ± 53 | 2.5 ± 2.6 | 43 ± 43 | 505 ± 74 | 47 ± 45 | ||
| 2S,4R-ITZs | 270 ± 161 | 24 ± 14 | 172 ± 94 | 738 ± 84 | 182 ± 96 | ||
| SI | 3.0* | 9.4* | 4.0* | 1.5* | 3.8* | ||
SI, stereoselectivity index: the parameter ratio between the high and low stereoisomer value, presented to demonstrate the fold difference between the stereoisomer pairs.
↵* Significant (p < 0.05) difference found between the stereoisomer pairs.