TABLE 3.
Distribution of radioactivity in pooled human urine extracts after a single oral dose of 399 mg of [14C]posaconazole to healthy human subjects
Peak | Rt (min) | m/z | Δa | % of profiled radioactivity | % of dose (0-120 h)b |
---|---|---|---|---|---|
Unknown | 12.0 | NDe | NAf | 9.38 | 1.24 |
Unknown | 12.6 | ND | NA | 1.38 | 0.18 |
Unknown | 13.7 | ND | NA | 15.5 | 2.04 |
Unknown | 16.7 | ND | NA | 5.19 | 0.69 |
Unknown | 18.2 | ND | NA | 6.37 | 0.84 |
M1 | 21.1 | 600 | −101 | 8.20 | 1.08 |
M2 | 22.9 | 263 | −438 | 4.57 | 0.60 |
M3 | 23.6 | 600 | −101 | 2.63 | 0.35 |
Unknown | 25.1 | ND | NA | 2.18 | 0.29 |
M4 | 26.2 | 305 | −396 | 6.61 | 0.87 |
Unknown | 29.8 | ND | NA | 1.38 | 0.18 |
M5 | 31.5 | 1053 | +352 | 15.0 | 1.97 |
M6c | 32.4 | 332 | −369 | 6.75 | 0.89 |
M7 | 32.9 | 424 | −277 | ||
M8 | 34.3 | 877 | +176 | 10.7 | 1.41 |
M9d | 38.5 | 877 | +176 | 4.29 | 0.57 |
M10 | 719 | +18 | |||
M11 | 715 | +14 | |||
M12 | 39.6 | 717 | +16 | BITg | 0.00 |
M13 | 40.1 | 717 | +16 | BIT | 0.00 |
M14 | 40.9 | 717 | +16 | BIT | 0.00 |
Posaconazole | 42.1 | 701 | 0 | BIT | 0.00 |
That is, the difference between the m/z of the metabolite and that of posaconazole.
The percentage of the dose is the percentage of chromatographic peak integration multiplied by the fraction of the dose excreted in urine. The radioactivity excreted in subjects 1 to 8 (0 to 120 h) was 13.2% of the dose.
Metabolites M6 and M7 were not resolved from each other by the radiometric detector.
Metabolites M9, M10, and M11 were not resolved from each other by the radiometric detector.
ND, not detected. No drug-related ion was detected by MS.
NA, not applicable.
BIT, below the integration threshold of the 14C detector but detected by MS.