Pharmacokinetics and tolerability of intravenous posaconazole in healthy Chinese volunteers: a randomized, open-label and single-dose study.

ABSTRACT

Posaconazole is a triazole antifungal drug with strong antifungal effect. The pharmacokinetics, safety, and tolerability were evaluated following the intravenous administration of posaconazole injection. A total of 36 healthy adults were enrolled in the parallel-designed clinical trial, and the subjects received single doses of posaconazole injection (100, 200 and 300 mg). Posaconazole concentrations in plasma were determined with liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The levels of posaconazole in plasma increased proportionally between 100 and 300-mg dose, but AUC showed a more-than-dose-proportional increase. Besides, decreased Vd and CL were observed, along with the increased posaconazole dosage. Posaconazole was well tolerated at all dose levels, and the adverse events were not dose dependent. No clinically significant changes in electrocardiograms were observed.