A comparative bioavailability study of two formulations of itraconazole 100 mg capsule in healthy human Indian subjects under fasting conditions

The objective of the study was to evaluate the effect of time of administration of food post-dosing on the oral bioavailability of two formulations of itraconazole 100 mg capsule in 24 healthy adult Indian subjects under fasting conditions. Three different paradigms for time of administrations of food post-dose were selected: 4 h, 5 h, and 6 h. A randomized two-treatment, four-period, three-sequence, single dose bioavailability study was conducted. After dosing, serial blood samples were collected for up to 72 h. Plasma samples were analyzed for Itraconazole (ITZ) and its metabolite Hydroxy Itraconazole (OH-ITZ) by a sensitive and validated simultaneous liquid-chromatographic and mass-spectrometric (LC-MS/MS) method. A comparison of effect of post-dose fasting up to 4 h, 5 h, and 6 h on pharmacokinetic parameters of the two formulations was done, and it was found that pharmacokinetic parameters (Cmax, AUC0–t, AUC0–∞, Tmax) were consistent for both formulations in all the paradigms tested. This result suggests no impact on itraconazole bioavailability is observed based on difference in time of administration of food post-dose.