Effects of Food and Omeprazole on Novel Formulation SUBA-Itraconazole in Healthy Subjects.

This study evaluated the pharmacokinetic profile of SUBA-itraconazole under fasting and fed conditions, as well as with the concomitant administration of a proton pump inhibitor. The effect of food was assessed in an open-label, randomized, cross-over bioavailability study of SUBA-itraconazole capsules 65 mg (2 x 65 mg BID) in healthy adults (n = 20) under fasting and fed conditions to steady-state levels. Secondly, an open-label, two-treatment, fixed-sequence comparative bioavailability study in healthy adults (n=28) under fasted conditions compared the pharmacokinetics of a single oral dose of SUBA-itraconazole capsules (2 x 65 mg/day) with and without co-administration of daily omeprazole delayed-release capsules (1 x 40 mg/day) under steady-state conditions. In the fed and fasted state SUBA-itraconazole demonstrated similar concentrations at the end of the dosing interval, with modestly lower total and peak itraconazole (ITZ) exposure when administered under fed conditions compared to the fasted state; fed/fasted ratios of 78.09% (90%CI 74.49-81.86%) for AUCtau [14183.2 vs. 18479.8 hr·ng/mL], 73.05% (90%CI 69.01-77.33%) for Cmax,ss [1519.1 vs. 2085.2 ng/mL] and 91.53% (90%CI 86.41-96.96%) for Ctrough [1071.5 vs. 1218.5 ng/mL]. When dosed concomitantly with omeprazole there was a 22% increase in total plasma exposure of ITZ, as measured by AUC0-∞ (p = 0.0069), and a 31% increase in peak plasma exposure of ITZ, as measured by Cmax (p = 0.0083). PMID: 30297369 [Pu...
Source: Antimicrobial Agents and Chemotherapy - Category: Microbiology Authors: Tags: Antimicrob Agents Chemother Source Type: research