The objective of this study was to assess the effect of a high-fat meal on the pharmacokinetics of moxidectin. Healthy male subjects were randomized to receive single oral 8 mg doses of moxidectin after an overnight fast or high-fat breakfast. In fasted subjects (N = 27), mean [SD] parameters were C(max): 58.9 [12.5] ng/mL; t(max): 3.7 [1.5] h; area under concentration-time curve (AUC): 3,387 [1,328] ng/h/mL; Vλ(z)/F: 2,829 [1,267] L; CL/F: 2.76 [1.28] L/h; and t(1/2): 784 [347] h. Compared with fasted subjects, fed subjects (N = 27) exhibited a 34% increase in C(max), delay in t(max) to 5.3 [2.1] h, 44% increase in AUC, 40% decrease in Vλ(z)/F, and a 35% decrease in CL/F. There was no significant change in t(1/2). The changes are consistent with an increase in moxidectin bioavailability following administration with food. There were no clinically relevant changes in vital signs, laboratory tests, or electrocardiograms.
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Korth‐Bradley et al. (2012) studied this question.