The effect of a high-fat breakfast on the pharmacokinetics of moxidectin in healthy male subjects: a randomized phase I trial.
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.
Joan M
JM
Korth-Bradley
Virginia
V
Parks
Stephan
S
Chalon
Ian
I
Gourley
Kyle
K
Matschke
Karine
K
Cailleux
Serge
S
Fitoussi
Lawrence
L
Fleckenstein
D000284:Administration, Oral; D000328:Adult; D000969:Antinematodal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D004041:Dietary Fats / Q000008:administration & dosage / Q000494:pharmacology*; D005215:Fasting; D018565:Food-Drug Interactions; D006801:Humans; D018942:Macrolides / Q000008:administration & dosage / Q000493:pharmacokinetics; D008297:Male; D008875:Middle Aged; D055815:Young Adult
D000969:Antinematodal Agents; D004041:Dietary Fats; D018942:Macrolides; C027837:moxidectin