High-fat breakfast increases bioavailability of albendazole compared to
light breakfast: single-dose study in healthy subjects
Abstract
Background – Albendazole is a benzoimidazole carbamate drug with
anthelmintic and antiprotozoal activity against intestinal and tissue
parasites. It has been described that the administration with meals
increases albendazole absorption. Objective – Our aim was to compare
the systemic exposure in healthy volunteers of two albendazole
formulations after a single oral dose under fed conditions and to
evaluate the effect of breakfast composition on its bioavailability.
Methods – 12 healthy volunteers were included in a crossover, open,
randomized comparative bioavailability trial including two stages.
Single oral doses of 400 mg albendazole were administered under fed
conditions (a light breakfast in first stage and a high-fat breakfast in
the second) separated by 7-day washout periods. Plasma albendazole and
albendazole sulfoxide concentrations were measured by HPLC-MS/MS.
Results – Albendazole absorption was clearly influenced by the meal
composition. A high-fat breakfast increased albendazole and albendazole
sulfoxide area under the concentration-time curve (AUC) and maximum
concentration (Cmax) by double compared to a light breakfast. The
bioavailability of the two formulations was very similar, although the
sample size was not sufficient to demonstrate bioequivalence because the
intra-individual variability of albendazole was approximately 60%.
Conclusions – The higher albendazole and albendazole sulfoxide levels
when administered with a high-fat meal could be of importance in
clinical practice. Since albendazole labelling recommends its
administration with meals, it is necessary to insist the patient to take
it with a fatty meal so that the effectiveness of albendazole is not
compromised.