Albendazole (ABZ) is a broad spectrum anthelmintic benzimidazole with very low bioavailability, and its activity is due to its main metabolite, Albendazole sulphoxide (ABZS). This work demonstrates the improvement of bioavailability when the ABZS is directly administered, compared with the ABZ administration, both orally given. This observation may be used as an interesting target in the design of new drugs with antihelmintic activity in systemic diseases, using ABZS as a parent drug.