Influence of surfactants on oral bioavailability of albendazole based on the formation of the sulphoxide metabolites in rats.
The influence of two surfactants, sodium taurocholate (STC) and polysorbate 80 (P80), on the bioavailability of albendazole (ABZ), orally administered to rats, has been studied. To assess the effect of the surfactants, they were administered at critical micellar and supramicellar concentrations, 5 and 10 mM for STC and 0.0022 and 0.22% for P80, along with a subclinical dose of 5 mg kg-1 of ABZ. Doses of 5 and 10.6 mg kg-1 ABZ were also administered as controls. The results show an increase in the sulphoxide AUC values: 55% in the STC 5 mM and 88% in the STC 10 mM and P80 0.0022% treatments when compared to the control ABZ 5 mg kg-1 dose. MRT values also show longer-lasting plasma albendazole sulphoxide concentration following these three treatments, particularly for the P80 0.0022% treatment. While there was no change in the apparent rate of formation of ABZSO, the amount of ABZSO formed was increased significantly by the addition of surfactants (STC 10 mM and P80 0.0022%).
Redondo
P A
PA
Department of Physiology, Pharmacology, and Toxicology, University of León, Spain.
Alvarez
A I
AI
García
J L
JL
Villaverde
C
C
Prieto
J G
JG
D015766:Albendazole / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D006207:Half-Life; D008297:Male; D008823:Micelles; D051381:Rats; D017208:Rats, Wistar; D013454:Sulfoxides / Q000378:metabolism; D013501:Surface-Active Agents / Q000494:pharmacology*
D000871:Anthelmintics; D008823:Micelles; D013454:Sulfoxides; D013501:Surface-Active Agents; D015766:Albendazole