Effect of amphiphilic surfactants agents on the gastrointestinal absorption of albendazole in cattle

VIRKEL G.,; IMPERIALE F,; LIFSCHITZ A,; PIS, A; ALVAREZ, A; MERINO, G; PRIETO, J; LANUSSE, C

BIOPHARMACEUTICS & DRUG DISPOSITION

JOHN WILEY & SONS LTD

Año: 2003 p. 95 - 103

0142-2782

Albendazole (ABZ) is a widely used broad-spectrum benzimidazole (BZD) anthelmintic. Low hydrosolubility and poor/erratic gastrointestinal (GI) absorption play against the systemic availability and resultant clinical efficacy of BZD compounds. Different strategies are currently investigated to improve their bioavailability and efficacy in different animal species and humans. Surfactant agents facilitate dissolution of lipophilic drugs and increase membrane permeability. The influence of amphiphilic surfactants on the pattern of absorption and systemic availability of ABZ and its metabolites in cattle was characterized in the current trial. Twenty (20) parasite-free Holstein calves (100-120 kg) were randomly allocated into four groups and treated intraruminally (10 mg/kg) using one of the following ABZ suspensions: control without surfactant (75/25 dimetyl sulphoxide/saline solution) (group A), 5 mM sodium taurocholate (STC) in saline solution (group B), 8.27 mM sodium lauryl sulphate (SLS) in saline solution (group C) and a commercial formulation (Valbazen((R)), Pfizer Inc. SA) (group D). Jugular blood samples were taken over 72 h post-treatment and plasma analysed by HPLC. Albendazole sulphoxide (ABZSO) and sulphone were the metabolites found in plasma. STC did not affect ABZ absorption while increased ABZSO peak plasma concentration (C(max)) (158% higher, P