CONICET | Buscador de Institutos y Recursos Humanos

The sustained therapeutic regimen (3-5 days) proposed in monogastrics to optimize the efficacy of methyl-carbamates benzimidazoles, may result unpractical from the clinical view. Development of new formulations with prolonged permanence of the active moiety at the infection site is a challenge and may result in a shorter therapeutic regimen, with equivalent efficacy. Solids dispersions (SDs) have been proposed as new alternative to improve the dissolution rate of low solubility drugs. In previous in vitro studies, formulations of albendazole (ABZ) with SDs showed higher dissolution, when compared with ABZ conventional formulations. The dissolution profiles indicated that ABZ incorporated in SDs was rapidly released compared with free ABZ. The aims of the present study were: a) to validate a laboratory animal model (mice) to screen the anthelmintic drug absorption pattern and, b) to compare the plasma concentration profiles of two different SD containing ABZ in mice. DSs with ABZ:P188 and ABZ:PEG6000 were prepared by the melting method. One hundred forty four BalbC mice (25 g b.w.) were divided in three groups (n=44) and orally treated with ABZ suspension (25 mg/kg) as follows: Group A, received a SD of ABZ (P188), the Group B was treated with the formulation ABZ:PEG6000 and, the Group C was dosed with ABZ conventional suspension. Blood samples were taken from the eye vein using 4 animals per sampling point, over 12 h post-treatment. Samples were analysed by High Performance Liquid Chromatography. ANOVA test was used for the statistical comparison of different points the concentration vs. time curves. The mice model resulted useful to primary screen different ABZ formulations before using superior species (dogs). The concentration-time curve values obtained for the Group A described significant higher concentrations (P

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