4.5 Article

Two novel ternary albendazole-cyclodextrin-polymer systems: Dissolution, bioavailability and efficacy against Taenia crassiceps cysts

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ACTA TROPICA
卷 113, 期 1, 页码 56-60

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ELSEVIER
DOI: 10.1016/j.actatropica.2009.09.006

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Taenia crassiceps cysts; Albendazole; Ternary systems; Bioavailability

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The effect of two water-soluble polymers: pectin and polyvinylpyrrolidone in combination with beta-cyclodextrin, on the dissolution, bioavailability and cysticidal efficacy of albendazole was evaluated using a commercial suspension as reference product. The dissolution of the albendazole-beta-cyclodextrin-pectin formulation was slow and incomplete (44.7%). No statistical differences in C-max and AUC were found between this formulation and the reference. Also its cysticidal efficacy (33%) was similar to the reference (38%). The albendazole-beta-cyclodextrin-polyvinylpyrrolidone formulation exhibited the highest dissolution rate (78.5%) and its bioavailability was also significantly increased (2.3-fold). In addition, the cysticidal activity of this formulation (83%) was greater than a commercial suspension. Our results suggest that the ternary system of albendazole-beta-cyclodextrin-polyvinylpyrrolidone could be a potential alternative for the treatment of systemic helmintic diseases and it is worth to continue its preclinical evaluation. (C) 2009 Elsevier B.V. All rights reserved.

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