Amorphous Mixtures of Albendazole with Carboxylic Acids By Cogrinding Technique: Solid State Characterizations and In Vitro Efficacy Study


In an attempt to improve the physicochemical properties of poorly aqueous soluble albendazole, its pharmaceutical co-ground amorphous mixtures were successfully formulated with different carboxylic acids like citric acid, benzoic acid, salicylic acid and succinic acid in equimolar ratios by grinding and solvent drop grinding technique without the formation of cocrystals. The physicochemical properties of pure albendazole and corresponding co-ground mixtures were assessed in terms of melting point, drug content, saturation solubility and dissolution studies, Infrared spectroscopy (IR), X-ray powder diffractometry (XRPD) and differential scanning calorimetry (DSC). The results indicated a marked improvement in flow properties and saturation solubility of amorphous mixtures. Further, in the case of dissolution experiments, the amorphous mixtures showed a significant enhancement in the dissolution profiles as compared to pure albendazole. In-vitro anthelmintic, as well as in in-vitro antifungal activity, was also improved. It could be concluded that better improvement of the physicochemical properties of albendazole could be possible with salicylic acid and citric acid using a cogrinding technique. From the present investigation, it could be concluded that it is possible to formulate cogrind amorphous mixtures of albendazole with different carboxylic acids without forming cocrystals still strong agreement to form cocrystals by solubility parameters, structural features.


Albendazole, Amorphous, Dissolution rate, Mxtures, ΔpKa.

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