Abstract
Co-crystallization is a promising technique for improving the biopharmaceutical properties of active pharmaceutical ingredients. The objective of present study was to prepare co-crystals to improve physicochemical properties of BCS class II drug, ketoconazole (KTZ). KTZ co-crystals were prepared with various coformers including oxalic acid, fumaric acid and nicotinamide by solvent crystallization method. The prepared co-crystals were evaluated regarding their thermal properties, crystalline nature, appearance, mean particle size, intrinsic dissolution rate and antifungal potential. The prepared co-crystals demonstrated improved solubility and dissolution rate. Moreover, co-crystals showed good antifungal potential against Candida albicans (MCC 1094). The prepared cocrystals were found to be stable over the period of 6 months verified from stability studies. Therefore, the present study showed that co-crystals may be a potential approach for a BCS class II drug, KTZ.
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The authors would like to acknowledge the support from Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Pune, Maharashtra, India.
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Kamble, R.N., Bothiraja, C., Mehta, P.P. et al. Synthesis, solid state characterization and antifungal activity of ketoconazole cocrystals. J. Pharm. Investig. 48, 541–549 (2018). https://doi.org/10.1007/s40005-017-0346-4
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DOI: https://doi.org/10.1007/s40005-017-0346-4