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KMID : 1146920180480050541
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Journal of Pharmaceutical Investigation
2018 Volume.48 No. 5 p.541 ~ p.549
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Synthesis, solid state characterization and antifungal activity of ketoconazole cocrystals
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Kamble R. N.
Bothiraja C.
Mehta P. P.
Varghese V.
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Abstract
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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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KEYWORD
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Ketoconazole, Crystal engineering, Co-crystals, Solvent crystallization and antifungal activity
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