Enhancement of solubility of antifungal Ketoconazole By Co-crystallization and Microemulsion

eman ahmad jameel shqirat
ايمان احمد جميل اشقيرات
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Al-Quds University
his study aims to synthesize and characterize cocrystal of ketoconazole to improve solubility properties of ketoconazole. Ketoconazole cocrystal synthesized by the solvent crystallization method and characterized using FTIR spectroscopy,DSC, melting point and solubility analysis. Synthesized co-crystal have wonderful crystals. FTIR spectrum show hydrogen bonding in the co-crystal, which gives it better physical properties (such as solubility, and melting point) compared to single component. Melting point was 146.0°C -148.0°C For the single API, after co-crystallization, it became (141.0 - 143.0 C) and (115.0-119.0 °C ) for subreic acid and sebacic acid co-crystals respectively .The ketoconazole co-crystal resulted in an improved solubility compared to ketoconazole. This research demonstratesthat co-crystallization between ketoconazole and suberic acid, sebacic acid and different co-solvent were effectively formed and enhanced the solubility of the drug. In addition, this research aims to prepare microemulsion of ketoconazole with a different formulations applied using the minimal amount of surfactant at ambient temperature by titration method.The effect of different percentages of co-surfactants &co-solvent on the phase behavior of the systems suggested at ambient temperature were also studied. The surfactant used in this research was Polyoxyethylene sorbitan monooleate (Tween 80). Short chain alcohol used as a co-surfactant was ethanol. The oil phase used was oleic acid. The aqueous phase was double distilled water with propylene glycol acting as co-solvent. The formulation which showed the area covered under the microemulsion was found to be larger in presence of higher amount of surfactant than co-surfactant.The surfactant /co-surfactant ratio (3:1) was found to be more efficient than the ratio (1:1) in formation of isotropic microemulsion region and produced liquid crystal region. The formulation which has propylene glycol as co-solvent gave large area of liquid crystal and microemulsion compared with the absence co-solvent.