Para-Hydroxy Benzoic Acid Coformer Enable Enhanced Solubility, Dissolution, and Antifungal Activity of Ketoconazole Cocrystals

A review on advancement of cocrystallization approach and a brief on screening, formulation and characterization of the same

“…on ketoconazole shows the formation of co-crystal (KTZ:PHBA) with para-hydroxy benzoic acid having ΔpKa of −1.6. The study suggests the formation of co-crystals while having a negative value of ΔpKa, is also possible [ 60 ]. European medicines agency have confirmed that ketoconazole is a dibasic agent and has two pKa values, which are 2.94 and 6.51.…”

“…Mehta et al also concluded that the hepatotoxic activity of ketoconazole was also reduced due to para hydroxyl benzoic acid having hepato-protective properties by performing an in-vitro hepatotoxicity study on a normal Chang liver cell line. In-vitro antifungal activity study shows improvement in the fungicidal activity of KTZ:PHBA co-crystal as compared to ketoconazole and para hydroxybenzoic acid alone [ 60 ].…”