ArticlePharmaceutical research2025
Pharmaceutical Co-crystal of Ketoconazole-adipic Acid: Excipient Compatibility and In Silico Antifungal Potential Studies.
Article in Pharmaceutical research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
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Who cites it
1 citing paper in PubMed.
- New Miconazole Salts with Heterocyclic Carboxylic Acids with Improved Water Solubility and Enhanced Antifungal Activity.Molecules (Basel, Switzerland) · 2026Article
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Authors and funding
7 authors.
Funding
Abstract
objectiveThis research aimed to investigate the compatibility of the Ketoconazole-Adipic Acid (KTZ-AA) co-crystal, which exhibits an improved dissolution profile over pure Ketoconazole, with various solid pharmaceutical excipients, as well as its in silico antifungal potential.
methodsBinary physical mixtures (1:1 w/w) of KTZ-AA co-crystal and excipients were analyzed using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier-transform infrared spectroscopy (FT-IR), and powder X-ray diffraction (PXRD). The molecular docking study targeting the sterol 14α-demethylase (CYP51) enzyme of the pathogenic yeast Candida albicans was performed.
resultsDSC results indicated compatibility between co-crystal and six tested excipients: lactose monohydrate, polyvinylpyrrolidone K90, microcrystalline cellulose, corn starch, colloidal silicon dioxide, and talc. In the case of the co-crystal and magnesium stearate mixture, DSC revealed a change in the thermal behavior, suggesting the formation of a eutectic system. However, TGA demonstrated that the decomposition profile of the co-crystal remained unaffected in all binary mixtures. PXRD and FT-IR further confirmed the absence of chemical interactions between the co-crystal and all excipients under ambient conditions. Moreover, the KTZ-AA co-crystal maintained its chemical stability without degradation after three months storage under accelerated conditions (40°C/75% RH). The molecular docking study demonstrated that co-crystallization of KTZ with AA enhances its binding affinity to CYP51 enzyme compared to KTZ alone.
conclusionThe excipient compatibility study conducted on the Ketoconazole-Adipic Acid co-crystal confirmed its potential for development as a solid oral dosage form with improved antifungal activity, presenting a promising alternative to the parent drug.
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