Improving Ketoconazole with Fumaric Acid for Better Drug Performance
Author Information
Author(s): Baldea Ioana, Moldovan Remus, Nagy Andras-Laszlo, Bolfa Pompei, Decea Roxana, Miclaus Maria Olimpia, Lung Ildiko, Gherman Ana Maria Raluca, Sevastre-Berghian Alexandra, Martin Flavia Adina, Kacso Irina, Răzniceanu Vlad, Fagadar-Cosma Eugenia-Lenuta, Bora Alina
Primary Institution: Department of Physiology, “Iuliu Haţieganu” University of Medicine and Pharmacy, Romania
Hypothesis
Can the cocrystallization of Ketoconazole with Fumaric Acid enhance its bioavailability and reduce toxicity?
Conclusion
The cocrystal of Ketoconazole and Fumaric Acid shows improved bioavailability and biocompatibility compared to Ketoconazole alone.
Supporting Evidence
- The cocrystal showed a 100-fold increase in solubility compared to pure Ketoconazole.
- Biological assays indicated improved cell viability with the cocrystal.
- In vivo studies demonstrated increased oral bioavailability of Ketoconazole when combined with Fumaric Acid.
- The cocrystal formulation did not induce skin sensitization in mice.
- Molecular docking studies revealed enhanced binding affinity of the cocrystal to the target enzyme.
Takeaway
Researchers combined two substances, Ketoconazole and Fumaric Acid, to make a new medicine that works better and is safer for people.
Methodology
The study involved cocrystallization processes, biological assays on cell cultures, and in vivo testing on rats and mice.
Potential Biases
Potential bias in the selection of animal models and the interpretation of results.
Limitations
The study primarily focused on specific animal models, which may not fully represent human responses.
Participant Demographics
Wistar rats and Balb C mice were used in the study.
Statistical Information
P-Value
0.0012
Statistical Significance
p<0.05
Digital Object Identifier (DOI)
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