Evaluating experimental, knowledge-based and computational cocrystal screening methods to advance drug-drug cocrystal fixed-dose combination development

Parkes, Alice; Ziaee, Ahmad; O'Reilly, Emmet

doi:10.1016/j.ejps.2024.106931

European Journal of Pharmaceutical Sciences

2024

DOI: 10.1016/j.ejps.2024.106931

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Evaluating experimental, knowledge-based and computational cocrystal screening methods to advance drug-drug cocrystal fixed-dose combination development

Alice Parkes,

Ahmad Ziaee,

Emmet O'Reilly

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Preparation and Characterization of Apixaban Cocrystals with Coformers for Improving Physical Properties

Al-Najjar,

Abbas,

Ghareeb

2024

Al-Rafidain J Med Sci

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Background: Cocrystals are stoichiometric, multicomponent crystalline materials composed of an active pharmaceutical ingredient (API) and a coformer arranged in a crystalline structure. Apixaban (APX) is an oral blood thinner that has a low aqueous solubility of 0.028mg/mL at 24 °C and a weak oral bioavailability of about 50% for doses below 10 mg, decreasing as doses above 25 mg are taken. Objectives: To develop and assess APX cocrystal to improve its solubility. Methods: Cocrystals of APX with diverse coformers were synthesized using the solvent evaporation technique in varying molar ratios. The structure of the synthesized cocrystals was validated by DSC, PXRD, and FTIR analyses. Saturation solubility of APX and cocrystals in water was also investigated. Results: APX cocrystals with diverse coformers exhibited distinct physicochemical features. The co-crystal of APX with oxalic acid at a 1:1 ratio exhibited a 2.54-fold enhancement in solubility relative to that of pure APX in water. Each coformer enhanced the solubility of the APX co-crystals. The FTIR spectra of the cocrystals indicated no interaction between the APX and the coformers. The DSC analysis revealed distinct endothermic peaks corresponding to its melting point, indicating the development of cocrystals. The PXRD diffractogram demonstrated fluctuation of 2 theta values of peaks and confirmed cocrystallization of APX. Conclusions: Cocrystallization may serve as a potential method to improve the solubility of APX.

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Preparation and Characterization of Apixaban Cocrystals with Coformers for Improving Physical Properties

Al-Najjar,

Abbas,

Ghareeb

2024

Al-Rafidain J Med Sci

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show abstract

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Evaluating experimental, knowledge-based and computational cocrystal screening methods to advance drug-drug cocrystal fixed-dose combination development

Cited by 1 publication

References 183 publications

Preparation and Characterization of Apixaban Cocrystals with Coformers for Improving Physical Properties

Preparation and Characterization of Apixaban Cocrystals with Coformers for Improving Physical Properties

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