Improving the Dissolution Characteristics of Itraconazole by Formulating Cocrystal with the Use of Appropriate Conformers Using Solvent Evaporation Method
Abstract
Introduction: Itraconazole BCS class II drugs have low solubility. Their solubility improves made cocrystal. Cocrystals can be made by many methods like solvent evaporation, cooling crystallisation, and freeze-drying.
Method: In this study, cocrystals were prepared by slow solvent evaporation method with the use of an appropriate coformer with a suitable stoichiometric ratio and COSMO-RS software. Itraconazole and the coformer were dissolved in the proper solvent or solvent mixture and swirled on a magnetic stirrer for 45 minutes at 600 rpm until the product was totally dry. Cocrystal characterisation was done on this product. To create cocrystals, organic acid coformers such as benzoic acid, salicylic acid, caffeine, oxalic acid, and nicotinamide were utilised. Prepared cocrystals were evaluated on the basis of FTIR spectra, DSC thermogram, powder X-ray diffraction, in vitro dissolution study and saturation solubility study.
Results: The FTIR, DSC, and PXRD results indicated that there was no cocrystallisation in organic acid coformers. The usage of amino acids such as glycine, alanine, cysteine, and proline followed. Of these, glycine and alanine showed promise in FTIR, DSC, PXRD, saturation solubility research, and in vitro dissolution studies. Alanine and oxalic acid showed promising results in powder X-ray diffraction.
Conclusion: In the current study, itraconazole cocrystals were effectively created by slow solvent evaporation and had better-dissolving properties than pure itraconazole. Additionally, it was shown that the manufactured cocrystal had a greater saturation solubility than pure itraconazole. Co-crystallisation is therefore a viable method to enhance medication solubility properties without compromising structural integrity and pharmacological effectiveness.
How to cite this article:
Kanabar V, Radadiya J, Gadhiya H. Improving the Dissolution Characteristics of Itraconazole by Formulating Cocrystal with the Use of Appropriate Conformers Using Solvent Evaporation Method. Chettinad Health City Med J. 2024;13(3):65-74.
DOI: https://doi.org/10.24321/2278.2044.202447
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