Amino Acid as Co-Crystal Coformer for Ebastine Solubility Enhancement

Document Type : Original Article

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Abstract

Background: Ebastine (EB) is a selective, nonsedating H1 antihistamine belonging to Class II(BCS); its insufficient water solubility limits its oral bioavailability. Cocrystal is one of the most modern techniques used to increase the solubility and dissolving rate of a medicine, among other physicochemical properties.
Aim: The primary purpose of this study was to construct and assess EB cocrystal as an experiment to improve its solubility.
Methods: Various processes, such as solvent evaporation and liquid asset grinding with varying molar ratios of amino acid as a co-former, have been used to produce cocrystals. The produced formulations were evaluated by yield %, drug content, saturation solubility, in vitro dissolution tests, Powder X-ray Diffraction (PXRD), and scanning electron microscopy.
Results: Increased solubility by 364 times in distilled water with an improved dissolving profile.
Conclusion: Due to its ability to enhance physicochemical and mechanical qualities, co-crystallization is a promising method for solid formation. Using unique hydrogen bond synthon motifs, co-crystals have been successfully produced from several medications and co-former
 

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The Egyptian Journal of Hospital Medicine
Volume 90, Issue 2
January 2023
Pages 2900-2908

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