Amino Acid as Co-Crystal Coformer for Ebastine Solubility Enhancement | ||
| The Egyptian Journal of Hospital Medicine | ||
| Article 136, Volume 90, Issue 2, January 2023, Pages 2900-2908 PDF (1.14 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejhm.2023.287835 | ||
| Authors | ||
| Zainab M. Salih* ; Eman B. H. Al-Khedairy | ||
| 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 | ||
| Keywords | ||
| Ebastine; l-prolin; l-histidin; asparagine; solvent evaporation; liquid assist grinding | ||
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