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Pharmaceutical Co-Crystals Of Eprosartan Mesylate:Formulation, Characterization And Evaluation
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| Author:
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DINESHMOHAN S, SANTHOSHA D, LAKSHMI SVVNSM, GUPTA VRM, SUDHA T
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| Abstract:
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The purpose of this study was to increase the solubility and dissolution rate of the drug Eprosartan mesylate, which belongs to the Biopharmaceutical Classification System-II. To improve the solubility and dissolution rate of eprosartan mesylate, the co-crystallization process was opted. The drug cocrystals were formulated by solvent drop grinding method using malic acid as coformer (1:1 ratio). The formulated co-crystals were characterized through various methods, namely differential scanning calorimetry, Fourier transform infrared spectroscopy, light microscopy, and powder X-ray diffraction. The solubility tests of prepared co-crystal were conducted in water, and the in vitro dissolution tests were done in phosphate buffer solution of pH 7.4. The co-crystals displayed new crystalline peaks at 2? values of 7.20, 12.56, 13.98, 14.40, 16.73, 17.76, 18.40, 19.00, 20.1621.07, 22.30, and 24.28 indicated the development of a new crystalline phase. The obtained co-crystals showed the melting point at 98.17oC, which was distinct from that of the pure drug and coformer. The IR spectra of the co-crystals indicated the shifting of absorption peaks of groups of pure components, which reflected the formation of new crystals through hydrogen bond interactions. The solubility and dissolution rate of co-crystals were found to be considerably higher than those of pure drug. The results suggest that co-crystallization process can be the best alternative process for enhancing solubility of poorly soluble drugs.
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| Keyword:
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Co-crystal; eprosartan mesylate; solvent-drop grinding; solubility; dissolution rate
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| EOI:
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-
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.03.175
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| Download:
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