Cocrystallization of gliclazide with improved physicochemical properties
نویسندگان
چکیده
Abstract Background Cocrystallization is one of the crystal engineering strategies used to alter physicochemical properties drugs that are poorly water-soluble. Gliclazide (GLZ), an antidiabetic drug, belongs Biopharmaceutical Classification System class-II (low solubility and high permeability) has low bioavailability, resulting in poor therapeutic effects patients. Therefore, impart better bioavailability GLZ, study was carried out by preparing GLZ cocrystals using liquid-assisted grinding method with three coformers [3,5-dinitrosalicylic acid (DNS), 2,6-pyridine dicarboxylic (PDA), L-proline (LPN)], these were characterized Differential Scanning Colorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier Transform Infra-red spectroscopy (FTIR), Raman spectral studies. Further, electron microscopy (SEM) analysis, accelerated stability, solubility, vitro dissolution studies, vivo pharmacokinetic studies performed male Wistar rats. Results DSC PXRD analysis confirmed formation cocrystals. Hydrogen bonding between pure its demonstrated based on FTIR analysis. SEM data showed morphological images for differed from those GLZ. In comparison have greatly improved dissolution, profiles. Among three, GLZ–DNS outperformed drug terms (6.3 times), degradation (1.5 relative (1.8 times). Conclusion Hence, cocrystallization leads soluble gliclazide.
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ژورنال
عنوان ژورنال: Future Journal of Pharmaceutical Sciences
سال: 2021
ISSN: ['2314-7245', '2314-7253']
DOI: https://doi.org/10.1186/s43094-021-00261-z