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Crystal Engineering: A Remedy To Tailor the Biopharmaceutical Aspects of Glibenclamide
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2017-11-27 00:00:00 , DOI: 10.1021/acs.cgd.7b00933
Parnika Goyal 1 , Dimpy Rani 1 , Renu Chadha 1
Affiliation  

New cocrystals of glibenclamide (GCM), namely, glibenclamide–hippuric acid, glibenclamide–nicotinic acid, glibenclamide–theophylline, and glibenclamide–succinic acid, were prepared using solvent assisted grinding. The formation of a new crystalline phase was preliminarily characterized by differential scanning calorimetry and powder X-ray diffraction (PXRD), which was further supported by Fourier transform infrared (FT-IR) spectroscopy and 13C solid state NMR analysis. The crystal structures of these cocrystals were determined from PXRD using BIOVIA material studio software. The data revealed the existence of new hydrogen bond interactions between -NH and the oxygen atom of the sulphamoyl group of GCM with carboxylic -C═O, aromatic N (Naromatic), imidazolic -NH, and carboxylic -OH of cocrystal coformers. Equilibrium solubility and intrinsic dissolution rate studies of cocrystals in phosphate buffer of pH 7.4 showed almost 1.5–3.5 times higher solubility as compared to that of pure of GCM. This further led to improvement in both the rate and extent of absorption, thereby improving bioavailability and remarkable enhancement in antidiabetic activity. These results, therefore, demonstrate that cocrystallization was able to overcome the poor water solubility of GCM and provide a remedy for tuning its biopharmaceutical aspects.

中文翻译:

晶体工程:定制格列本脲生物制药方面的补救措施

使用溶剂辅助研磨制备了新的格列本脲共结晶,即格列本脲-马尿酸,格列本脲-烟酸,格列本脲-茶碱和格列本脲-琥珀酸。通过差示扫描量热法和粉末X射线衍射(PXRD)初步表征了新晶相的形成,并通过傅里叶变换红外(FT-IR)光谱和13 C固态NMR分析进一步证明了这一点。这些共晶体的晶体结构是使用BIOVIA Material Studio软件从PXRD确定的。数据揭示了-NH和GCM的氨磺酰基基团的氧原子与羧基-C═O,芳香族N(N芳香族)之间存在新的氢键相互作用),共晶共成型体的咪唑基-NH和羧基-OH。共晶体在pH 7.4的磷酸盐缓冲液中的平衡溶解度和固有溶解速率研究表明,与纯GCM相比,其溶解度高出近1.5-3.5倍。这进一步导致吸收速率和吸收程度的改善,从而改善了生物利用度并显着增强了抗糖尿病活性。因此,这些结果表明,共结晶能够克服较差的GCM水溶性,并为调节其生物制药方面提供了一种补救方法。
更新日期:2017-11-28
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