In this present study a new co-crystals of zoledronic acid with DL-tar的简体中文翻译

In this present study a new co-crys

In this present study a new co-crystals of zoledronic acid with DL-tartaric acid and nicotinamide has been developed with improved solubility. Zoledronic acid is a class III drug with poor oral bioavailability due to its poor permeability and low aqueous solubility; hence an attempt has been made to improve its solubility by co-crystallization technology. Pharmaceutical cocrystals are multi-component crystals with a stoichiometric ratio of active pharmaceutical ingredients (APIs) and cocrystal coformers (CCFs) that are assembled by noncovalent interactions such as hydrogen bonds, π-π packing, and Vander Waals forces. In this study the coformers selected were DL-tartaric acid and nicotinamide based on ease of hydrogen bond formation. The co-crystal of zoledronic acid with DL-tartaric acid were prepared in three ratios (1 : 1, 1 : 2 and 2 : 1) by slow solvent evaporation method and with nicotinamide in 1 : 1 ratio by dry grinding method. The formation of co-crystal was confirmed by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and Fourier transform (FT)IR. The dynamic solubility of co-crystals with DL-tartaric acid in the ratios 1 : 1, 1 : 2 and 2 : 1 increased by fold as compared to pure drug.
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在本研究中,已经开发了唑来膦酸与DL-酒石酸和烟酰胺的新共晶体,具有改善的溶解度。唑来膦酸是一种III类药物,由于其渗透性差和水溶性低,口服生物利用度差。因此尝试通过共结晶技术来提高其溶解度。药物共晶体是具有化学计量比的活性药物成分(API)和共晶体共形成物(CCF)的多组分晶体,它们是通过非共价相互作用(例如氢键,π-π堆积和范德华力)组装而成的。在这项研究中,根据氢键形成的难易程度,选择的共形成剂为DL-酒石酸和烟酰胺。唑来膦酸与DL-酒石酸的共晶体以三种比例(1:1、1、2和2:1)通过慢速溶剂蒸发法,并通过干磨法与烟酰胺以1:1的比例混合。通过粉末X射线衍射法(PXRD),差示扫描量热法(DSC)和傅里叶变换(FT)IR确认了共晶体的形成。与纯药物相比,共晶体与DL-酒石酸的比例为1:1、1:1:2和2:1的动态溶解度增加了几倍。
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In this present study a new co-crystals of zoledronic acid with DL-tartaric acid and nicotinamide has been developed with improved solubility. Zoledronic acid is a class III drug with poor oral bioavailability due to its poor permeability and low aqueous solubility; hence an attempt has been made to improve its solubility by co-crystallization technology. Pharmaceutical cocrystals are multi-component crystals with a stoichiometric ratio of active pharmaceutical ingredients (APIs) and cocrystal coformers (CCFs) that are assembled by noncovalent interactions such as hydrogen bonds, π-π packing, and Vander Waals forces. In this study the coformers selected were DL-tartaric acid and nicotinamide based on ease of hydrogen bond formation. The co-crystal of zoledronic acid with DL-tartaric acid were prepared in three ratios (1 : 1, 1 : 2 and 2 : 1) by slow solvent evaporation method and with nicotinamide in 1 : 1 ratio by dry grinding method. The formation of co-crystal was confirmed by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and Fourier transform (FT)IR. The dynamic solubility of co-crystals with DL-tartaric acid in the ratios 1 : 1, 1 : 2 and 2 : 1 increased by fold as compared to pure drug.
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本文研究了唑来膦酸与DL-酒石酸和烟酰胺共晶体的制备及其溶解性能。唑来膦酸是一种口服生物利用度差的Ⅲ类药物,由于其渗透性差,水溶性差,因此尝试采用共结晶技术提高其溶解度。药物共晶是由非共价相互作用(如氢键、π-π堆积和范德瓦尔斯力)组装而成的多组分晶体,其化学计量比为活性药物成分(api)和共晶共形物(ccf)。在本研究中,根据氢键形成的难易程度,选择了DL-酒石酸和烟酰胺作为共形物。采用慢溶剂蒸发法,以1:1、1:2、2:1三种配比制备了唑来膦酸与DL-酒石酸的共晶,采用干磨法制备了烟酰胺的共晶。用粉末X射线衍射(PXRD)、差示扫描量热(DSC)和傅立叶变换(FT)红外光谱(IR)等方法证实了co晶体的形成。与纯药物相比,DL-酒石酸在1:1、1:2和2:1比例下的动态溶解度增加了一倍。<br>
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