新型格列吡嗪共晶:绿色超分子机械合成

Dimpy Rani, Sarb Sukhmani Kaur Dargan, Parnika Goyal, R. Chadha
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引用次数: 2

摘要

本研究证实了格列吡嗪(GPZ)与吡啶酸(PA)、己二酸(AA)、异烟酸(INA)、富马酸(FA)和山梨酸(SRA)的五种新型共晶。通过绿色超分子机械合成方法制备了共晶,其化学计量比为1:1。用热(DSC)和光谱(PXRD, FTIR和SSNMR)技术对共晶进行了表征。利用PXRD数据对晶体结构进行了分析。GPZ-PA、GPZ-AA、GPZ-INA、GPZ-FA和GPZ-SRA在P-1、P1和P21空间群中以三斜晶和单斜晶的形式结晶。与GPZ相比,显著改善溶解度和内在溶出率(IDR),显著降低大鼠血清葡萄糖水平和高Cmax。
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Novel Cocrystals of Glipizide: Green Supramolecular Mechanosynthesis
The present research demonstrates the five novel cocrystals of glipizide (GPZ) with picolinic acid (PA), adipic acid (AA), isonicotinic acid (INA), fumaric acid (FA) and sorbic acid (SRA). The cocrystals were prepared via green supramolecular mechanosynthesis approach and exhibited 1:1 stoichiometric ratio. The cocrystals were characterized by thermal (DSC) and spectroscopic (PXRD, FTIR and SSNMR) techniques. PXRD data was used to elucidate the crystal structure. GPZ-PA, GPZ-AA, GPZ-INA, GPZ-FA and GPZ-SRA were found to be crystallized in triclinic and monoclinic crystal systems, which exist in P-1, P1 and P21 space groups. Remarkable improvement in solubility and intrinsic dissolution rate (IDR) was observed along with significant reduction in rat blood serum glucose level and high Cmax in comparison to GPZ.
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