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首页> 外文期刊>Crystal growth & design >Co-crystals and co-crystal hydrates of the antibiotic nitrofurantoin: Structural studies and physicochemical properties
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Co-crystals and co-crystal hydrates of the antibiotic nitrofurantoin: Structural studies and physicochemical properties

机译：抗生素呋喃妥因的共晶体和共晶体水合物：结构研究和理化性质

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The current contribution aims to prepare a family of nitrofurantoin (NF) co-crystals and to investigate the ability of these co-crystals in enhancing the photostability and clinically relevant physicochemical properties of NF. Accordingly, supramolecular synthesis of the antibiotic drug NF with the co-formers 3-aminobenzoic acid (3ABA), 4-aminobenzoic acid (4ABA), urea, 4-hydroxybenzamide (4HBAM), phenazine (PHEN), melamine (MELA), 4,4′-bipyridine (BIPY) and 1,2-bis(4-pyridyl ethane) (BIPE) have produced five co-crystals and three co-crystal hydrates. Solid-state physical characterizations have been conducted by powder X-ray diffraction (PXRD), single crystal X-ray diffraction, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), hot-stage microscopy (HSM) and spectroscopy (Raman and ~1H NMR). Crystal structures have been analyzed based on homo- and heterosynthons. Six out of eight multicomponent crystals are primarily stabilized by heterosynthons, whereas the remaining two co-crystals (NF-4ABA and NF-UREA) contain homosynthons. Notably, thermal analysis of co-crystal hydrates showed high thermal stability (166 °C, NF-MELA-H_2O) or upon dehydration provided new anhydrous co-crystals, NF-BIPY and NF-BIPE in a 2:1 molar ratio. Physicochemical properties such as aqueous solubility, intrinsic dissolution rate and photostability have been investigated for NF-3ABA, NF-4ABA, NF-UREA and NF-4HBAM. Co-crystals display enhanced physicochemical properties as compared to that of NF: NF-4HBAM > NF-3ABA > NF-4ABA > NF-UREA > NF (β-form). The results suggest that co-crystals can be a viable alternative for improving the biopharmaceutical properties of API.
机译：目前的贡献旨在制备硝基呋喃妥因（NF）共晶家族，并研究这些共晶增强NF的光稳定性和临床相关理化特性的能力。因此，抗生素分子NF与以下共形成物的3-氨基苯甲酸（3ABA），4-氨基苯甲酸（4ABA），尿素，4-羟基苯甲酰胺（4HBAM），吩嗪（PHEN），三聚氰胺（MELA），4 1,4'-联吡啶（BIPY）和1,2-双（4-吡啶基乙烷）（BIPE）已产生五个共晶体和三个共晶体水合物。通过粉末X射线衍射（PXRD），单晶X射线衍射，差示扫描量热法（DSC），热重分析（TGA），热台显微镜（HSM）和光谱学（Raman and 〜1H NMR）。晶体结构已根据同位和异位合成进行了分析。 8个多组分晶体中有6个主要由杂合子稳定，而其余两个共晶体（NF-4ABA和NF-UREA）含有同合子。值得注意的是，对共晶体水合物的热分析显示出高的热稳定性（166°C，NF-MELA-H_2O），或者在脱水后提供了摩尔比为2：1的新的无水共晶体NF-BIPY和NF-BIPE。已研究了NF-3ABA，NF-4ABA，NF-UREA和NF-4HBAM的理化性质，如水溶性，固有溶解速率和光稳定性。与NF相比，共晶体的理化性能增强：NF-4HBAM> NF-3ABA> NF-4ABA> NF-UREA> NF（β形式）。结果表明，共晶可以作为改善API的生物药物特性的可行替代方法。

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