Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

Owoyemi Bolaji C. Dayo; da Silva Cecilia C. P.; Souza Matheus S.; Diniz Luan F.; Ellena Javier; Carneiro Renato L.

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Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

机译：氟康唑：四种新药物间形式的合成和结构表征

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Pharmaceutical cocrystals have emerged over the past several decades as an alternative path for synthesizing stable and/or improved crystalline forms of active pharmaceutical ingredients. In this contribution, we developed a reproducible cocrystallization path for the supramolecular synthesis of four new pharmaceutical cocrystal forms of fluconazole (FLZ), an antifungal multifunctional drug: fluconazole- fumaric acid monohydrate (1:1:1), fluconazole-malic acid (1:1), fluconazole- dipicolinic acid (1:1), and fluconazole-adipic acid (1:1). All the new cocrystals were characterized by powder/single-crystal X-ray diffraction, Raman, Fourier transform infrared spectroscopy, differential scanning calorimetry/thermogravimetric analysis, and hot-stage polarized optical microscopy, and their water solubility was determined. Structurally, although the coformers were different, the same strong O-H center dot center dot center dot N hydrogen bond between the FLZ molecule and the coformers was observed. The aqueous solubility studies revealed that all the cocrystals were found to exhibit improved aqueous solubility when compared to the commercialized FLZ polymorph.

机译：在过去几十年中出现了药物池库作为合成稳定和/或改进的结晶形式的活性药物成分的替代路径。在这一贡献中，我们开发了一种可重复的共分子合成的再分子合成四种新的药物碳酰胺形式的氟康唑（FLZ），一种抗真菌多功能药物：氟康唑 - 富马酸一水合物（1：1：1），氟康唑 - 苹果酸（1 ：1），氟康唑-二聚辛酸（1：1）和氟康唑 - 己二酸（1：1）。所有新的聚晶都是通过粉末/单晶X射线衍射，拉曼，傅里叶变换红外光谱，差分扫描量热法/热重分析和热级偏振光光学显微镜，并测定它们的水溶性。在结构上，虽然CoFormers是不同的，但是观察到FLZ分子和共焦型之间的相同强大的O-H中心点中心点中心点N氢键。含水溶解度研究表明，与商业化FLZ多晶型物相比，发现所有钴晶均被发现表现出改善的含水溶解度。

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《Crystal growth & design》 |2019年第2期|共10页
作者
Owoyemi Bolaji C. Dayo; da Silva Cecilia C. P.; Souza Matheus S.; Diniz Luan F.; Ellena Javier; Carneiro Renato L.;
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Fed Univ Sao Carlos UFSCar Dept Chem Rod Washington Luis Km 235 BR-13560905 Sao Carlos SP Brazil;

Fed Univ Sao Carlos UFSCar Dept Chem Rod Washington Luis Km 235 BR-13560905 Sao Carlos SP Brazil;

Univ Sao Paulo Inst Fis Sao Carlos CP 369 BR-13560970 Sao Carlos SP Brazil;

Univ Sao Paulo Inst Fis Sao Carlos CP 369 BR-13560970 Sao Carlos SP Brazil;

Univ Sao Paulo Inst Fis Sao Carlos CP 369 BR-13560970 Sao Carlos SP Brazil;

Fed Univ Sao Carlos UFSCar Dept Chem Rod Washington Luis Km 235 BR-13560905 Sao Carlos SP Brazil;

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正文语种 eng
中图分类晶体学;
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机译：氟康唑：四种新的药物间晶体形式的合成和结构表征
2. Synthesis and Structural Characterization of Cocrystals and Pharmaceutical Cocrystals: Mechanochemistry vs Slow Evaporation A from Solution [J] . Weyna DR, Shattock T, Vishweshwar P, Crystal growth & design . 2009,第2期

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3. New Pharmaceutical Cocrystal Forms of Flurbiprofen: Structural, Physicochemical, and Thermodynamic Characterization [J] . Surov Artem O., Manin Alex N., Voronin Alexander P., Crystal growth & design . 2019,第10期

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Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

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