Diniz Mariana O, Spoletti Enrico, Ghosh Peuli, Lusi Matteo, Svärd Michael, Rasmuson Åke, Hudson Sarah P
SSPC, the Science Foundation Ireland Research Centre for Pharmaceuticals, University of Limerick, Limerick V94 T9PX, Ireland.
Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick V94 T9PX, Ireland.
Cryst Growth Des. 2023 Nov 15;23(12):8953-8961. doi: 10.1021/acs.cgd.3c01011. eCollection 2023 Dec 6.
This work presents two new solid forms, a polymorph and a solvate, of the antifungal active pharmaceutical ingredient griseofulvin (GSF). The novel forms were characterized by powder X-ray diffraction, differential scanning calorimetry, and thermogravimetric analysis, and their crystal structures were determined by single-crystal X-ray diffraction. The new polymorphic form (GSF Form VI) was obtained upon drying at room temperature the GSF-acetonitrile solvate. GSF Form VI is a relict structure related to reported solvates of GSF. Thermal stability studies show that Form VI is metastable and monotropically related to the stable GSF Form I. The new GSF--butyl acetate solvate was obtained by crystallization from an -butyl acetate solution. The stoichiometry of the -butyl acetate solvate is 1:0.5. The solvate loses the solvent from the crystal lattice at a temperature between 363.15 and 374.15 K.
这项工作展示了抗真菌活性药物成分灰黄霉素（GSF）的两种新的固体形式，即一种多晶型物和一种溶剂化物。通过粉末X射线衍射、差示扫描量热法和热重分析对这些新形式进行了表征，并通过单晶X射线衍射确定了它们的晶体结构。新的多晶型形式（GSF晶型VI）是在室温下干燥GSF - 乙腈溶剂化物后获得的。GSF晶型VI是一种与已报道的GSF溶剂化物相关的残留结构。热稳定性研究表明，晶型VI是亚稳态的，并且与稳定的GSF晶型I呈单向关系。新的GSF - 乙酸丁酯溶剂化物是通过从乙酸丁酯溶液中结晶得到的。乙酸丁酯溶剂化物的化学计量比为1:0.5。该溶剂化物在363.15至374.15 K的温度范围内从晶格中失去溶剂。
