Novel solid forms of lonidamine: crystal structures and physicochemical properties

作者:Mapp Lucy K; Coles Simon J; Aitipamula Srinivasulu*
来源:CrystEngComm, 2017, 19(21): 2925-2935.
DOI:10.1039/c7ce00651a

摘要

Lonidamine finds potential applications in cancer treatments, and its current marketed solid form, the sodium salt, displays poor solubility. The presence of a single carboxylic acid group makes it an ideal target for co-crystal design as design strategies involving carboxylic acid groups are well-established. CSD statistics combined with known hydrogen bonding preferences allowed suitable co-former selection which resulted in nine new multicomponent crystals with pharmaceutically acceptable co-formers. These included co-crystals, salts and some hybrid (co-crystal salt) structures. All the solid forms were characterized by X-ray diffraction techniques with subsequent measurement of physicochemical properties, such as stability, solubility, and dissolution rate. It was found that the co-formers were able to modulate the properties of lonidamine.

  • 出版日期2017-6-7