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首页> 外文期刊>Crystal growth & design >Two anhydrous and a trihydrate form of tilorone dihydrochloride: Hydrogen-bonding patterns and reversible hydration/dehydration solid-state transformation
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Two anhydrous and a trihydrate form of tilorone dihydrochloride: Hydrogen-bonding patterns and reversible hydration/dehydration solid-state transformation

机译：盐酸替洛龙的两种无水和三水合物形式：氢键模式和可逆的水合/脱水固相转化

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摘要

During the polymorph screening of an active pharmaceutical ingredient tilorone dihydrochloride (chemical name 2,7-bis[2-(diethylamino)ethoxy]-9- fluorenone dihydrochloride) two new polymorphic modifications - III and IV - were obtained. The crystal structures of both polymorphs were established from X-ray powder diffraction. An interesting phenomenon has been observed at ambient conditions for III, which transforms into a novel hydrated form IIIh during 2-3 h when the humidity in the storage room increases to 70% or more. As soon as the relative humidity falls to 30% or less, IIIh transforms into the parent anhydrous form III within an hour. Form IIIh has been identified as a trihydrate of tilorone dihydrochloride, and its crystal structure has been established from X-ray powder diffraction. On the basis of the crystal structures and hydrogen-bonding patterns, a mechanistic model of reversible hydration/dehydration solid-state transformation III ? IIIh depending on the relative humidity is proposed.
机译：在活性药物成分盐酸替洛龙（化学名称2,7-双[2-（二乙基氨基）乙氧基] -9-芴酮二盐酸盐）的多晶型物筛选过程中，获得了两个新的多晶型物修饰-III和IV-。通过X射线粉末衍射确定两种多晶型物的晶体结构。在环境条件下，III出现了一个有趣的现象，当储藏室中的湿度增加到70％或更高时，该现象在2-3 h内转化为新型的水合形式IIIh。相对湿度降至30％或更低时，IIIh会在一小时内转变为母体无水形式III。晶型IIIh已被确定为盐酸替洛龙的三水合物，其晶体结构已通过X射线粉末衍射确定。根据晶体结构和氢键模式，建立了可逆水合/脱水固相转化的机理模型。建议根据相对湿度IIIh。

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