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Application of slurry bridging experiments at controlled water activities to analyze the phase conversion between anhydrous and hydrated ciprofloxacin

机译:浆料桥接实验在受控水中的应用分析无水水合环丙沙星之间的相转化

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The hydration state of a hydrate depends on the water activity, aw, in the crystallization medium. Selection of an appropriate ratio of water to cosolvent in the crystallization medium of a hydrate is critical. This study attempts to elucidate this selection process by using slurry bridging at controlled water activity and studying the conditions of physical stability of the solid phases of ciprofloxacin, which comprise an anhydrate and a hydrate. If the system is not in equilibrium, a mixture of the anhydrate and the monohydrate may sometimes be obtained. The excess solid phase was characterized by powder X-ray diffractometry (PXRD), thermogravimetric analysis (TGA) and Differential scanning calorimetry (DSC). These results suggest that water activity is the major factor determining the nature of the solid phase of ciprofloxacin which crystallizes from methanol and water. The solubilities of the two solid forms in the mixed solvent system were also measured by HPLC and are discussed. The data suggest that the slurry bridging technique at controlled water activities provides an accurate method of rapidly predicting the physically stable form in anhydrous/hydrate systems.
机译:水合物的水合状态取决于水性活性,在结晶介质中。在水合物的结晶培养基中选择适当的水与太阳能的比例是至关重要的。该研究试图通过在受控水活动中使用浆料桥接并研究环丙沙星的固相的物理稳定性的条件来阐明这种选择过程,其包含一种无水水合物和水合物。如果系统不平衡,则有时可以获得余量和一水合物的混合物。通过粉末X射线衍射法(PXRD),热重分析(TGA)和差示扫描量热法(DSC)的特征过多的固相。这些结果表明,水活性是确定从甲醇和水结晶的环丙沙星固相性质的主要因素。通过HPLC测量混合溶剂系统中两种固体形式的溶解度,并讨论。该数据表明,受控水活动的浆料桥接技术提供了一种快速预测无水/水合物系统中物理稳定形式的准确方法。

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