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化合物的水合状态有赖于结晶溶媒中水的活度(aH2O).通过制备不同体积比水-有机溶媒的潜溶剂来控制aH2O,用粉末X射线衍射(PXRD)、热重分析(TGA)和差示扫描热量(DSC)等方法表征在具有不同aH2O的水-甲醇中平衡一段时间后的过剩环丙沙星固体的结晶状态.同时采用高效液相色谱测定环丙沙星水合物、无水合物以及它们的混合物在具有不同aH2O的水-甲醇混合溶液中的溶解度.结果表明溶解度变化规律与在相应aH2O的水-甲醇中多余固体的晶型变化规律基本一致.利用实验所得数据构建了环丙沙星无水合物/水合物相稳定性与aH2O的关系图.将该图像与放置于室温以及一定相对湿度条件下时间长达十二周的样品的PXRD数据对比,表明本实验所用的研究方法能够快速、精确地预测无水合物与水合物之间的相互转变过程以及水-有机溶媒的aH2O对它们的相对稳定性的影响.
The hydration state of the compound depends on the activity (aH2O) of water in the crystallization solvent.The aH2O is controlled by preparing the water-organic solvent of the latent solvent at different volume ratios, and the results are analyzed by powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA) Scanning calorimetry (DSC) was used to characterize the crystalline state of excess ciprofloxacin solid after a period of equilibration with different concentrations of aH2O.At the same time, the determination of ciprofloxacin hydrate and hydrate by high performance liquid chromatography As well as the solubility of their mixtures in water-methanol mixed solutions with different concentrations of aH2O.The results show that the variation of solubility is basically the same as that of the excess solids in water-methanol with aH2O.The cyclodextrins Comparison of siloxane anhydrate / hydrate phase stability with aH2O The comparison of the image with the PXRD data of samples placed for 12 weeks at room temperature and at a certain relative humidity shows that the method of study used in this experiment The ability to quickly and accurately predict the interconversion between anhydrates and hydrates and the effect of aH2O in water-organic solvents on their relative stability.