期刊
出版社
INT UNION CRYSTALLOGRAPHY
DOI: 10.1107/S2052520615018582
关键词
ciprofloxacin; salt screening; solubility; solvent drop grinding; solvent evaporation method; APIs
资金
- Ministry of Science and Technology of the People's Republic of China [2012ZX0930101002-001-013, 2013ZX09102110]
- General Administration of Quality Supervision, Inspection, and Quarantine of the People's Republic of China [2012104008-1-14]
With the aim of improving the solubility of ciprofloxacin, polybasic organic acids were utilized to react with ciprofloxacin in different stoichiometric proportions. The use of the solvent drop grinding (SDG) method, as well as the solvent evaporation method, resulted in the crystalline salts ciprofloxacin/fumaric acid (1:1, 2:1), ciprofloxacin/maleic acid (1:1) and ciprofloxacin/citric acid (2:1). The solubilities of these salts in pure water (pH 7.0) were determined using high-performance liquid chromatography (HPLC) at 310 K, with the salts showing considerably greater solubility than ciprofloxacin itself and, interestingly, ciprofloxacin/fumaric acid (2:1) being more soluble than ciprofloxacin/fumaric acid (1:1). Intrigued by this phenomenon, we undertook a comparison of the crystal structures of the salts:the three-dimensional sandwich-like structure observed in the 2:1 salt indicates that the preferred stacking may be a factor in increasing the solubility of ciprofloxacin.
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