Effect of preparation methods on tosufloxacin tosylate/ hydroxypropyl-β-cyclodextrin inclusion complex

Abstract The main purpose of this work was to compare the effects of the four preparation methods on the TFLX/HP-β-CD inclusion complex. The effects of different preparation methods on the inclusion complex were investigated by SEM, DSC, PXRD, FT-IR and 1H NMR. All the characterization information indicated that the four preparation methods could cause interaction between TFLX and HP-β-CD, but the inclusion complex prepared by solvent evaporation has more reaction sites. Phase solubility experiments demonstrated that the inclusion reaction was spontaneous. In vitro dissolution experiments showed that the dissolution of the inclusion complex in water was: solvent evaporation method (64.39%) > grinding method (42.37%) > ultrasonic method (40.00%) > freezing method (36.08%), and all higher than pure TFLX and physical mixture. These results suggest that the solvent evaporation is the most suitable method for preparing TFLX/HP-β-CD inclusion complexes.

摘要 本研究的核心目的为对比四种制备方法对TFLX/羟丙基-β-环糊精（HP-β-CD）包合物的影响。采用扫描电子显微镜（SEM）、差示扫描量热法（DSC）、粉末X射线衍射（PXRD）、傅里叶变换红外光谱（FT-IR）以及1H核磁共振谱（1H NMR）考察了不同制备方法对该包合物的影响。所有表征结果均表明，四种制备方法均可使TFLX与HP-β-CD之间发生相互作用，但溶剂蒸发法制备的包合物具备更多的反应位点。相溶解度实验证实该包合反应为自发过程。体外溶出实验结果显示，包合物在水溶液中的溶出率依次为：溶剂蒸发法（64.39%）＞研磨法（42.37%）＞超声法（40.00%）＞冷冻法（36.08%），且均高于纯TFLX及物理混合物。上述结果表明，溶剂蒸发法是制备TFLX/HP-β-CD包合物的最优方法。