沙拉沙星环糊精包合物的制备与体外释放度研究

为了制备沙拉沙星的新剂型,评价其体外释放度,采用响应面法优化沙拉沙星/β-环糊精包合物微囊的制备条件,用扫描电子显微镜(SEC)进行表征试验,对环糊精包合物微囊的粒径和释放度进行评价。响应面法优化后的参数为沙拉沙星和β-环糊精混合液以300 r/min转速在50℃下搅拌4 h,粒径试验表明包合物粒径平均值为1.0μm。体外释放度试验表明,SAR/β-CD包合物在60 min后累积溶出度达到97%左右并保持稳定,物理混合物60 min后累积溶出度仅63%左右,SAR粉剂在60 min后累积溶出率仅74.4%左右。将沙拉沙星成功制备成一种新型包合物制剂,提高了药物的释放性质,对沙拉沙星的推广具有积极意义。

Preparation,Characterization and in Vitro Drug Release of Sarafloxacin Inclusion Complex

In order to prepare a new dosage form of sarafloxacin,the in vitro release of sarafloxacin was evaluated.The preparation conditions of sarafloxacin/β-cyclodextrin inclusion complex microcapsules were optimized by response surface method.The characterization experiment was carried out by scanning electron microscope(SEC).The particle size and release of cyclodextrin inclusion complex microcapsules were evaluated.The optimized parameters of response surface method were as follows:the mixture of sarafloxacin andβ-cyclodextrin was stirred at 50℃for 4 h at 300 r/min.The particle size experiment showed that the average particle size of the inclusion complex was 1.0μm.The in vitro release experiment showed that the cumulative dissolution of SAR/β-CD inclusion complex reached about 97%and remained stable after 60min,the cumulative dissolution rate of physical mixture after 60min was only about 63%,and the cumulative dissolution rate of SAR powder after 60min was only about 74.4%.Sarafloxacin was successfully prepared into a new type of inclusion complex preparation,which improved the release properties of the drug and was of positive significance to the popularization of sarafloxacin.