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目的研究注射用多烯紫杉醇-β-环糊精包合物的最佳制备工艺。方法采用溶液-搅拌与冷冻干燥结合的方法 ,以包合物的包合率和溶解度为考察指标,通过正交实验设计,综合平衡后确定最佳制备工艺。结果最佳包合条件为:多烯紫杉醇与HP-β-CD的投料摩尔比为1:12,在25℃条件下以700 r.min-1包合2 h。经红外光谱法、紫外光谱法、光学显微镜法、差示扫描热分析等方法鉴定,确证形成多烯紫杉醇-β-环糊精包合物。结论采用优化条件制备的多烯紫杉醇包合物的包合率达到80%以上,溶解度达4 mg.mL-1。增加了多烯紫杉醇在水中的溶解性,制备工艺简单。
Objective To study the best preparation process of docetaxel-β-cyclodextrin inclusion compound for injection. Methods The method of solution-mixing and freeze-drying was used. The inclusion rate and solubility of the inclusion compound were taken as the investigation indexes. Through the orthogonal experimental design, the optimum preparation process was determined after the balance was comprehensively taken. Results The optimal conditions of inclusion were as follows: the molar ratio of docetaxel to HP-β-CD was 1:12, and the inclusion of docetaxel at 700 r.min-1 for 2 h at 25 ℃. By infrared spectroscopy, ultraviolet spectroscopy, optical microscopy, differential scanning calorimetry and other identification methods, confirmed the formation of docetaxel-β-cyclodextrin inclusion complex. Conclusions The inclusion rate of docetaxel clathrate prepared by the optimized conditions is more than 80%, and its solubility reaches 4 mg.mL-1. Increased docetaxel solubility in water, the preparation process is simple.