摘要
目的制备熊果酸(UA)-磺丁基醚-β-环糊精(SBE-β-CD)包合物,提高熊果酸的溶出度。方法采用溶液搅拌法、超声法和研磨法等3种不同方法比较包合物的制备效果;通过比较,采用溶液搅拌法制备UA-SBE-β-CD包合物,以包合率为指标,考察投料摩尔比、包合温度、包合时间及搅拌速度对包合率的影响,通过正交试验优化工艺;用相溶解度法、差示扫描量热分析法(DSC)与X-射线衍射法(XPD)对包合物进行鉴定;对UA原药、UA与SBE-β-CD的物理混合物及UA-SBE-β-CD包合物进行体外溶出试验,比较其溶出效果。结果采用溶液搅拌法制备的包合物包合率较高、可重复性较好;溶液搅拌法制备UA-SBE-β-CD包合物的最佳包合条件为:UA与SBE-β-CD的摩尔比为1∶4,包合温度为65℃,包合4 h;UA-SBE-β-CD包合物能显著增加UA的体外溶出度。结论溶液搅拌法可用于UA-SBE-β-CD包合物的制备且包合物能明显增加UA的溶出度。
Objective To prepare ursolic acid-sulfobutyl ether-β-cyclodextrin （UA-SBE-β-CD） inclusion complex and to improve the dissolution rate of ursolic acid （UA）. Methods Three methods, including solution mixing method, ultrasonic method and grinding method were used to prepare the inclusion complexes and compare their effects. By comparison, we decided to prepare UA-SBE-β-CD inclusion complex by solution mixing method and the inclusion rate was used as the index. The technological conditions, including the feed molar ratio, inclusion temperature, inclusion time and agitation speed were investigated respectively, and optimized based on the orthogonal experiment. The inclusion complex was identified by phase-solubility method, differential scanning calorimetry （DSC） and X-ray diffraction （XPD） method. The in vitro dissolution of free drug, physical mixture of UA and SBE-β-CD, and UA-SBE-fl-CD inclusion complex were determined. Results The UA-SBE-fl-CD inclusion complex had a higher inclusion rate and a better reproducibility when prepared by the solution mixing method. The optimum condition for preparing UA-SBE-β-CD inclusion complex was A2B3C2： the molar ratio of UA to SBE-β-CD was 1 ： 4, the preparation temperature was 65℃, the time required for preparation was 4 h. Conclusion The UA-SBE-fl-CD inclusion complex can be prepared by the solution mixing method and UA-SBE- β-CD inclusion complex can obviously enhance the dissolution rate of UA.
出处
《中南药学》
CAS
2017年第11期1519-1523,共5页
Central South Pharmacy
关键词
磺丁基醚-Β-环糊精
熊果酸
包合物
正交试验
sulfobutyl ether-β-cyclodextrin
ursolic acid
inclusion complex
orthogonal test
