α-常春藤皂苷-羟丙基-β-环糊精包合物的制备及鉴定  

Preparation and Identification of α-Hederagenin-Hydroxypropyl β-Cyclodextrin Inclusion Complex

作　　者：饶涛[1] 李东勋[2] 何秀菊[2] 冯育林[2] 罗晓健[1,2] 

机构地区：[1]江西中医学院,南昌330006 [2]中药固体制剂制造技术国家工程研究中心,南昌330006

出　　处：《中国实验方剂学杂志》2013年第18期1-4,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家"十二五重大新药创制"项目(2012zx09103201-008);江西省科技支撑项目(20111BBG70005-2;20121BBG70019);江西省自然科学基金项目(20122BAB205032)

摘　　要：目的:制备并鉴定α-常春藤皂苷-羟丙基-β-环糊精包合物(BD-HP-β-CD)。方法:采取饱和水溶液法制备BDHP-β-CD,以包合物得率和包封率为指标,通过正交试验考察温度、时间和搅拌速度对包合工艺的影响;采用X-射线衍射法(XRD)及差示扫描量热法(DSC)鉴定包合物物相,相溶解度法考察HP-β-CD对α-常春藤皂苷(BD)的增溶效果。结果:最佳包合工艺为包合温度37℃,搅拌速度300 r·min-1,包合时间2 h,包合物平均得率93.3%,包封率70.7%。BD-HP-β-CD在pH8.5,1.2,6.8介质中表观溶解度较BD分别约提高了4,60,200倍,XRD和DSC中BD的特征峰消失证实包合物已形成。结论:HP-β-CD对BD具有较好的增溶作用。Objective： To prepare and identify α-hederagenin-hydroxypropyl-β-cyclodextrin inclusion complex（BD-HP-β-CD）.Method： BD-HP-β-CD was prepared by saturated aqueous solution.With yield of inclusion complex and entrapment efficiency as indexes,effects of temperature,time and stirring speed on inclusion technology was investigated by orthogonal design.Phase of BD-HP-β-CD was characterized by X-ray diffractometry（XRD） and differential scanning calorimetry（DSC）,solubilization effect of HP-β-CD to BD was investigated by phase solubility method.Result： Optimum inclusion technology was as following： inclusion temperature of 37 ℃,stirring speed 300 r·min-1,inclusion time 2 h.Average yield of inclusion complex was 93.3%,encapsulation efficiency was 70.7%,apparent solubility of BD-HP-β-CD compared to BD in pH 8.5,1.2,6.8 medium increased by about 4,60,200 times,disappearance of BD characteristic peak in XRD and DSC confirmed that inclusion has been formed.Conclusion： HP-β-CD could significantly improve solubility and dissolution of BD.

关 键 词：α-常春藤皂苷 羟丙基-Β-环糊精 包合物 溶解度 

分 类 号：R283.6[医药卫生—中药学] R943[医药卫生—中医学]