羟丙基-β-环糊精对葛根素的增溶作用及其包合物的研制  

Solubilization on puerarin by hydroxypropropyl-β-cyclodextrin and preparation of their inclusion compound

作　　者：宋金春[1] 邓睿园[2] 陈佳丽[2] 赵婧[2] 以盛[2] 

机构地区：[1]武汉大学人民医院药学部,湖北武汉430060 [2]武汉大学药学院,湖北武汉430072

出　　处：《中国医院药学杂志》2008年第13期1070-1074,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备和鉴定葛根素羟丙基-β-环糊精包合物,提高葛根素溶出度。方法:运用相溶解度法进行增溶实验,通过冷冻干燥法制备葛根素羟丙基-β-环糊精包合物;采用X射线衍射,差示扫描量热法,体外溶出度法对包合物进行鉴定。结果:冻干粉经鉴别已形成包合物,葛根素与羟丙基-β-环糊精的包合比例是1∶1,包合物在5min的溶出度可达到原料药的9倍。结论:葛根素与羟丙基-β-环糊精形成包合物后,其溶解度明显增大,能显著提高其溶出度。OBJECTIVE To prepare Puerarin-cyclodextrin indusion compound and improve dissolution of puerarin METHODS Phase solubility studies at pH values （pH 3. 5-5. 5） and physiologically acceptable HP-β-CD-concentrations （0%-25%） were performed, and the amounts of solubilized puerarin quantified by HPLC. The Puerarin-cyclodextrin inclusion compound was prepared with lyophilization technique. The inclusion compound was identified by X-ray diffraction（XRD） and differential scanning calorimetry（DSC） methods and in vitro dissolution test. RESULTS Inclusion ratio of puerarin to HP-β-CD was 1 ： 1. Dissolution of puerarin-HP-β-CD inclusion compound at 5 min was 9 times of drug substanc〈 CONCLUSION An inclusion compound of Puerarin and HP-β-CD can be formed. The solubility and dissolution of puerarin is improved remarkably in puerarin-HP-βCD inclusion compound.

关 键 词：羟丙基-Β-环糊精 葛根素 溶解度 

分 类 号：R943[医药卫生—药剂学]