格列吡嗪-β-环糊精包合物的制备及其理化性质考察  

Preparation and Physicochemical Properties of Glipizide- β -Cyclodextrin Inclusion Complex

作　　者：谭丰苹[1] 江田民[1] 蒋国强[1] 昝佳[1] 丁富新[1] 

机构地区：[1]清华大学化工系生物化工研究所,北京100084

出　　处：《精细化工》2004年第3期191-194,共4页Fine Chemicals

基　　金：教育部高等学校博士点专项基金(项目编号20020003056)

摘　　要：研究了格列吡嗪 β 环糊精包合物的制备方法,考察了包合物的理化性质。通过实验优化了格列吡嗪 β 环糊精包合物的制备工艺,确定n(格列吡嗪)∶n(β 环糊精)=1∶2,包合时间为8h;制得产物的包合率为91 73%。HPLC图谱显示,格列吡嗪被β 环糊精包合前后的主成分没有发生变化,包合物的DSC图谱和X射线粉末衍射图谱与格列吡嗪、格列吡嗪 β 环糊精混合物的图谱具有显著性差异。格列吡嗪包合物的溶解度是格列吡嗪的10倍,体外溶出速率有显著提高。实验表明,格列吡嗪被β 环糊精包合后呈现出新的物相特征,与格列吡嗪相比其理化性质有显著的改变。The glipizide- β -cyclodextrin ( β -CD) inclusion complex was prepared with n (glipizide)∶ n(β -CD)=1∶ 2 in time duration of 8 h,and inclusion rate of the inclusion complex was 91.73%.The results of HPLC showed that the main composition of glipizide had no change before and after being included by β -CD.The thermograph of DSC and X-ray powder diffraction pattern of the inclusion complex were remarkably different from those of glipizide and glipizide- β -CD mixture.The water-solubility of the inclusion complex was 10 times that of glipizide, and the dissolution rate of the inclusion complex was significantly increased. It was shown that the glipizide- β -CD inclusion complex exhibited some new physical characteristic and its physicochemical properties were significantly different from those of glipizide.

关 键 词：格列吡嗪 Β-环糊精 包合物 理化性质 

分 类 号：R97[医药卫生—药品]