卡维地洛羟丙基-β-环糊精包合物的制备与评价  

Preparation and Evaluation of Carvedilol Hydroxypropyl-β-Cyclodextrin Inclusion Complex

作　　者：周洁[1] 蒋曙光[1] 周建平[1] 

机构地区：[1]中国药科大学,南京210009

出　　处：《中国现代应用药学》2012年第6期516-519,共4页Chinese Journal of Modern Applied Pharmacy

基　　金："重大新药创制"科技重大专项(2009ZX09310-004)

摘　　要：目的制备卡维地洛羟丙基-β-环糊精包合物,对包合物进行物性研究。方法采用超声法制备包合物,通过相溶解度研究包合类型,以差示扫描热分析法(DSC)和X-射线衍射法验证卡维地洛羟丙基-β-环糊精包合物的形成,并测定包合物的溶解度和溶出度。结果相溶解度曲线呈AL型,表明卡维地洛能够与羟丙基-β-环糊精形成1∶1的包合物。DSC和X-射线衍射结果显示药物峰消失,证明包合物的形成。包合物的溶解度比原药提高5倍,溶出速度明显加快。结论超声法制备的卡维地洛羟丙基-β-环糊精包合物能显著提高原药的溶解度和溶出速度。OBJECTIVE To prepare carvedilol hydroxypropyl-β-cyclodextrin（HP-β-CD） inclusion complex by ultrasonic method and to investigate its physical properties. METHODS The inclusion complex was prepared by ultrasonic method and analyzed by DSC, XRD, phase solubility and dissolution test. RESULTS The solubility of carvedilol increased with increasing HP-β-CD concentration, showing an ALtype phase solubility diagram which revealed that the molar ratio of drug to HP-β--CD was 1 ： 1. The drug peak disappeared in the DSC and XRD which approved that the inclusion complex was prepared. CONCLUSION By forming inclusion complex with HP-β-CD, the solubility and dissolution rate of carvedilol was increased.

关 键 词：卡维地洛 羟丙基-Β-环糊精 包合物 

分 类 号：R943.4[医药卫生—药剂学]