羟丙基-β-环糊精包合对茜草双酯的增溶作用  

Effect of hydroxypropyl-β-cyclodextrin on solubility of rubidate

作　　者：肖若蕾[1] 陈莉[1] 

机构地区：[1]咸宁学院药学院,湖北咸宁437100

出　　处：《中国医院药学杂志》2010年第22期1922-1924,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究羟丙基-β-环糊精(HP-β-CD)包合对茜草双酯溶解度和溶出度的增强作用。方法:采用旋转蒸发法制备茜草双酯/HP-β-CD包合物,测定其表观溶解度和体外溶出度,并与茜草双酯原药以及茜草双酯与HP-β-CD的物理混合物的溶出性能进行比较。采用差示扫描量热法(DSC)对包合物进行物相鉴别。结果:茜草双酯原药及其茜草双酯/HP-β-CD不同物质的量比(1:1,1:1.5,1:2)的包合物在37℃时的溶解度分别为18.33,117.81,112.66,100.76mg·L-1,45min时的累积溶出百分率分别为49.99%,90.27%,94.84%,90.78%,包合物的溶出度高于同比例的物理混合物。包合物的DSC曲线中茜草双酯药物的特征峰消失。结论:HP-β-CD可明显增加药物的溶解度和溶出度。ORIECTIVE To investigate the enhancement of dissolution and solubility of rubidate by its complexation with hydroxypropyl-β-cyelodextrinHP -β-CD）. METHODS The inclusion complexes of rubidate/HP-β-CD were prepared by co-evaporating. The apparent solubility and in vitro dissolution characteristics of inclusion complexes were determined and compared with free rubidate and its physical mixture. The binary systems of rubidate and HP-β-CD were characterized by differential scanning calorimetry. RESULTS The apparent solubility of ruhidate and its inclusion complexes prepared from ruhidate and HP-β-CD at different molar ratios（ 1 ： 1,1 ： 1.5,1 ： 2） were 18. 33, 117. 81, 112. 66, 100. 76 mg· L^- 1 at 37 ℃, respectively , ahd their 45 min dissolution rates were 49. 99%, 90. 27%, 94. 84% and 90. 78%, respectively. In the same ratio , the dissolution rates of the inclusion complexes were higher than those of their physical mixtures. Characteristic peak of rubidate in DSC curve of inclusion complex disappeared. CONCLUSION The solubility and dissolution rate of rubidate are increased by HP-β-CD inclusion eomplexation evidently.

关 键 词：茜草双酯 羟丙基-Β-环糊精 包合物 溶解度 溶出度 

分 类 号：R943[医药卫生—药剂学]