布洛芬-羟丙基-β-环糊精包合物的制备及处方优化  

Preparation and Formula Optimization of Ibuprofen-HP-β-CyD Inclusion Complex

作　　者：徐春红[1] 谢梅[1] 徐力[1] 

机构地区：[1]解放军第452医院,成都610021

出　　处：《中国药师》2009年第11期1585-1588,共4页China Pharmacist

摘　　要：目的:制备布洛芬-羟丙基-β-环糊精(IBU-HP-β-CyD)包合物,提高布洛芬(IBU)在水中溶解度。方法:冷冻干燥法制备IBU-HP-β-CyD包合物,连续变化法确定包合比例,正交设计优化处方,紫外分光光度法测定包合物的载药量和溶解度,差式扫描量热法(DSC)法鉴别包合物的形成。结果:包合比例1:1时载药量最高,所制备的三批包合物平均载药量分别为10.52%、10.21%、10.38%,溶解度分别为46.14,45.42,45.78 mg·ml^(-1)。结论:通过HP-β-CyD的包合作用使IBU的溶解度显著提高。Objective： To prepare the ibuprofen-HP-β-CyD inclusion complex and elevate the dissolubility of IBU. Method： The inclusion complex of ibuprofen HP-β-CyD was produced by lyophillization method. The molar ratio of drug and HP-β-CyD was determined by method of continuous variation. The formula was optimized by orthogonal design. The solubility and the load-drug of IBU-HP-β-CyD inclusion complexes which were identified using differential scanning calorimetry （DSC） were determined by UV. Result： The best molar ratio of drug and HP-β-CyD was 1： 1. The load-drug of IBU-HP-β-CyD in three batches were 10.52%, 10.21%, 10.38% and the solubility were 46.14, 45.42, 45.78 mg.ml^-1 respectively. Conclusion： The solubility of IBU could be elevated significantly using HP-β-CyD.

关 键 词：布洛芬 羟丙基-Β-环糊精 包合物 连续变化法 正交设计 

分 类 号：R944.9[医药卫生—药剂学]