布洛芬／HP-β-CD包合物固态体系的表征和溶解性能研究

Characteristics and dissolution of ibuprofen/HP-β-CD solid inclusion complex

目的:研究布洛芬／羟丙基-β-环糊精(HP-β-CD)固体包合物的表征与溶解性能的关系。方法:应用X射线衍射、差示热分析、红外光谱、扫描电镜、溶出率测定等物理化学分析方法对不同主客体物质的量比(1:0．5,1: 1,1:2)、不同方法(胶体磨法、研磨法、喷雾干燥法和冷冻干燥法)制备的布洛芬／HP-β-CD包合物进行表征及溶解性能研究。结果:制备方法对各包合物体系的相互作用的表征和溶出速率有显著影响。制备方法显著影响包合物体系内相互作用程度,喷雾干燥制备的体系相互作用程度最强,溶出优劣顺序为:肢体磨>研磨>喷雾干燥>冷冻干燥;对于同一制备条件,提高主客体物质的量比有利于改善包合体系的相互作用和溶出。结论:制备方法和主客体物质的量比可不同程度地影响布洛芬和环糊精的相互作用和布洛芬溶出性能。

Objective： To study the correlation between characteristics of ibuprofen/HP-β-CD solid inclusion complex and its dissolution. Methods： The characteristics and dissolution of ibuprofen/HP-13-CD inclusion complexes, made in different host/guest molar ratios （ 1 ： 0.5, 1 ： 1 and 1 ： 2） and byvarious procedures including colloid grinding, kneading, spray drying and freeze drying, were analyzedusing several physical and chemical analytical methods including DSC, IR, XRPD, SEM and dissolutiontest. Results： The characteristics and dissolution behaviors mainly depended on the preparation proce-dures of the stoichiometric complexes. The best chemical complex was formed using the spray-dryingmethod. The optimal dissolution outcomes was in the order of ground system 〉 kneaded system 〉 spray-dr-ying system 〉 freeze-drying system. In consideration of each preparation procedure, higher host/guestmolar ratios the complex has, better chemical combination and dissolution they are. Conclusion： Prepa-ration procedures and host/guest molar ratios are closely associated with the chemical combination of ibu-profen/HP-β-CD inclusion complex and the dissolution of ibuprofen.