热熔挤出法增加布洛芬的溶出度并掩盖其苦味  

Improving dissolution properties and masking bitterness of ibuprofen by hot-melt extrusion

作　　者：王勤[1] 崔岚[1] 

机构地区：[1]上海交通大学医学院附属仁济医院药剂科,上海200001

出　　处：《药学服务与研究》2012年第2期123-125,共3页Pharmaceutical Care and Research

摘　　要：目的:制备布洛芬固体分散体,以增加布洛芬的溶出度并掩盖其苦味。方法:取布洛芬原料药与丙烯酸树脂Eudragit EPO,以1∶1.5(w/w)混合,采用热熔挤出法制备布洛芬固体分散体。用差示扫描量热法和粉末X射线衍射法分析布洛芬在Eudragit EPO中的分散状态。测定固体分散体、物理混合物和市售布洛芬片剂的溶出度,并评价布洛芬固体分散体的掩味效果。结果:布洛芬晶体结构的特征峰在差示扫描量热和粉末X射线衍射图中消失。在磷酸盐缓冲液中,固体分散体的溶出速度大于物理混合物和布洛芬片。志愿者对布洛芬固体分散体的味觉评价优于物理混合物和布洛芬原料。结论:热熔挤出法制备的Eudragit EPO固体分散体能增加布洛芬的溶出度,并有明显的掩味效果。Objective： To prepare the solid dispersions of ibuprofen,in order to improve dissolution properties and mask bitterness of ibuprofen. Methods： Ibuprofen raw materials were mixed with Eudragit EPO in the proportion of 1 to 1.5（w/zc） and the solid dispersions were produced by hot-melt extrusion. The dispersed state of ibuprofen in Eudragit EPO was analyzed by differential scanning calorimetry（DSC） and powder X-ray diffraction method. In vitro drug dissolution rates from ibuprofen solid dispersions, physical mixtures and marketed ibuprofen tablets were determined. In vivo bitterness evaluation of ibuprofen solid dispersions was carried out in healthy volunteers. Results： Specific peak of ibuprofen crystal structure was disappeared in DSC and X-ray diffraction profiles. In phosphate buffer solution,drug released faster from solid dispersions than from physical mixtures and ibuprofen tablets. The taste evaluation in volunteers showed considerable masking of bitterness in solid dispersions com- paring to physical mixtures and ibuprofen raw materials. Conclusion： Hot-melt extrusion process can be employed to form the ibuprofen solid dispersions with Eudragit EPO to improve ibuprofen dissolution properties significantly and to mask the bitterness of ibuprofen.

关 键 词：热熔挤出法 布洛芬 固体分散体 溶出度 掩味 EUDRAGIT EPO 

分 类 号：R944.9[医药卫生—药剂学] R971.1[医药卫生—药学]