热熔挤出法制备的双氯芬酸钠固体分散体系的溶出度

The Release Behaviors of Diclofenac Sodium Solid Dispersion Prepared by Ho-t Melt Extrusion Method

选用聚乳酸(PLA)为骨架基体,聚乙二醇(PEG)6000为致孔剂,用热熔挤出技术(HME)制备了难溶性药物双氯芬酸钠(DS)的固体分散物。通过改变PEG6000与DS含量,比较了对DS体外溶出速率的影响。结果发现,DS的溶出速率随着PEG6000与DS含量的增加而增加,且呈现良好的线性关系。当PLA、PEG6000、DS质量分数为67%、30%、3%时,体系18d药物溶出度为76.5%,若将DS质量分数提高到5%或将PEG6000质量分数提高到40%,则体系分别在4d和3d即达到最大溶出度。文中还对体系中DS的分散机制进行了研究,发现DS主要分散于PEG6000中,而PLA作为骨架材料有效稀释了药物浓度,并延长了药物的释放时间。

The solid dispersion system of poorly water-soluble diclofenac sodium （DS） using polylactic acid （PLA） as polymer matrix and polyethylene glycol （PEG） as pore-making agent was prepared by hot-melt extrusion （HME） method. The dissolution was investigated in vitro by changing PEG and drug load content. The experimental results show that the DS dissolution rate increases with increase of the contents of PEG and drug load, and the dissolution curves are approximately linear~ When the mass ratio of PLA, PEG and DS is 67：30：3, the dissolution rate reaches 7 6.5 % for 18d, but when the mass fraction of DS is increased to 5% or that of PEG is increased to 40%, the maximum dissolution rate is reached for just 4d or 3d, respectively. Furthermore, the dissolution mechanism of DS was also investigated. It is also found that DS mainly is dissolved in PEG at the molecular level, and PLA as the framework material can dilute the DS distribution and prolong the drug release duration.