热熔挤出技术提高水飞蓟素溶出度的初步研究

目的:研究热熔挤出技术是否提高难溶性药物溶出度.方法:以难溶性水飞蓟素为模型药物,以泊洛沙姆-188为亲水性载体,采用热熔挤出技术和熔融法分别制备挤出物和固体分散体,比较两者的差示扫描量热(DSC)图谱和累积溶出曲线.结果:挤出物是分散程度较高的固体分散体,DSC图谱中药物的吸热峰均消失,载体泊洛沙姆-188的吸热峰向低温方向移动,挤出物中的移行程度大于固体分散体;药物在90 min时从挤出物中溶出90.63%,而在固体分散体中的溶出量为71.06%.结论:热熔挤出技术可提高水飞蓟素的溶出度,且效果优于熔融法.

A preliminary evaluation of hot melt extrusion technology on improvement of silimarin dissolution

Objective:To assess if the hot melt extrusion(HME) technique enhances the dissolution of hydrophobic drugs.Methods:A powder blend of silimarin and poloxamer-188 was hot-melt extruded.The resulting composite rod was cut into cylindrical pellets and then pulverized to power.The same solid dispersion of another powder blend was processed using conventional melting techniques.Differential scanning calorimetry(DSC) and dissolution measurements were employed to explain the differences in drug release rates of silimarin from powders produced by the two processing techniques.Results:The powders prepared from hot-melt extrusion displayed a fine solid particle size distribution in the matrix.No endothermic peaks of the hot-melt extrudates were observed by DSC.The endothermic peaks of the carrier were shifting towards the low temperature region,and such shifting of the extrudate was bigger than that of the other solid dispersion.The drug release rate from the extrudate was 90.63% per 90 minutes and the dissolution of the other solid dispersion was 71.06%.Conclusion:Silimarin's release from the hot-melt extruded power showed significant improvement compared with the conventional melting technique.