热熔挤出法制备黄连提取物固体分散体的研究

Study on the preparation of solid dispersion of Coptis Extract by hot melt extrusion

目的制备一种可以掩盖苦味的黄连提取物(CoptisExtract,CE)固体分散体。方法以尤特奇E100为分散载体,利用热熔挤出技术制备黄连提取物固体分散体(CE-SD),并采用溶出度试验法、口尝法和形态表征等方法评价掩味效果。结果当CE∶尤特奇E100∶聚乙二醇6000=2∶7∶1(质量比)时,药物在pH=6.8的磷酸盐介质中的溶出率在90 min时可降至10%,尤其在5 min时,溶出度不超过6%。其苦味评分小于0.5分,掩味效果明显。结论热熔挤出法制备的CE-SD可以较好掩盖黄连原有的苦味,且不影响CE在胃肠道的释放行为。

Objective To prepare a solid dispersion that can mask the bitter of Coptis Extract(CE).Methods The solid dispersion of CE was prepared by hot melt extrusion with Eudragit E100 as dispersion carrier,and dissolution test,taste test and morphological characterization were used to evaluate the taste masking effect.Results When mass ratio of CE∶Eudragit E100∶polyethylene glycol 6000 was 2∶7∶1,the dissolution rate of the drug in phosphate medium with pH=6.8 could be reduced to 10%at 90 min,especially at 5 min,the dissolution rate did not exceed 6%.The bitterness score was less than 0.5 points,the taste masking effect was obvious.Conclusion The solid dispersion of CE prepared by hot melt extrusion could conceal the original bitterness of coptis,which doesn’t affect the release of CE in gastrointestinal tract.