羟基红花黄色素A-磷脂复合物及其微丸的制备研究

Study on Preparation of Hydroxysafflor Yellow A-Phospholipid Complex and Its Pellets

目的:确定羟基红花黄色素A-磷脂复合物及其微丸的制备工艺。方法:以羟基红花黄色素A与磷脂的复合率为指标,通过正交试验对羟基红花黄色素A-磷脂复合物的制备条件进行优化。应用挤出-滚圆技术制备羟基红花黄色素A-磷脂复合物微丸,以综合指标为微丸质量评价指标,通过正交试验对制备条件进行优化。使用转篮法考察微丸中羟基红花黄色素A在不同介质中的溶出度。结果:羟基红花黄色素A-磷脂复合物的最佳制备条件为:羟基红花黄色素A与磷脂用量比1∶3,反应时间2小时,反应温度40℃;微丸的最佳制备条件为:黏合剂浓度3%,滚圆时间10分钟,滚圆转速20 Hz。微丸内羟基红花黄色素A在pH分别为6.8和7.4的磷酸盐缓冲溶液及去离子水中均可很好地溶出3,0分钟内溶出度达90%以上。结论:该处方工艺制备的羟基红花黄色素A-磷脂复合物微丸质量符合应用要求。

Objective：To confirm the preparation conditions of hydroxysafflor yellow A（HSYA）-phospholipid（PS） complex and pellets.Methods：The preparation conditions of HSYA-PS complex were optimized by orthogonal design.The recombination rate of HSYA and PS was used to evaluate the complex quality.After the HSYA-PS complex was dissolved in oil,its pellets were prepared by extrusion-spheronization method,then the preparation conditions of pellets were optimized by orthogonal design,with the overall desirability as quality evaluation index.The dissolution of HYSA from the pellets was evaluated by basket method.Results：The optimal preparation conditions of HSYA-PS complex were confirmed,with HSYA-PS ratio of 1 ∶3,reaction time of 2 h,and reaction temperature of 40 ℃;The optimal preparation conditions of pellets were as follows：adhesive concentration of 3%,spheronization time of 10 min,and spheronization speed of 20 Hz.HSYA can release from the pellets effectively in phosphate buffer with pH of 6.8 and 7.4,as well as deionized water.The dissolution of HSYA from the pellets was more than 90% at 30 min.Conclusion：The quality of the HSYA-PS complex pellets prepared under the optimal condition can meet the requirement of application.