共研磨法改善水飞蓟素固体分散体的溶出度

Study on the improvement in the dissolution of silymarin solid dispersion prepared by co-grinding method

目的:通过共研磨技术改善水飞蓟素固体分散体的体外溶出度。方法:设计单因素试验考察溶出度的影响因素,如共研磨载体材料的种类及与共研磨药物的比例,研磨的时间等因素。结果:以甘露醇与PVP K30为混合亲水性载体材料,与药物的比例为1∶1∶1,研磨6 h,以pH7.4的磷酸盐缓冲溶液为溶出介质。结论:共研磨法制备水飞蓟素固体分散体能显著提高药物的体外溶出度,且制备工艺简单易行。

OBJECTIVE To improve the dissolution rate of silymarin solid dispersion in vitro by using co-grinding technology.METHODS Single-factor test was employed to investigate the influencing factors of dissolution,such as phases of co-grinding,category of excipients,ratio of silymarin to co-grinding excipients,time of co-grinding,method of dissolution and so on.RESULTS Used mannitol and PVP K30 as complex carriers and silymarin/mannitol/PVP K30 ratio was 1∶1∶1.Time of co-grinding was 6 h and dissolution medium was phosphate buffer（pH 7.4）.CONCLUSION The silymarin solid dispersion prepared by co-grinding method can greatly improve the dissolution.The formulation and technique are simple and can be applicable in production.