水飞蓟素固体分散体的制备及溶解性能研究

Preparation of Silymarin Solid Dispersion and Study on Its Solubility

筛选出高分子材料制备水飞蓟素固体分散体,提高水飞蓟素的溶解度和溶出速率。分别采用聚乙二醇6000(PEG6000)、聚维酮K30(PVPK30)为载体,制备水飞蓟素固体分散体。采用高效液相法进行含量测定,差示热分析法鉴别药物在载体中的存在状态,并进行溶解度、体外溶出速率实验。结果表明,两种载体的固体分散体均能增加水飞蓟素的溶解度和溶出速率,水飞蓟素在载体中以高度分散状态存在,而非晶型形态存在。以PVPK30为载体明显优于以PEG6000为载体的水飞蓟素固体分散体体外溶解度和溶出速率。

To select a kind of suitable high polymer material which can be used to prepare silymarin solid dispersions,for improving solubility and dissolution rates of silymarin.The silymarin solid dispersions were prepared with polyethy-leneglycol 6000（PEG6000） and polyvinylpyrrolidone K30（PVPK30） as carriers respectively.HPLC was used to determine the contents of silybin.The physical and chemical properties of silymarin solid dispersions,starting material and physical mixtures were investigated by differential thermal analysis.The solubilities and dissolution rates in vitro were stu-died.Results showed the solubility and dissolution rates of silymarin were enhanced for the formation of silymarin solid dispersions,and silymarin exists in a highly dispersed state in the carriers.The silymarin solid dispersions prepared with PVPK30 can increase the solubility and dissolution rate of silymarin remarkably,superior to PEG6000.