基于有效成分的溶出性与粉末分散性构建通脉大生片的粉末分散体

Constructing powder dispersion of Tongmai Dasheng Tablets based on dissolution of effective components and dispersibility of medicinal powder

目的改善通脉大生片中丹参与白芍的溶出性,构建优良的粉末分散体。方法采用普通粉碎法及超微粉碎法对白芍、丹参及紫河车进行粉碎,并将六偏磷酸钠(SH)作为粉碎分散剂,共制备19个粉末分散体样品。考察各粉末分散体的粒径分布、红外光谱、分散性,比表面积及孔隙率,采用HPLC法测定丹酚酸B、芍药苷含量,评价不同粉末分散体中丹酚酸B及芍药苷的溶出度。结果红外光谱结果显示超微粉碎、药材混合打粉、SH均没有使药材粉末产生新的物质。丹参-白芍混合超微粉末分散体中丹酚酸B及芍药苷的溶出度最高,丹酚酸B 83.57%,RSD 2.03%;芍药苷80.75%,RSD 0.61%。结论溶出度不仅受粉末比表面积的影响,同时还受到粉末分散性的影响。在改善粉末中有效成分溶出度时,不仅要考虑增大粉末的比表面积,还应改善粉末的分散性。紫河车与丹参-白芍的混合超微粉末中,丹酚酸B、芍药苷溶出度较丹参-白芍混合粉末中两者的溶出度低,因此将紫河车单独粉碎后与另两者混合。

Objective To improve the dissolution of Salviae Miltiorrhizae Radix et Rhizoma（SMRR） and Paeoniae Radix Alba（PRA） in Tongmai Dasheng Tablets（TDT）, and to construct a good powder dispersion. Methods SMRR, PRA, and Placenta Hominis（PH） were crushed by common method and ultramicro method using calgon as a dispersant to prepare 19 powder dispersion samples. The particle size distribution, infrared spectrum, dispersion, specific surface area, and porosity of the powder dispersions were investigated. The contents of salvianolic acid B and paeoniflorin were measured by HPLC, and the dissolution of salvianolic acid B and paeoniflorin in different powder dispersions was evaluated. Results Infrared spectrum results showed that superfine pulverization, mixed comminution or adding the auxiliary pulverizing cannot produce new substances in medicinal powder. The dissolution rate of salvianolic acid B and paeoniflorin in the mixed ultramicro powder dispersions of SMRR and PRA was the highest, salvianolic acid B 83.57%, RSD 2.03%, paeoniflorin 80.75%, RSD 0.61%. Conclusion The dissolution rate is affected not only by the specific surface area of the powder but also by the dispersity of the powder. In order to improve the dissolution rate of active ingredients in powder, it is important to increase the specific surface area of the powder and improve the dispersity of the powder. In the mixed powder of SMRR, PRA, and PH, the dissolution rate of salvianolic acid B and paeoniflorin was lower than that of the mixed powder of SMRR and PRA. Hence, PH was smashed alone, and then mixed with the other two kinds of medicinal powder.