目的 考察六味地黄丸粉体粒径与细胞破壁率、体外溶出度之间的关系。方法 采用激光粒度仪和光学显微镜测定4种六味地黄丸粉体(粗粉、细粉、极细粉、微粉)的粒径、细胞破壁率;采用桨法,以马钱苷、丹皮酚为指标,考察上述4种粉体的溶出特征;比较粉体粉碎程度与细胞破壁率、溶出度之间的关系。结果 不同粉碎程度的六味地黄丸粉体的粒径分布、破壁率以及溶出度在一定范围内相关性较强,在该范围内,特征细胞破壁率以及马钱苷、丹皮酚累积释放率都随粉体粒径的减小而提高,而山茱萸、泽泻、牡丹皮微粉的特征细胞破壁率均能达到100%。结论 适度的改变粉碎程度能改变中药细胞破壁率,从而控制中药有效成分溶出的速率和程度。

Objective To investigate the relationship among powder particle size, cell wall-breaking rate, and dissolution of Liuwei Dihuang Pill (LDP) in vitro. Methods Particle size and cell wall-breaking rate of four kinds of LDP were measured by laser particle size instrument and optical microscope. The loganin and paeonol were taken as indexes, the feature of dissolution for the above four kinds of LDP was examined by grouting method. Results There were significant differences in the distribution of particle size, wall-breaking rate, and dissolution among different crushing degrees of LDP. With the decrease of the powder particle size, the wall-breaking rate and relative cumulative dissolution of loganin and paeonol increased. The rate of characteristic cell wall-breaking in the micro powder of Corni Fructus, Alismatis Rhizoma, and Moutan Cortex could reach 100%. Conclusion Moderately changing degree of smash could cause cell wall-breaking rate changes, so as to control effective ingredient the dissolution rate and extent of Chinese medicine.

国家自然科学基金资助项目(81274090);浙江省中医药科技项目(2014ZB129)