逐步回归分析方法研究影响山楂叶颗粒溶出行为的关键颗粒物理特性参数

研究颗粒的关键物理特性参数对山楂叶颗粒溶出行为的影响。以山楂叶提取物为模型药物,将提取物以不同的工艺分别与微晶纤维素或淀粉等比例混合,其中部分混合粉体再加入适量润滑剂和崩解剂,分别采用摇摆挤压与高速搅拌湿法制粒。以金丝桃苷平衡溶出量与溶出速率常数为指标评价颗粒溶出行为,运用逐步回归分析方法分析影响颗粒溶出的关键颗粒物理特性参数。山楂叶颗粒中金丝桃苷平衡溶出量与吸附热常数和单层吸附量呈正相关,与吸湿速率常数呈负相关,溶出速率常数随着Hausner率、单层吸附量和吸附热常数值的增大而减小,随着Carr指数和比表面积的增加而增大。吸附热常数、单层吸附量、吸湿速率常数、Carr指数、Hausner率和比表面积是影响山楂叶颗粒溶出行为的关键颗粒物理特性参数。

Key physical parameters of hawthorn leaf granules by stepwise regression analysis method

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.