微粉化对穿心莲内酯粉体学性质和溶出度的影响

Infl uence of Micronization of Andrographolide on Micromeritic Properties and Dissolution

采用振动磨制备了穿心莲内酯微粉,并以原药细粉为对照,进行了粉体学性质、溶解度和溶出度的比较研究。结果表明,超微粉碎5 min得到的微粉粒径、松密度与振实密度明显减小(P<0.01),比表面积与孔隙率增大(P<0.01)。两种穿心莲内酯粉末的红外光谱、差示扫描量热曲线和表观溶解度未发生明显变化。溶出试验结果显示,微粉化穿心莲内酯在0.2%十二烷基磺酸钠溶液中的溶出速率明显加快。这些结果提示溶出速率的加快主要是粒径减小、比表面积与孔隙率增大引起的。

The ultrafine powder of andrographolide was prepared by vibromill. The micromeritic properties, solubility and dissolution of the product were compared with those of bulk drug powder. The results showed that the diameter, bulk density and tap density of the powder grinded for 5 min were significantly decreased （P〈0.01）, while the specific surface area and porosity were significantly increased （P〈0.01）. There were no significant differences between these two kinds of andrographolide powder in aspects of IR spectrum, DSC curve and apparent solubility in PBS with different pH values. The results of dissolution test showed that the dissolution rate of the ultrafine powder in 0.2 % SDS increased dramatically. These findings indicated that the decrease of the size distribution and the increase of the specifc surface area and porosity mainly contributed to the dissolution increase in ultrafine powder.