Department of Pharmaceutical Technology, University of Szeged, Szeged, Hungary.
Pharm Dev Technol. 2012 Mar-Apr;17(2):204-11. doi: 10.3109/10837450.2010.531734. Epub 2010 Nov 10.
The aim of this study was to investigate the effects of alkalizing components and the nature of the wetting liquid on the properties of matrix pellets prepared by extrusion and spheronization. Atenolol was used as an active pharmaceutical ingredient, ethylcellulose as a matrix former, microcrystalline cellulose as a filler and disodium phosphate anhydrous and trisodium phosphate dodecahydrate as alkalizing materials. Water and a water-ethanol mixture served as granulation liquids. Pellet formation was evaluated via mechanical, dissolution and morphological studies. In order to enhance the dissolution of Atenolol from the pellets, alkalizing components were used and the influence of these components on the pH was tested. Investigations of the breaking hardness, the morphology and the dissolution revealed that the pellets containing trisodium phosphate dodecahydrate and prepared with a higher amount of water as binding liquid displayed the best physico-chemical parameters and uniform dissolution. In in vitro experiments, the dissolution release complied with the texture of the pellets and the effect of pH. The pellets have suitable shape and very good hardness for the coating process and are appropriate for subsequent in vivo experiments.
本研究旨在探讨碱化成分的性质和润湿液对挤出滚圆法制备基质丸的性质的影响。阿替洛尔被用作活性药物成分，乙基纤维素作为基质形成剂，微晶纤维素作为填充剂，无水磷酸二氢钠和十二水合磷酸三钠作为碱化材料。水和水-乙醇混合物用作造粒液。通过机械、溶解和形态学研究评估了丸粒的形成。为了提高阿替洛尔从丸粒中的溶解速率，使用了碱化成分，并测试了这些成分对 pH 值的影响。对破碎硬度、形态和溶解的研究表明，含有十二水合磷酸三钠且使用更多的水作为结合液制备的丸粒显示出最佳的物理化学参数和均匀的溶解速率。在体外实验中，释放符合丸粒的质地和 pH 值的影响。这些丸粒具有适合包衣过程的合适形状和非常好的硬度，适合随后的体内实验。
