Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.
Drug Dev Ind Pharm. 2012 Feb;38(2):209-26. doi: 10.3109/03639045.2011.597400. Epub 2011 Nov 16.
In recent years, coprocessing has been the most successful approach to improve and correct the functionality of excipients. The aim of this study is to coprocessed cellulose II with SiO(2) and to evaluate the resulting powder and tableting properties.
Novel cellulose II:SiO(2) (98:2, 95:5, 90:10 and 80:20 w/w ratios) composites were produced by spray drying, wet granulation and spheronization techniques and the resulting powder and tableting properties were assessed.
Cellulose II:SiO(2) composites produced by spray- drying exhibited spherical/oblongate shape, narrow distribution and mean diameter from 51 to 75 µm. The composites produced by wet granulation had larger distribution, granular shape and a mean diameter from 105 to 129 µm. The spheronized composites showed the highest size (from 148 to 450 µm) and round shape. Bulk and tap densities and flow were reduced as the silicification level increased in the spray dried and wet granulated materials. Likewise, silicification increased the true density, porosity and surface roughness of these materials. Water sorption decreased only at silicification level of 20% being comparable to the ones shown by Prosolv(®) samples. Contact angles of all cellulose II materials were lower than those of cellulose I except for Celphere203 indicating better wettability. A 5% and 10% silicification levels rendered the strongest compacts for the spray dried and wet granulated materials, respectively. Silicification did not affect the fast disintegration properties of MCCII.
Coprocessing proved to be useful tool to modify the powder and tableting properties of cellulose II.
近年来，共处理已成为改善和纠正赋形剂功能最成功的方法。本研究的目的是共处理纤维素 II 与 SiO(2)，并评估所得粉末和压片性质。
采用喷雾干燥、湿法制粒和造粒技术制备新型纤维素 II:SiO(2)（98:2、95:5、90:10 和 80:20 w/w 比）复合材料，并评估所得粉末和压片性质。
喷雾干燥制备的纤维素 II:SiO(2)复合材料呈球形/长形，分布狭窄，平均粒径为 51-75 µm。湿法制粒制备的复合材料粒径较大，呈颗粒状，平均粒径为 105-129 µm。造粒的复合材料粒径最大（148-450 µm），形状最圆。喷雾干燥和湿法制粒材料的硅化水平增加时，堆密度和振实密度以及流动性降低。同样，硅化增加了这些材料的真密度、孔隙率和表面粗糙度。仅当硅化水平为 20%时，水分吸湿性才会降低，与 Prosolv(®)样品相当。所有纤维素 II 材料的接触角均低于纤维素 I，除 Celphere203 外，表明润湿性更好。5%和 10%的硅化水平分别使喷雾干燥和湿法制粒材料的压片强度最强。硅化对 MCCII 的快速崩解性能没有影响。
共处理被证明是一种有用的工具，可以改变纤维素 II 的粉末和压片性质。
