Tsai T, Wu J S, Ho H O, Sheu M T
Graduate Institute of Pharmaceutical Sciences, Taipei Medical College, Taiwan, ROC.
J Pharm Sci. 1998 Jan;87(1):117-22. doi: 10.1021/js960486a.
In an attempt to modify the physical properties of microcrystalline cellulose (MCC), the slurry form of this material was codried with beta-cyclodextrin (beta-CD). MCC slurry was blended with beta-CD at concentrations of 10%-50% w/w as a dried mass relative to MCC. The mixtures were then granulated with water and codried at 60 degrees C for 12 h or until a constant weight was reached. Codried granules were pulverized, and the fraction between 61 and 150 microns in size was reserved. The powder and tableting properties of the codried products were compared to those of various grades of MCC and the corresponding components and physical mixtures. The results showed that the products of MCC codried with beta-CD significantly improved the flowability of MCC powder. It is probable that the improved flowability was due to the more rounded shape of particles formed with this codried process, which was confirmed by SEM photographs. Moreover, the compactibility and disintegration properties of tablets produced from the codried products were even better than those using MCC alone, physical mixtures, or various grades of MCC. MCC in a slurry form was more efficient than the existing MCC products in achieving these results, which is postulated to be due to the greater amount of water required and the higher solubility of beta-CD in water promoting the interaction between beta-CD and MCC during granulation. In conclusion, MCC codried with beta-CD provides a useful excipient for direct compression.
为了改变微晶纤维素(MCC)的物理性质,将该材料的浆料形式与β-环糊精(β-CD)共同干燥。将MCC浆料与β-CD以相对于MCC的干燥质量计10%-50% w/w的浓度混合。然后将混合物用水制粒,并在60℃下共同干燥12小时或直至达到恒定重量。将共同干燥的颗粒粉碎,并保留尺寸在61至150微米之间的部分。将共同干燥产品的粉末和压片性能与各种等级的MCC以及相应的组分和物理混合物的性能进行比较。结果表明,与β-CD共同干燥的MCC产品显著改善了MCC粉末的流动性。改善的流动性可能是由于这种共同干燥过程形成的颗粒形状更圆润,扫描电子显微镜照片证实了这一点。此外,由共同干燥产品制成的片剂的可压性和崩解性能甚至优于单独使用MCC、物理混合物或各种等级MCC制成的片剂。浆料形式的MCC在实现这些结果方面比现有的MCC产品更有效,据推测这是由于所需水量更大以及β-CD在水中的溶解度更高,促进了制粒过程中β-CD与MCC之间的相互作用。总之,与β-CD共同干燥的MCC为直接压片提供了一种有用的辅料。