Industrial Pharmacy Lab, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland.
Int J Pharm. 2010 Aug 30;396(1-2):53-62. doi: 10.1016/j.ijpharm.2010.06.009. Epub 2010 Jun 19.
The effect of roller compaction on disintegration time, dissolution rate and compressibility of tablets prepared from theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate was studied. In addition, the influence of adding microcrystalline cellulose, a commonly used excipient, in mixtures with these materials was investigated. Theophylline anhydrate powder was used as a model drug to investigate the influence of different compaction pressures on the tablet properties. Tablets with same porosity were prepared by direct compaction and by roller compaction/re-compaction. Compressibility was characterized by Heckel and modified Heckel equations. Due to the property of polymorphic materials to change their form during milling and compression, X-ray diffraction analysis of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate powders and granules was carried out. After roller compaction the disintegration time and the dissolution rate of the tablets were significantly improved. Compressibility of theophylline anhydrate powder and theophylline anhydrate fine powder was decreased, while theophylline monohydrate showed higher compressibility after roller compaction. Microcrystalline cellulose affected compressibility of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate whereby the binary mixtures showed higher compressibility than the individual materials. X-ray diffraction analyses confirmed that there were no polymorphic/pseudopolymorphic changes after roller compaction.
研究了干法制粒对茶碱无水物粉末、茶碱细粉和茶碱一水合物制备的片剂的崩解时间、溶出速率和可压缩性的影响。此外，还研究了在与这些材料混合时添加常用赋形剂微晶纤维素的影响。茶碱无水物粉末被用作模型药物，以研究不同压缩压力对片剂性质的影响。通过直接压片和干法制粒/再压片制备具有相同孔隙率的片剂。通过 Heckel 和改进的 Heckel 方程来表征可压缩性。由于多晶型材料在研磨和压缩过程中改变其形态的特性，对茶碱无水物粉末、茶碱无水物细粉和茶碱一水合物粉末和颗粒进行了 X 射线衍射分析。干法制粒后，片剂的崩解时间和溶出速率显著提高。茶碱无水物粉末和茶碱无水物细粉的可压缩性降低，而茶碱一水合物在干法制粒后表现出更高的可压缩性。微晶纤维素影响茶碱无水物粉末、茶碱无水物细粉和茶碱一水合物的可压缩性，使得二元混合物的可压缩性高于单一材料。X 射线衍射分析证实，干法制粒后没有多晶型/准多晶型变化。
