Thommes Markus, Blaschek Wolfgang, Kleinebudde Peter
Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Duesseldorf, Germany.
Eur J Pharm Sci. 2007 Jun;31(2):112-8. doi: 10.1016/j.ejps.2007.02.010. Epub 2007 Mar 6.
kappa-Carrageenan is a new pelletisation aid for the wet extrusion/spheronisation process. Its promising behavior during pelletisation offers a potential replacement of the commonly used microcrystalline cellulose in several formulations. Due to its high water binding, the drying step of the pelletisation has gained increasing attention. Therefore, a systematic investigation of the effect of drying conditions on pellet properties was the aim of this study. Pellets with different formulations were dried in fluid bed, circulation-, and vacuum oven and then characterized by mean dissolution time, tensile strength and disintegration time. Increasing the temperature and duration of the drying process decreased the mean dissolution time, tensile strength and disintegration time of the pellets. The observed effects were attributed to a cautious decomposition of the kappa-carrageenan above 70 degrees C. Furthermore an ionic interaction between calcium ions of dicalciumphosphate and sulfate ester groups of kappa-carrageenan affected the pellet properties like drug release.
κ-卡拉胶是一种用于湿法制粒/滚圆工艺的新型制粒助剂。它在制粒过程中的良好表现为几种制剂中常用的微晶纤维素提供了潜在的替代品。由于其高吸水性，制粒的干燥步骤受到了越来越多的关注。因此，本研究的目的是系统研究干燥条件对颗粒性质的影响。将不同配方的颗粒在流化床、循环烘箱和真空烘箱中干燥，然后通过平均溶出时间、拉伸强度和崩解时间进行表征。干燥过程温度和时间的增加会降低颗粒的平均溶出时间、拉伸强度和崩解时间。观察到的这些影响归因于κ-卡拉胶在70摄氏度以上的缓慢分解。此外，磷酸氢钙中的钙离子与κ-卡拉胶的硫酸酯基团之间的离子相互作用影响了诸如药物释放等颗粒性质。
