Lyons John G, Devine Declan M, Kennedy James E, Geever Luke M, O'Sullivan Patrick, Higginbotham Clement L
Centre for Biopolymer and Biomolecular Research, Athlone Institute of Technology, Westmeath, Ireland.
Eur J Pharm Biopharm. 2006 Aug;64(1):75-81. doi: 10.1016/j.ejpb.2006.03.008. Epub 2006 May 11.
The use of filler materials in an extended release monolithic polymer matrix can lead to a vastly altered release profile for the active pharmaceutical ingredient. A range of excipients for use in monolithic matrices have been discussed in the literature. The body of work described in this research paper outlines the use of agar as a novel filler material in a hot melt extruded polymer matrix. Several batches of matrix material were prepared with Diclofenac sodium used as the active pharmaceutical ingredient (API). Agar and microcrystalline cellulose were used as the filler materials in varying ratios, to examine the effect of % filler content as well as filler type on the properties of the hot melt extruded matrix. The resultant extrudates were characterised using steady state parallel plate rheometry, differential scanning calorimetry (DSC) and dissolution testing. The rheometry analysis concluded that the fillers used resulted in an increase in the matrix viscosity. The DSC scans obtained showed negligible effects on the melting behavior of the matrix as a result of the filler inclusion. Dissolution analysis showed that the presence of the fillers resulted in a slower release rate of API than for the matrix alone. The results detailed within this paper indicate that agar is a viable filler for extended release hot melt produced dosage forms.
在缓释整体聚合物基质中使用填充材料可导致活性药物成分的释放曲线发生极大改变。文献中已讨论了一系列用于整体基质的辅料。本研究论文中所描述的工作主体概述了琼脂作为一种新型填充材料在热熔挤出聚合物基质中的应用。以双氯芬酸钠作为活性药物成分（API）制备了几批基质材料。琼脂和微晶纤维素以不同比例用作填充材料，以研究填充剂含量百分比以及填充剂类型对热熔挤出基质性能的影响。使用稳态平行板流变仪、差示扫描量热法（DSC）和溶出度测试对所得挤出物进行表征。流变学分析得出结论，所使用的填充剂导致基质粘度增加。获得的DSC扫描结果表明，由于填充剂的加入，对基质的熔融行为影响可忽略不计。溶出度分析表明，填充剂的存在导致API的释放速率比单独的基质慢。本文详述的结果表明，琼脂是用于热熔生产的缓释剂型的一种可行填充剂。
