Department of Pharmaceutical, Technology, University of Athens, Greece.
Curr Drug Deliv. 2010 Oct;7(4):334-42. doi: 10.2174/156720110793360568.
The purpose of this research was to develop and evaluate different sustained release preparations, using swellable polymers as carriers in the form of matrices and three-layer tablets. These preparations may offer a number of therapeutic advantages over immediate release dosage forms in drug delivery. The materials used for the fabrication of these systems were hydrophilic swellable polymers namely Metolose, Polyox, Xanthan gum and an erodible material Gantrez, acting as drug(diclofenac sodium) carriers. The powder characteristics determined for these polymers suggest good flowability with the exception of Gantrez. The addition of 1% of magnesium stearate resulted in improved flow properties for all polymers including Gantrez. Tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. Our findings show that both preparations exhibit sustained release characteristics; also the structure of the device considerably affects the drug release and the release rate. Furthermore erosion and swelling greatly influence the overall behavior, function and performance of the systems. Finally kinetic analysis studies indicated that the drug release mechanisms were also affected by these effects.
本研究的目的是开发和评估不同的缓释制剂,使用可溶胀聚合物作为基质和三层片剂的载体。与即时释放剂型相比,这些制剂在药物传递方面可能具有许多治疗优势。用于制造这些系统的材料是亲水性可溶胀聚合物,即甲基纤维素、聚氧、黄原胶和可蚀性材料 Gantrez,用作药物(双氯芬酸钠)载体。这些聚合物的粉末特性表明,除了 Gantrez 之外,它们都具有良好的流动性。添加 1%的硬脂酸镁可改善所有聚合物(包括 Gantrez)的流动性。片剂通过直接压缩制备,而三层片剂则通过在含有药物的核心的两侧压缩聚合物阻隔层来制备。我们的研究结果表明,这两种制剂都表现出缓释特性;此外,装置的结构对药物释放和释放速率有很大影响。此外,侵蚀和溶胀极大地影响了系统的整体行为、功能和性能。最后,动力学分析研究表明,药物释放机制也受到这些影响的影响。