The aim of this study was to compare aqueous dispersion and organic solution of Eudragit RS in preparation of sustained release theophylline microparticles using spray drying technique. Spray dried samples (SD) with drug:polymer (D:P) ratios of 1:1, 1:2, 1:3 were prepared using aqueous dispersion (SDaq) or organic solutions of Eudragit RS in ethanol (SDor). Properties of spray dried samples including yield, particle morphology, size distribution and drug dissolution were examined. Differential scanning calorimetry (DSC) and FTIR studies were performed to track any polymorphic changes in drug and/or drug- polymer interaction respectively. The SD samples were compacted and the crushing strengths and release profiles of tablets were determined. The yields of samples were in the range of 33-74%. The yield was higher for SDaq samples, being higher at higher D:P ratios. The SDor samples were smaller in size. SEM images confirmed the formation of spherical particles with somehow different structures for SDaq or SDor samples. Tablets prepared from SDor samples exhibited the highest crushing strengths. In study on release profiles for uncompacted samples, SDor samples exhibited superior sustained release properties. The same results were observed for compacted SD samples. DSC studies showed no polymorphism in SD samples and FTIR analysis showed that there was not any interaction between drug and polymer. In conclusion spray dried samples prepared from organic solution of Eudragit RS had superior sustained release properties and have more potential for application in sustained release formulation of theophylline than aqueous dispersion of the polymer.

译文

这项研究的目的是比较Eudragit RS的水分散体和有机溶液在使用喷雾干燥技术制备缓释茶碱微粒中的应用。使用水分散液 (SDaq) 或eudragitrs在乙醇中的有机溶液 (SDor) 制备具有药物: 聚合物 (D:P) 比率的1:1,1:2,1:3的喷雾干燥样品 (SD)。研究了喷雾干燥样品的性能,包括产率,颗粒形态,尺寸分布和药物溶出度。进行差示扫描量热法 (DSC) 和FTIR研究以分别跟踪药物和/或药物-聚合物相互作用的任何多态性变化。压实SD样品,并确定片剂的压碎强度和释放曲线。样品的产率在33-74% 的范围内。SDaq样品的产率较高,在较高的D:P比下产率较高。SDor样品的尺寸较小。SEM图像证实了SDaq或SDor样品具有不同结构的球形颗粒的形成。由SDor样品制备的片剂具有最高的压碎强度。在研究未压实样品的释放曲线时,SDor样品表现出优异的缓释性能。对于压实的SD样品,观察到相同的结果。DSC研究显示SD样品中没有多态性,FTIR分析表明药物与聚合物之间没有任何相互作用。总之,由Eudragit RS有机溶液制备的喷雾干燥样品具有优异的缓释性能,并且比聚合物的水分散体在茶碱的缓释制剂中具有更大的应用潜力。

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