Organic solution versus aqueous dispersion of Eudragit RS in preparation of sustained release microparticles of theophylline using spray drying.
Organic solution versus aqueous dispersion of Eudragit RS in preparation of sustained release microparticles of theophylline using spray drying.
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DOI：
10.1016/j.colsurfb.2013.03.012
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发表时间：
2013-08
期刊：
影响因子：
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通讯作者：
H. A. Garekani;Z. Moghaddam;F. Sadeghi
中科院分区：
文献类型：
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作者：
H. A. Garekani;Z. Moghaddam;F. Sadeghi
采用喷雾干燥法制备缓释茶碱微球，比较了Eudradit RS水分散体法和有机溶液法制备缓释茶碱微球的优劣。用水分散体系(SDaq)或有机乙醇溶液(SDOR)制备了药物：聚合物(D：P)比例为1：1、1：2、1：3的喷雾干燥样品(SD)。考察了喷雾干燥样品的产率、颗粒形态、粒度分布和药物溶出度等性能。差示扫描量热法(DSC)和FTIR研究分别跟踪药物和/或药物-聚合物相互作用中的任何多态变化。将SD样品压实，测定了片剂的粉碎强度和释放度曲线。样品的收率在33-74%之间。SDAQ样品的产率较高，D：P比越高，产率越高。SDR样本的大小较小。扫描电子显微镜照片证实了SDAQOR样品形成了不同结构的球形颗粒。用SDOR样品制备的片剂显示出最高的粉碎强度。在未压实样品的释放曲线研究中，SDOR样品表现出优异的缓释性能。压实的SD样品也观察到了同样的结果。差示扫描量热法(DSC)和傅立叶变换红外光谱(FTIR)分析表明，SD样品中不存在多态现象，药物与聚合物之间没有任何相互作用。综上所述，由Eudradit RS有机溶液制备的喷雾干燥样品具有更好的缓释性能，比聚合物水分散体更有潜力应用于茶碱的缓释制剂。
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 SDaqsamples, being higher at higher D:P ratios. The SDorsamples were smaller in size. SEM images confirmed the formation of spherical particles with somehow different structures for SDaqor SDorsamples. Tablets prepared from SDorsamples exhibited the highest crushing strengths. In study on release profiles for uncompacted samples, SDorsamples 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.