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热治疗对聚丙烯酸树脂RS基质影响的机理评估

Mechanistic evaluation of the effect of thermal-treating on Eudragit RS matrices.

作者信息

Azarmi Shirzad, Ghaffari Fatemeh, Löbenberg Raimar, Nokhodchi Ali

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran.

出版信息

Farmaco. 2005 Nov-Dec;60(11-12):925-30. doi: 10.1016/j.farmac.2005.07.009. Epub 2005 Oct 11.

Abstract

Thermal treatment of acrylic matrices was recently introduced as a tool for prolonging the release of drug. Thermal treatment at temperatures above the T(g) of the polymer can decrease drug release rate. In this research we studied the mechanism of the effect of thermal treatment on Eudragit RS matrices. Indomethacin was used as model drug. The results showed that polymer chain movement and redistribution of the polymer in the tablet matrix structure after thermal-treating is the possible mechanism of drug release prolongation. The melting and resolidification of the polymer, due to the thermal treatment has apparently resulted in a redistribution of the polymer throughout the matrix and a change in the porosity of the tablet. FTIR results did not show any drug-polymer interaction due to heat-treatment. DSC and PXD studies ruled out the occurrence of solid solution and polymorphic change of the drug.

摘要

丙烯酸酯基质的热处理最近被引入作为延长药物释放的一种手段。在高于聚合物玻璃化转变温度(T(g))的温度下进行热处理可以降低药物释放速率。在本研究中,我们研究了热处理对Eudragit RS基质影响的机制。吲哚美辛用作模型药物。结果表明,热处理后聚合物链的运动以及聚合物在片剂基质结构中的重新分布是药物释放延长的可能机制。由于热处理导致的聚合物的熔化和再固化显然导致了聚合物在整个基质中的重新分布以及片剂孔隙率的变化。傅里叶变换红外光谱(FTIR)结果未显示出由于热处理而产生的任何药物 - 聚合物相互作用。差示扫描量热法(DSC)和粉末X射线衍射(PXD)研究排除了药物固溶体的形成和多晶型变化的发生。

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