热处理对Eudragit RS基体影响的机理评价

Shirzad Azarmi , Fatemeh Ghaffari , Raimar Löbenberg , Ali Nokhodchi
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引用次数: 35

摘要

丙烯酸基体的热处理最近被介绍为一种延长药物释放的工具。在高于聚合物Tg的温度下进行热处理可以降低药物释放速率。本文研究了热处理对Eudragit RS基体的影响机理。以吲哚美辛为模型药。结果表明,热处理后聚合物链的移动和聚合物在片剂基体结构中的重新分布是延长药物释放的可能机制。由于热处理,聚合物的熔化和再固化明显地导致聚合物在整个基质中的重新分布和片剂孔隙率的变化。FTIR结果没有显示任何药物-聚合物相互作用由于热处理。DSC和PXD研究排除了药物的固溶体和多态变化的发生。
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Mechanistic evaluation of the effect of thermal-treating on Eudragit RS matrices

Thermal treatment of acrylic matrices was recently introduced as a tool for prolonging the release of drug. Thermal treatment at temperatures above the Tg 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.

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