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Formulation of Indomethacin Colon Targeted Delivery Systems Using Polysaccharides as Carriers by Applying Liquisolid Technique

机译:通过施加液质溶剂技术,使用多糖作为载体的吲哚美辛结肠靶向递送系统的制剂

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摘要

The present study aimed at the formulation of matrix tablets for colon-specific drug delivery (CSDD) system of indomethacin (IDM) by applying liquisolid (LS) technique. A CSDD system based on time-dependent polymethacrylates and enzyme degradable polysaccharides was established. Eudragit RL 100 (E-RL 100) was employed as time-dependent polymer, whereas bacterial degradable polysaccharides were presented as LS systems loaded with the drug. Indomethacin-loaded LS systems were prepared using different polysaccharides, namely, guar gum (GG), pectin (PEC), and chitosan (CH), as carriers separately or in mixtures of different ratios of 1 : 3, 1 : 1, and 3 : 1. Liquisolid systems that displayed promising results concerning drug release rate in both pH 1.2 and pH 6.8 were compressed into tablets after the addition of the calculated amount of E-RL 100 and lubrication with magnesium stearate and talc in the ratio of 1 : 9. It was found that E-RL 100 improved the flowability and compressibility of all LS formulations. The release data revealed that all formulations succeeded to sustain drug release over a period of 24 hours. Stability study indicated that PEC-based LS system as well as its matrix tablets was stable over the period of storage (one year) and could provide a minimum shelf life of two years.
机译:本研究旨在基质片剂的用于通过应用液固体(LS)技术吲哚美辛(IDM)的结肠特异性药物递送(CSDD)系统中的配制剂。建立了基于时间相关的聚甲基丙烯酸酯和酶可降解的多糖甲CSDD系统。 EUDRAGIT RL 100(E-100 RL)被用作随时间变化的聚合物,而细菌降解的多糖呈现为负载药物LS系统。使用不同的多糖,即,瓜尔胶(GG),果胶(PEC),以及脱乙酰壳多糖(CH)制备吲哚美辛加载LS系统,单独的载体或以不同比率的1的混合物:3,1:1和3 :1.所显示有希望在两个pH值1.2和pH 6.8的有关药物释放速率的结果液固体系统是在1:1的比例加入E-RL 100的计算出的量和润滑与硬脂酸镁和滑石后压制成片剂:9 。结果发现,E-RL 100改善所有LS制剂的流动性和可压缩性。释放数据表明,所有制剂成功历时24小时,以维持药物释放。稳定性研究表明,基于PEC-LS系统以及它的骨架片结束存储(一年)期间稳定和可提供的至少两年的保质期。

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