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

机译:液固技术以多糖为载体制备消炎痛结肠靶向给药系统

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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:本研究旨在通过应用liquisolid(LS)技术来配制消炎痛(IDM)结肠专用药物递送(CSDD)系统的基质片剂。建立了基于时间依赖性的聚甲基丙烯酸酯和酶降解多糖的CSDD系统。 Eudragit RL 100(E-RL 100)被用作时间依赖性聚合物,而细菌可降解多糖则以载有该药物的LS系统出现。负载吲哚美辛的LS系统是使用瓜耳胶(GG),果胶(PEC)和壳聚糖(CH)的不同多糖分别作为载体或以1:3、1:1和3的不同比例的混合物作为载体制备的:1。在加入计算量的E-RL 100并用硬脂酸镁和滑石粉按1:9的比例润滑后,将在pH 1.2和pH 6.8下均显示出关于药物释放速率的有希望的结果的Liquisolid系统压制成片剂。发现E-RL 100改善了所有LS制剂的流动性和可压缩性。释放数据表明,所有制剂均能在24小时内成功维持药物释放。稳定性研究表明,基于PEC的LS系统及其基质片剂在储存期间(一年)是稳定的,并且可以提供至少两年的保存期限。

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