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球芯的浸渍涂层,由壳聚糖和钙组成,用于结肠药物传递。

Immersion coating of pellet cores consisting of chitosan and calcium intended for colon drug delivery.

机构信息

Department of Pharmacy, University of Oslo, Oslo, Norway.

出版信息

Eur J Pharm Biopharm. 2010 Jun;75(2):245-53. doi: 10.1016/j.ejpb.2010.02.012. Epub 2010 Feb 25.

Abstract

Biopolymers such as pectin, alginate, and chitosan have a great potential in colon drug delivery. The aim of this study was to produce pellets with calcium and chitosan in the core and then by an interfacial complexation reaction coat the cores with pectin or alginate in combination with calcium or chitosan. Pellets with calcium in the core acted as a reference. The drug release was investigated in environments mimicking the stomach and the small intestine. The morphology of the coatings indicated a more wrinkled and irregular structure for coatings composed of pectin or alginate in combination with chitosan compared to the coat consisting of alginate in combination with calcium. The results from the drug release experiments showed that all the investigated coatings, especially with alginate, slowed down the drug release compared to the uncoated cores. The release from the chitosan-containing pellets was higher than the reference. The swelling studies revealed a high degree of swelling of the core consisting of chitosan. This probably explains the higher drug release from the coated chitosan pellets.

摘要

生物聚合物,如果胶、藻酸盐和壳聚糖,在结肠药物传递中有很大的潜力。本研究的目的是制备以钙和壳聚糖为核的微丸,然后通过界面复合反应,用果胶或藻酸盐与钙或壳聚糖结合来包衣核心。以含有钙的微丸作为参考。在模拟胃和小肠的环境中研究了药物的释放情况。涂层的形态表明,与由藻酸盐与钙结合形成的涂层相比,由果胶或藻酸盐与壳聚糖结合形成的涂层具有更皱缩和不规则的结构。药物释放实验的结果表明,所有研究的涂层,特别是与藻酸盐结合的涂层,都能减缓药物的释放,与未涂层的核心相比。含壳聚糖的微丸的释放速度高于参考值。溶胀研究表明,由壳聚糖组成的核具有很高的溶胀度。这可能解释了包衣壳聚糖微丸中药物释放较高的原因。

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