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新型壳聚糖-镁铝硅纳米复合膜涂层用于控释片剂。

Novel chitosan-magnesium aluminum silicate nanocomposite film coatings for modified-release tablets.

机构信息

Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.

出版信息

Int J Pharm. 2011 Apr 4;407(1-2):132-41. doi: 10.1016/j.ijpharm.2011.01.049. Epub 2011 Feb 1.

Abstract

Chitosan (CS), a positively charged polysaccharide, and magnesium aluminum silicate (MAS), a negatively charged clay with silicate layers, can electrostatically interact to form nanocomposite films. In this study, CS-MAS nanocomposite films were evaluated for use in tablet film coating. Effects of CS-MAS ratio and coating level on water uptake and drug release from the coated tablets were investigated. Surface and film matrix morphology of the coated film and the effect of enzymes in the simulated gastro-intestinal fluid on drug release were also examined. The results demonstrated that the CS-MAS coated tablets had a rough surface and a layered matrix film, whereas a smooth surface and dense matrix film on the CS coated tablets was found. However, the CS-MAS coated tablets provided fewer film defects than the CS coated tablets. Nanocomposite formation between CS and MAS could retard swelling and erosion of CS in the composite films in acidic medium. The higher MAS ratio of the CS-MAS coated tablets gave lower water uptake and slower drug release when compared with the CS coated tablets. Moreover, the CS-MAS films on the tablets presented good stability towards enzymatic degradation in simulated intestinal fluid. The release of drug from the CS-MAS coated tablets could be modulated by varying CS-MAS ratios and coating levels. Additionally, drug solubility also influenced drug release characteristics of the CS-MAS coated tablets. These findings suggest that the CS-MAS nanocomposites displays a strong potential for use in tablet film coating intended for modifying drug release from tablets.

摘要

壳聚糖(CS)是一种带正电荷的多糖,而硅酸镁铝(MAS)是一种带负电荷的层状硅酸盐黏土,它们可以通过静电相互作用形成纳米复合材料薄膜。本研究评估了 CS-MAS 纳米复合材料薄膜在片剂薄膜包衣中的应用。考察了 CS-MAS 比例和包衣水平对包衣片吸水和药物释放的影响。还研究了包衣膜的表面和膜基质形态以及模拟胃肠液中的酶对药物释放的影响。结果表明,CS-MAS 包衣片具有粗糙的表面和分层的基质膜,而 CS 包衣片则具有光滑的表面和致密的基质膜。然而,CS-MAS 包衣片比 CS 包衣片提供的膜缺陷更少。CS 和 MAS 之间的纳米复合材料形成可以延缓酸性介质中 CS 的溶胀和侵蚀。与 CS 包衣片相比,CS-MAS 包衣片中 MAS 比例较高的片剂吸水率较低,药物释放速度较慢。此外,CS-MAS 薄膜在模拟肠液中对酶降解表现出良好的稳定性。通过改变 CS-MAS 比例和包衣水平可以调节 CS-MAS 包衣片中药物的释放。此外,药物溶解度也影响 CS-MAS 包衣片的药物释放特性。这些发现表明,CS-MAS 纳米复合材料在用于调节片剂药物释放的片剂薄膜包衣中具有很大的应用潜力。

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