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魔芋葡甘聚糖及魔芋葡甘聚糖/黄原胶混合物作为控释给药系统的辅料。小分子药物的扩散。

Konjac glucomannan and konjac glucomannan/xanthan gum mixtures as excipients for controlled drug delivery systems. Diffusion of small drugs.

作者信息

Alvarez-Manceñido Felipe, Landin Mariana, Lacik Igor, Martínez-Pacheco Ramón

机构信息

Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

出版信息

Int J Pharm. 2008 Feb 12;349(1-2):11-8. doi: 10.1016/j.ijpharm.2007.07.015. Epub 2007 Jul 20.

Abstract

Konjac glucomannan (KGM), alone or in combination with xanthan gum (XG), was evaluated as main component of systems capable of controlling the diffusion of small molecules with a view of their use in drug delivery. To provide the study with enough general character, KGM batches were obtained from the three main areas of excipient harmonization (Europe, USA and Japan). The rheological evaluation at physiological temperature of KGM (0.5%, w/v) aqueous dispersions, with or without XG at different ratios, showed significant variability among the three KGMs owing to differences in the acetylation degree. The Japanese and European varieties of KGM synergically interact with XG giving rise to gel formation; the synergism being maximum at a 1:1 ratio. By contrast, the American KGM does not show such effect forming only viscous solutions. Drug diffusion coefficients of theophylline and diltiazem HCl, with different molecular size and net charge, were evaluated in systems containing KGM/XG ratio 1:1. KGM/XG systems were more efficient than the XG alone dispersion for controlling drug diffusion of small molecules because of the gel formation. These results point out the potential of mixtures of some KGM types with XG to develop delivery systems capable of maintaining physical integrity and drug release control for up to 8-h period.

摘要

魔芋葡甘聚糖(KGM)单独或与黄原胶(XG)联合使用,被评估为能够控制小分子扩散的系统的主要成分,以期用于药物递送。为使该研究具有足够的普遍性,KGM批次取自辅料协调的三个主要地区(欧洲、美国和日本)。在生理温度下,对含或不含不同比例XG的0.5%(w/v)KGM水分散体进行流变学评估,结果显示,由于乙酰化程度不同,三种KGM之间存在显著差异。日本和欧洲品种的KGM与XG协同相互作用,形成凝胶;在1:1比例时协同作用最大。相比之下,美国的KGM仅形成粘性溶液,未显示出这种效果。在含有1:1比例KGM/XG的系统中,评估了不同分子大小和净电荷的茶碱和盐酸地尔硫䓬的药物扩散系数。由于形成了凝胶,KGM/XG系统在控制小分子药物扩散方面比单独的XG分散体更有效。这些结果指出了某些类型的KGM与XG的混合物在开发能够在长达8小时内保持物理完整性并控制药物释放的递送系统方面的潜力。

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