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美沙拉嗪从聚合物包衣且载药的SBA - 16体系中的pH依赖性释放。

A pH dependent delivery of mesalazine from polymer coated and drug-loaded SBA-16 systems.

作者信息

Trendafilova Ivalina, Szegedi Ágnes, Yoncheva Krassimira, Shestakova Pavletta, Mihály Judith, Ristić Alenka, Konstantinov Spiro, Popova Margarita

机构信息

Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.

Research Centre for Natural Sciences, Institute of Materials and Environmental Chemistry, Hungarian Academy of Sciences, 1117 Budapest, Magyar tudósok körútja 2, Hungary.

出版信息

Eur J Pharm Sci. 2016 Jan 1;81:75-81. doi: 10.1016/j.ejps.2015.10.003. Epub 2015 Oct 8.

Abstract

SBA-16 silica was synthesized and modified by post-synthesis method with amino groups. Wet milling in acidic media was applied for loading of poorly soluble drug mesalazine (5-aminosalicylic acid — 5-ASA) in different drug/carrier ratios (1:1; 0.75:1; 0.5:1; 0.25:1). The parent and drug loaded mesoporous silicas were characterized by XRD, TEM,N2 physisorption, thermal analysis, FT-IR and solid state NMR spectroscopy. The drug loaded mesoporous systems were single-coated with Eudragit S or double-coated with Eudragit S and Eudragit RL. The polymer coating significantly modified the rate of mesalazine release fromS BA-16NH2 materials. Applying the double coating method makes possible the sustained delivery of the drug in the intestinal area avoiding the burst release in the gastric fluid. The functionalized, polymer coated mesoporous system could be considered an appropriate oral delivery system for mesalazine. In addition, reduction of mesalazine cytotoxicity on epithelial cells could be achieved by its loading into mesoporous silica particles.

摘要

采用后合成法合成并对SBA - 16二氧化硅进行氨基改性。在酸性介质中进行湿磨,以不同药物/载体比例(1:1;0.75:1;0.5:1;0.25:1)负载难溶性药物美沙拉嗪(5 - 氨基水杨酸 - 5 - ASA)。通过XRD、TEM、N₂物理吸附、热分析、FT - IR和固态NMR光谱对母体和载药介孔二氧化硅进行表征。载药介孔体系用Eudragit S单包衣或用Eudragit S和Eudragit RL双包衣。聚合物包衣显著改变了美沙拉嗪从SBA - 16NH₂材料中的释放速率。采用双包衣法可使药物在肠道区域实现持续释放,避免在胃液中出现突释。功能化、聚合物包衣的介孔体系可被认为是美沙拉嗪合适的口服给药系统。此外,将美沙拉嗪负载到介孔二氧化硅颗粒中可降低其对上皮细胞的细胞毒性。

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