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化学交联法延长基于果胶的递药系统中双氯芬酸钠的释放。

Chemical cross-linking approach for prolonging diclofenac sodium release from pectin-based delivery system.

机构信息

College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.

College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.

出版信息

Int J Biol Macromol. 2019 Sep 15;137:512-520. doi: 10.1016/j.ijbiomac.2019.07.011. Epub 2019 Jul 2.

Abstract

To overcome the instability of pectin-Ca gels based oral colon-specific drug delivery system (OCDDS) in the upper gastrointestinal tract, the chemical cross-linked pectin carriers were prepared by adding succinic anhydride and glutaric dialdehyde as the cross-linking reagents. The diclofenac sodium was employed as the water-soluble drug model to calculate the controlled release properties. The encapsulation efficiency and loading efficiency were measured and the sample PG1 shows the best efficiency of 78.81% and 7.78%, respectively. The simulative release rate was estimated and the cumulative release rate of sample PG reached to a maximum of 3.04, 3.66 and 79.43% in SGF, SSIF and SCF. The release data was employed to fit the First order, Higuchi, Bhaskar, and Ritger-peppas model and the goodness of the fit was calculated by the regression coefficient. The succinic anhydride and glutaric dialdehyde cross-linked pectin were characterized by FTIR to prove the cross-linking reaction. In addition, FE-SEM characterization of sample PG1 indicated the rally microsphere with smooth surface. The sample PG1 after the digestion was also characterized by the FE-SEM, and irregularly structure was obtained.

摘要

为了克服果胶-Ca 凝胶在上消化道中不稳定的问题,本研究采用琥珀酸酐和戊二醛作为交联试剂,制备了化学交联的果胶载体。以双氯芬酸钠为水溶性药物模型,计算了控制释放性能。测量了包封效率和载药效率,样品 PG1 表现出最好的效率,分别为 78.81%和 7.78%。估计了模拟释放率,样品 PG 在 SGF、SSIF 和 SCF 中的累积释放率分别达到 3.04%、3.66%和 79.43%。通过回归系数计算了拟合度,将释放数据拟合到一阶、Higuchi、Bhaskar 和 Ritger-peppas 模型中。采用傅里叶变换红外光谱(FTIR)对琥珀酸酐和戊二醛交联的果胶进行了表征,以证明交联反应的发生。此外,通过 FE-SEM 对样品 PG1 进行了表征,结果表明其为表面光滑的团聚微球。对经过消化的样品 PG1 也进行了 FE-SEM 表征,得到了不规则的结构。

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