基于黄原胶的结肠靶向多颗粒制剂的优化与表征

M Koteswara Rao Sandu , Subhabrota Majumdar , Shayeri Chatterjee , Rana Mazumder
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摘要

优化黄原胶多颗粒制剂并确定其特性,以增加在结肠吸收表面的停留时间,实现结肠靶向治疗。将黄原胶分散在含有药物的冷水中,并使其膨胀 2 小时。海藻酸钠在 10 毫升水中充分混合。将含有药物的黄原胶溶液加入海藻酸钠溶液中,并在不断搅拌的情况下向分散液中加入 0.3 毫升戊二醛。然后,在不断搅拌的情况下,将聚合物-药物溶液滴加到 5% w/v 氯化钙溶液中,用 Whatman 滤纸过滤后,在 30 °C-40 °C 下干燥,得到微球。用戊二醛对微球进行化学交联,在优化的 F6 批次中,随着黄原胶聚合物浓度 0.7% w/v 的增加,药物的最大包埋效率提高到 73.63 ± 0.65%。随着戊二醛浓度的增加,聚合物浓度也随之增加,结果更好。F6 批次的药物释放动力学被视为优化批次,因为在 peppas 模型中发现回归值为 0.997。对优化后的 F6 批次进行了加速稳定性研究,以了解药物在使用期间是否发生变化。多糖在胃肠中保持完整,药物在结肠中释放,毒性低,生物降解性好。本研究表明,优化和表征黄原胶多颗粒制剂用于结肠靶向给药,可使甲硝唑得到最有效和可控的给药。
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Optimization and characterization of xanthan gum based multiparticulate formulation for colon targeting

To optimize and characterize xanthan gum multi-particulate formulation for colon targeting, which increases the residence time at the absorbing surface of the colon. Xanthan gum was dispersed in cold water containing drug and was permitted to expand for 2 ​h. Sodium alginate was blended well in 10 ​ml of water. Xanthan gum solution containing the drug was added to sodium alginate solution and 0.3 ​ml of glutaraldehyde was added to the dispersion, with constant stirring. Then, polymer-drug solution was added dropwise into 5% w/v calcium chloride solution with continuous stirring, producing microspheres filtered by Whatman filter paper and dried at 30 ​°C–40 ​°C. Microspheres were performed by chemical cross-linking with glutaraldehyde, which increased the maximum drug entrapment efficiency up to 73.63 ​± ​0.65% with an increasing concentration of xanthan gum polymer 0.7% w/v for the optimized F6 batch. Better results were found by increasing the polymer concentration along with the glutaraldehyde concentration. The kinetics of drug release for the F6 batch was considered as an optimized batch because the regression value was found to be 0.997 in the peppas model. The accelerated stability study on the optimized F6 batch performed to learn whether the drug has any change during its period of usability. The polysaccharide remains intact in the stomach and intestine and the drug was released in the colon with low toxicity and biodegradability. The present studies showed that optimizing and characterizing xanthan gum multi-particulate formulation for colon targeting gives metronidazole the most effective and controlled delivery.

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