Department of Pharmaceutics, S.S.R. College of Pharmacy, Saily-Silvassa Road, Saily, Silvassa 396230, U.T. of Dadra and Nagar Haveli, India.
Department of Pharmaceutics, S.S.R. College of Pharmacy, Saily-Silvassa Road, Saily, Silvassa 396230, U.T. of Dadra and Nagar Haveli, India.
Carbohydr Polym. 2014 Nov 26;113:138-48. doi: 10.1016/j.carbpol.2014.06.061. Epub 2014 Jul 1.
The study shows the development and optimization of locust bean gum (LBG)-alginate mucoadhesive macromolecules containing aceclofenac through ionotropic-gelation using 3(2) factorial design. The effect of amount of LBG and sodium alginate on drug entrapment efficiency (%DEE), % mucoadhesion at 8h (M8) and % in vitro drug release at 10h (%Q10h) were optimized. The percentage yield, average size and DEE of macromolecules were found within the range of 93.19 to 96.65%, 1.328 ± 0.11 to 1.428 ± 0.13 μm, and 56.37 to 68.54%, respectively. The macromolecules were also characterized by SEM, FTIR and DSC. The in vitro drug release from these macromolecules (84.95 ± 2.02 to 95.33 ± 1.56% at 10h) exhibited sustained release (first-order) pattern with super case-II transport mechanism. The swelling and mucoadhesivity of these macromolecules were affected by pH of the medium. The design established the role of derived polynomial equations and plots in predicting the values of dependent variables for the preparation and optimization.
本研究通过离子凝胶化作用，使用 3(2) 析因设计，开发和优化了含有醋氯芬酸的刺槐豆胶-海藻酸钠黏附性大分子。优化了刺槐豆胶和海藻酸钠的用量对药物包封效率（%DEE）、8 小时时的%黏附性（M8）和 10 小时时的%体外药物释放（%Q10h）的影响。大分子的产率、平均粒径和 DEE 分别在 93.19%至 96.65%、1.328±0.11 至 1.428±0.13μm 和 56.37%至 68.54%的范围内。这些大分子还通过 SEM、FTIR 和 DSC 进行了表征。这些大分子的体外药物释放（10 小时时为 84.95±2.02%至 95.33±1.56%）呈现出持续释放（一级）模式，并具有超二级传输机制。这些大分子的溶胀性和黏附性受介质 pH 的影响。该设计确定了导出的多项式方程和图在预测制备和优化中因变量值的作用。
