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载有布洛芬赖氨酸盐的海藻酸钙珠的特性描述及制备方法的优化。

Characterization of alginate beads loaded with ibuprofen lysine salt and optimization of the preparation method.

机构信息

Unit of Pharmaceutical Technology, Pharmacy and Parmaceutical Technology Department, School of Pharmacy, University of Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain.

Unit of Pharmaceutical Technology, Pharmacy and Parmaceutical Technology Department, School of Pharmacy, University of Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain.

出版信息

Int J Pharm. 2014 Jan 2;460(1-2):181-8. doi: 10.1016/j.ijpharm.2013.10.034. Epub 2013 Oct 28.

Abstract

The parameters influencing alginate ionotropic gelation and the production of alginate beads loaded with hydrosoluble ibuprofen lysine salt (IBU-L) were studied, as well as the optimization of the method for its attainment. A three-factor and three-level factorial design (3(3)) was carried out to determine the influence of three experimental variables: polymer concentration, CaCl2 concentration, and curing time on the dependent variables drug load and encapsulation efficiency. The effect of the pH used in the preparation bath was also evaluated. Concentrations of CaCl2 and pH of gelling bath were seen to affect bead formation and stability as well as their ability to properly entrap the drug. In this work, IBU-L was used as a model of a non-steroidal anti-inflammatory drug with good solubility in alginate solutions. IBU-L was successfully encapsulated in alginate beads obtained by the ionotropic gelation method. The obtained alginate matrixes are able to modify the release of the entrapped IBU-L and this occurs in a pH-sensitive way that can be correlated with the swelling behaviour of the alginate-produced beads. Morphological characteristics were evaluated by means of scanning electron microscopy.

摘要

研究了影响海藻酸钠离子凝胶化的参数以及载水不溶性布洛芬赖氨酸盐(IBU-L)的海藻酸钠珠的制备,优化了获得IBU-L 的方法。采用三因素三水平析因设计(3(3))来确定三个实验变量(聚合物浓度、CaCl2 浓度和固化时间)对依赖变量药物负载和包封效率的影响。还评估了制备浴中 pH 的影响。胶凝浴中的 CaCl2 浓度和 pH 值会影响珠粒的形成和稳定性,以及它们对药物的适当包封能力。在这项工作中,IBU-L 被用作海藻酸钠溶液中具有良好溶解度的非甾体抗炎药物的模型。IBU-L 成功地被包封在离子凝胶化方法获得的海藻酸钠珠中。所得到的海藻酸钠基质能够修饰包封的 IBU-L 的释放,并且以与海藻酸钠产生的珠的溶胀行为相关的 pH 敏感的方式发生。通过扫描电子显微镜评估了形态特征。

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