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使用表面交联改性聚乙烯醇水凝胶中茶碱缓释制剂的释放

Modifying the release of proxyphylline from PVA hydrogels using surface crosslinking.

作者信息

Wu Linfeng, Brazel Christopher S

机构信息

Department of Chemical and Biological Engineering, Box 870203, 201 7th Avenue, The University of Alabama, Tuscaloosa, AL 35487, USA.

出版信息

Int J Pharm. 2008 Feb 12;349(1-2):144-51. doi: 10.1016/j.ijpharm.2007.08.007. Epub 2007 Aug 12.

Abstract

Drug release profiles were altered to prevent the initial burst effect or introduce a lag phase by creating surface crosslinked layers in poly(vinyl alcohol) (PVA) hydrogels. Confocal laser scanning microscopy (CLSM) confirmed the successful introduction of these surface crosslinked layers. The thickness and crosslinking density of the surface crosslinked layer were highly dependent on the surface crosslinking conditions (i.e., exposure time and glutaraldehyde (GTA) concentration used). By judicious selection of these parameters, the initial burst release could be eliminated and a reproducible delayed release could be achieved. Highly surface crosslinked layers had a tendency to rupture during the swelling process of PVA hydrogels; these raptures were found to coincide with delayed release of proxyphylline from surface crosslinked PVA hydrogels.

摘要

通过在聚乙烯醇(PVA)水凝胶中创建表面交联层,改变药物释放曲线以防止初始突释效应或引入滞后阶段。共聚焦激光扫描显微镜(CLSM)证实了这些表面交联层的成功引入。表面交联层的厚度和交联密度高度依赖于表面交联条件(即使用的暴露时间和戊二醛(GTA)浓度)。通过明智地选择这些参数,可以消除初始突释,并实现可重现的延迟释放。高度表面交联的层在PVA水凝胶的溶胀过程中倾向于破裂;发现这些破裂与茶碱从表面交联的PVA水凝胶中的延迟释放相吻合。

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