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交联海藻酸盐-明胶珠:一种用于控释吲哚洛尔的新型基质。

Cross-linked alginate-gelatine beads: a new matrix for controlled release of pindolol.

作者信息

Ferreira Almeida P, Almeida A J

机构信息

Unidade de Ciências e Tecnologia Farmacêuticas, Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003, Lisboa, Portugal.

出版信息

J Control Release. 2004 Jul 7;97(3):431-9. doi: 10.1016/j.jconrel.2004.03.015.

Abstract

This work is focused on the development of a new particulate drug delivery system using a sodium alginate matrix containing pindolol as a model drug molecule for intestinal drug prolonged release. Calcium alginate beads are known to be unable to control the release of most insoluble drugs. Pindolol-loaded alginate-gelatine beads have been developed using a solvent-free technique that involves a cross-linking reaction. Modifications in matrix structure and physicochemical behaviour caused by the cross-linking reaction were assessed during particle formation and drug release. Several parameters, such as matrix gelling rate, encapsulation efficiency, drug release profile and matrix erosion rate, were investigated. Physicochemical characterisation indicates the formation of a new alginate-gelatine matrix and shows that pindolol does not interfere with the matrix formation process. Matrix swelling of calcium alginate beads induced by phosphate buffer ends up in erosion and destruction. However, for cross-linked beads swelling does not lead to complete erosion, which may be the main cause of pindolol retention within the matrix. The modifications introduced in the initial calcium alginate formulation by means of an appropriate method such as the use of a cross-linking agent successfully changed the matrix performance, allowing the controlled release of pindolol.

摘要

本研究聚焦于开发一种新型颗粒药物递送系统,该系统采用含吲哚洛尔的海藻酸钠基质作为肠道药物缓释的模型药物分子。已知海藻酸钙珠无法控制大多数不溶性药物的释放。已采用涉及交联反应的无溶剂技术制备了负载吲哚洛尔的海藻酸钠-明胶珠。在颗粒形成和药物释放过程中,评估了交联反应引起的基质结构和物理化学行为的变化。研究了几个参数,如基质胶凝速率、包封效率、药物释放曲线和基质侵蚀速率。物理化学表征表明形成了一种新的海藻酸钠-明胶基质,并表明吲哚洛尔不干扰基质形成过程。磷酸盐缓冲液诱导的海藻酸钙珠的基质溶胀最终导致侵蚀和破坏。然而,对于交联珠,溶胀不会导致完全侵蚀,这可能是吲哚洛尔保留在基质中的主要原因。通过使用交联剂等适当方法对初始海藻酸钙制剂进行的改性成功改变了基质性能,实现了吲哚洛尔的控释。

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