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由聚丙烯酸主链上的聚(L-乳酸)接枝共聚物制成的载布洛芬薄膜和微球的制备及体外释放研究

Preparation and in vitro release studies of ibuprofen-loaded films and microspheres made from graft copolymers of poly(L-lactic acid) on acrylic backbones.

作者信息

Gallardo A, Eguiburu J L, Fernandez Berridi M J, San Román J

机构信息

Instituto de Ciencia y Tecnología de Polímeros, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

出版信息

J Control Release. 1998 Nov 13;55(2-3):171-9. doi: 10.1016/s0168-3659(98)00047-9.

Abstract

The present article describes the preparation of films of various thickness and microspheres from new resorbable graft copolymers of polyacrylic (methyl methacrylate, MMA, or methyl acrylate, MA), or polyvinylic (vinyl pyrrolidone, VP) chains and poly(l-lactic acid) (PLLA) side blocks charged with 15-20% of ibuprofen (IBU) (a non-steroidic antiinflammatory agent). In the case of MMA-LLA and MA-LLA graft copolymers the release of IBU in buffered solution is modulated by the flexibility of the copolymer chains in a first step of one to two days and in a second step by the diffusive properties of the system as well as by the biodegradation of the polymers. The VP-PLLA graft copolymers are highly hydrophilic and the release of IBU is modulated by the diffusion of the drug through the swollen system. Specific interactions between the IBU molecules and the pyrrolidone rings also participate in the kinetic behaviour of the release process.

摘要

本文描述了由聚丙烯酸(甲基丙烯酸甲酯,MMA,或丙烯酸甲酯,MA)或聚乙烯基(乙烯基吡咯烷酮,VP)链与聚(L-乳酸)(PLLA)侧链组成的新型可吸收接枝共聚物制备不同厚度的薄膜和微球的方法,这些接枝共聚物负载了15 - 20%的布洛芬(IBU)(一种非甾体抗炎药)。对于MMA-LLA和MA-LLA接枝共聚物,在缓冲溶液中IBU的释放首先在一到两天的时间内由共聚物链的柔韧性调节,第二步则由体系的扩散性质以及聚合物的生物降解调节。VP-PLLA接枝共聚物具有高度亲水性,IBU的释放由药物在溶胀体系中的扩散调节。IBU分子与吡咯烷酮环之间的特定相互作用也参与了释放过程的动力学行为。

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