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喹硫平从乙烯-醋酸乙烯酯基质中的释放特性。

Release characteristics of quinupramine from the ethylene-vinyl acetate matrix.

作者信息

Kim Jin, Kim Woong-Jang, Kim Seong-Jin, Cho Cheong-Weon, Shin Sang-Chul

机构信息

College of Pharmacy, Chonnam National University, Gwangju 500-757, South Korea.

出版信息

Int J Pharm. 2006 Jun 6;315(1-2):134-9. doi: 10.1016/j.ijpharm.2006.03.019. Epub 2006 Mar 27.

Abstract

An ethylene-vinyl acetate (EVA) matrix containing quinupramine was prepared in an attempt to develop a controlled delivery system for quinupramine. Permeation studies of quinupramine through the EVA copolymer membrane were carried out using a two-chamber diffusion cell. The rate of drug permeation through the EVA membrane was proportional to the PEG 400 volume fraction. The release of quinupramine from the EVA matrix was examined using a modified Franz diffusion cell. A plasticizer was added to prepare the pore structure of the EVA matrix in order to increase the rate of drug release. The effects of PEG 400, membrane thickness, drug concentration, temperature, and plasticizer on drug release rate were investigated. The drug release rate from the EVA matrix increased with increasing PEG 400 volume fraction, temperature and drug loading dose. The activation energy for drug release was 5.91, 5.39, 4.68 and 4.52 kcal/mol for a loading dose of 0.5%, 1%, 1.5%, and 2%, respectively. Among the plasticizers used, diethyl phthalate showed the best results. The release of quinupramine from the EVA matrix follows a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The controlled release of quinupramine was achieved using the EVA polymer including a plasticizer.

摘要

制备了一种含有喹硫平的乙烯-醋酸乙烯酯(EVA)基质,试图开发一种喹硫平控释系统。使用双室扩散池对喹硫平透过EVA共聚物膜进行了渗透研究。喹硫平透过EVA膜的速率与聚乙二醇400体积分数成正比。使用改良的Franz扩散池研究了喹硫平从EVA基质中的释放情况。添加了增塑剂以制备EVA基质的孔结构,从而提高药物释放速率。研究了聚乙二醇400、膜厚度、药物浓度、温度和增塑剂对药物释放速率的影响。喹硫平从EVA基质中的释放速率随聚乙二醇400体积分数、温度和药物载药量的增加而增加。载药量为0.5%、1%、1.5%和2%时,药物释放的活化能分别为5.91、5.39、4.68和4.52千卡/摩尔。在所使用的增塑剂中,邻苯二甲酸二乙酯效果最佳。喹硫平从EVA基质中的释放遵循扩散控制模型,即单位面积释放量与时间的平方根成正比。使用含增塑剂的EVA聚合物实现了喹硫平的控释。

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