Fu C, Zhao L, Jiang X
Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433.
Yao Xue Xue Bao. 1998 Jul;33(7):538-43.
The swelling behavior of acrylic polymer Eudragit RL in different concentration and species of electrolyte aqueous media, and the effect of media and polymer swelling on drug release from Eudragit RL matrix system were investigated with nifedipine, chlorpheniramine maleate and indomethacin as model drugs. It was found that Eudragit RL was sensitive to the electrolytes in aqueous media. The swelling of Eudragit RL decreased with increasing electrolyte concentration and was significantly affected by the electrolyte species. The swelling behavior was reversible. The release of 3 drugs from Eudragit RL matrix was remarkably affected by the electrolytes in the media. The rates of release of nifedipine and chlorpheniramine maleate from the polymer matrices were controlled by the polymer swelling behavior, and the rate of release correlated well with the swelling behavior. However, the rates of release of indomethacin from the Eudragit RL matrix were controlled not only by the polymer swelling but also by the drug displacement by the medium anion, which was attributed to the presence of an interaction between indomethacin and Eudragit RL.
以硝苯地平、马来酸氯苯那敏和吲哚美辛为模型药物,研究了丙烯酸聚合物Eudragit RL在不同浓度和种类的电解质水溶液介质中的溶胀行为,以及介质和聚合物溶胀对Eudragit RL基质系统药物释放的影响。结果发现,Eudragit RL对水性介质中的电解质敏感。Eudragit RL的溶胀随着电解质浓度的增加而降低,并且受到电解质种类的显著影响。溶胀行为是可逆的。介质中的电解质对3种药物从Eudragit RL基质中的释放有显著影响。硝苯地平和马来酸氯苯那敏从聚合物基质中的释放速率受聚合物溶胀行为控制,且释放速率与溶胀行为相关性良好。然而,吲哚美辛从Eudragit RL基质中的释放速率不仅受聚合物溶胀控制,还受介质阴离子对药物的置换作用控制,这归因于吲哚美辛与Eudragit RL之间存在相互作用。