El-Kamel A H, Sokar M S, Al Gamal S S, Naggar V F
Department of Pharmaceutics, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Int J Pharm. 2001 Jun 4;220(1-2):13-21. doi: 10.1016/s0378-5173(01)00574-9.
A sustained release system for ketoprofen designed to increase its residence time in the stomach without contact with the mucosa was achieved through the preparation of floating microparticles by the emulsion-solvent diffusion technique. Four different ratios of Eudragit S100 (ES) with Eudragit RL (ERL) were used to form the floating microparticles. The drug retained in the floating microparticles decreased with increase in ERL content. All floating microparticle formulations showed good flow properties and packability. Scanning electron microscopy and particle size analysis revealed differences between the formulations as to their appearance and size distribution. X-ray and DSC examination showed the amorphous nature of the drug. Release rates were generally low in 0.1 N HCl especially in presence of high content of ES while in phosphate buffer pH 6.8, high amounts of ES tended to give a higher release rate. Floating ability in 0.1 N HCl, 0.1 N HCl containing 0.02% Tween 20 and simulated gastric fluid without pepsin was also tested. The formulation containing ES:ERL1:1 (FIII) exhibited high percentage of floating particles in all examined media.
通过乳液-溶剂扩散技术制备漂浮微粒,实现了一种酮洛芬缓释系统,该系统旨在增加其在胃中的停留时间且不与黏膜接触。使用四种不同比例的尤特奇S100(ES)与尤特奇RL(ERL)来形成漂浮微粒。保留在漂浮微粒中的药物量随ERL含量的增加而减少。所有漂浮微粒制剂均显示出良好的流动性和可压性。扫描电子显微镜和粒度分析揭示了各制剂在外观和粒度分布方面的差异。X射线和差示扫描量热法检查显示药物为无定形性质。在0.1 N盐酸中释放速率通常较低,尤其是在ES含量高的情况下,而在pH 6.8的磷酸盐缓冲液中,高含量的ES往往会导致更高的释放速率。还测试了在0.1 N盐酸、含0.02%吐温20的0.1 N盐酸和不含胃蛋白酶的模拟胃液中的漂浮能力。含ES:ERL 1:1的制剂(FIII)在所有检测介质中均表现出高比例的漂浮颗粒。