Kállai-Szabó Nikolett, Luhn Oliver, Bernard Joerg, Kállai-Szabó Barnabás, Zelkó Romána, Antal István
Department of Pharmaceutics, Semmelweis University, Hőgyes E. Street 7-9, 1092 Budapest, Hungary.
Südzucker AG, Central Department Research, Development and Technological Services, Department of Product Technology, Pharmaceutical Technology, Wormser Street 11, 67283 Obrigheim, Germany.
J Pharm Biomed Anal. 2014 Sep;98:339-44. doi: 10.1016/j.jpba.2014.06.005. Epub 2014 Jun 10.
Layered and coated pellets were formulated to control the release of the diclofenac sodium selected as model drug. A highly water soluble isomalt inert pellet core material was used to osmotically modulate the drug release through the swellable polyvinyl acetate coating layer. Image analysis was applied to determine the shape parameters and the swelling behavior of the pellets. UV-spectroscopy and liquid chromatography with refractive index detection were applied to measure the concentration of the model drug and the core materials. Simultaneous dissolution of both the diclofenac sodium and isomalt was observed. Relationship was found between the dissolution profile of the drug and the core material which linear correlation was independent on the coating level. The latter enables the modulation of drug release beside the permeability control of the swelled coating polymer.
制备了分层和包衣微丸以控制作为模型药物的双氯芬酸钠的释放。使用高度水溶性的异麦芽酮糖醇惰性微丸核心材料，通过可膨胀的聚醋酸乙烯酯包衣层渗透调节药物释放。应用图像分析来确定微丸的形状参数和溶胀行为。采用紫外光谱法和示差折光检测液相色谱法来测定模型药物和核心材料的浓度。观察到双氯芬酸钠和异麦芽酮糖醇同时溶解。发现药物的溶出曲线与核心材料之间存在关系，其线性相关性与包衣水平无关。后者除了能控制溶胀包衣聚合物的渗透性外，还能调节药物释放。
