Rimoli Maria G, Rabaioli Maria R, Melisi Daniela, Curcio Annalisa, Mondello Sandro, Mirabelli Rosella, Abignente Enrico
Department of Pharmaceutical and Toxicological Chemistry, Faculty of Pharmacy, Federico II University of Naples, via Domenico Montesano 49, 80131 Naples, Italy.
J Biomed Mater Res A. 2008 Oct;87(1):156-64. doi: 10.1002/jbm.a.31763.
Synthetic zeolites were studied in order to investigate their ability to encapsulate and to release drugs. In particular, a zeolite X and a zeolitic product obtained from a cocrystallization of zeolite X and zeolite A were examined. These materials were characterized by chemical analyses (ICP-AES), X-ray diffraction, nitrogen adsorption isotherm, scanning electron microscopy, laser diffraction, and infrared spectroscopy. Since ketoprofen was chosen as a model drug for the formulation of controlled-release dosage forms, it was encapsulated into these two types of synthetic zeolites by a soaking procedure. Drug-loaded matrices were then characterized for entrapped drug amount and thermogravimetric behavior. In both types of activated zeolites, the total amount of ketoprofen (800 mg) was encapsulated in 2 g of matrix. By using HPLC measurements, ketoprofen release studies were done at different pH conditions so as to mimick gastrointestinal fluids. The absence of release in acid conditions and a double phased release, at two different pH values (5 and 6.8), suggest that after activation these materials offer good potential for a modified release delivery system of ketoprofen.
为了研究合成沸石包封和释放药物的能力，对其进行了研究。特别地，研究了一种X型沸石以及通过X型沸石与A型沸石共结晶得到的沸石产物。这些材料通过化学分析（电感耦合等离子体发射光谱法）、X射线衍射、氮吸附等温线、扫描电子显微镜、激光衍射和红外光谱进行表征。由于选择酮洛芬作为制备控释剂型的模型药物，通过浸泡法将其包封于这两种合成沸石中。然后对载药基质的包封药量和热重行为进行表征。在两种类型的活性沸石中，2g基质中均包封了总量为800mg的酮洛芬。通过高效液相色谱测量，在不同pH条件下进行酮洛芬释放研究，以模拟胃肠液。在酸性条件下无释放以及在两个不同pH值（5和6.8）下的双相释放表明，活化后这些材料在酮洛芬的缓释给药系统方面具有良好的潜力。
