Navarro-Ruíz Eva, Álvarez-Álvarez Covadonga, Peña M Ángeles, Torrado-Salmerón Carlos, Dahma Zaid, de la Torre-Iglesias Paloma Marina
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
Instituto Universitario de Farmacia Industrial, Complutense University, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
Pharmaceutics. 2022 Jul 20;14(7):1504. doi: 10.3390/pharmaceutics14071504.
The aim of this research is the development of new colonic release systems of meloxicam (MLX) a non-steroidal anti-inflammatory drug (NSAIDs) with pH and time-dependent vehicles for cancer or autoimmune diseases. The colon has a higher pH than the rest of the gastrointestinal tract (GIT) and this can be used as a modified release strategy. Eudragit polymers are the most widely used synthetic products in the design of colonic release formulations because they might offer mucoadhesiveness and pH-dependent release. Colonic delivery systems produced with pH-dependent and permeable polymers (FS-30D) or with pH-independent and low permeability polymers (NM-30D), must dissolve at a pH range of 6.0-7.0 to delay the release of the drug and prevent degradation in the GIT, before reaching the colon. The conditions prepared to simulate a gastrointestinal transit showed the CNM multiparticulate system, composed of Eudragit NM and cellulose, as the best release option for MLX with a more sustained release with respect to the other formulations. CNM formulation followed Higuchi and First-order release kinetics, thus MLX release was controlled by a combination of diffusion and polymers swelling/eroding processes.
本研究的目的是开发美洛昔康(MLX,一种非甾体抗炎药)的新型结肠释放系统,该系统采用pH值和时间依赖性载体,用于治疗癌症或自身免疫性疾病。结肠的pH值高于胃肠道(GIT)的其他部位,这可作为一种缓释策略。Eudragit聚合物是结肠释放制剂设计中使用最广泛的合成产品,因为它们可能具有粘膜粘附性和pH依赖性释放特性。用pH依赖性和可渗透聚合物(FS-30D)或pH非依赖性和低渗透性聚合物(NM-30D)制备的结肠给药系统,必须在pH值为6.0 - 7.0的范围内溶解,以延迟药物释放并防止在到达结肠之前在胃肠道中降解。为模拟胃肠道转运而准备的条件表明,由Eudragit NM和纤维素组成的CNM多颗粒系统是MLX的最佳释放选择,相对于其他制剂,其释放更持久。CNM制剂遵循Higuchi和一级释放动力学,因此MLX的释放受扩散和聚合物溶胀/侵蚀过程的共同控制。