University of Szeged, Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, Szeged, Hungary.
University of Szeged, Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, Szeged, Hungary.
Int J Pharm. 2019 Mar 25;559:68-75. doi: 10.1016/j.ijpharm.2019.01.034. Epub 2019 Jan 21.
Meloxicam is an anti-inflammatory drug that could be interesting to deliver locally to the lungs to treat inflammation occurring in cystic fibrosis or chronic obstructive pulmonary disease (COPD). Spray drying conditions were optimized to prepare inhalable dry powders, from meloxicam aqueous solution with pH adjustment. A comparison study between non-porous and large porous particles (LPPs) was carried out to demonstrate the relevance of the aimed large size (>5 µm) and low density (<0.2 mg/cm) formulations. With the appropriate amount of porogen agent, ammonium bicarbonate, LPPs exhibited the same aerodynamic diameter and a higher deposited fraction than smaller but dense particles. The aerodynamic evaluation of LPPs showed that the fine particle fraction (FPF) reached up to 65.8%, while the emitted fraction (EF) reached 85.4%, both higher than for the non-porous particles. Stability tests demonstrated that, after 10 weeks of storage, no significant difference could be detected in the aerodynamic behaviour of the formulations. To the best of our knowledge this is the first time large porous particles, with enhanced aerodynamic properties, from an aqueous solution of meloxicam are reported.
美洛昔康是一种抗炎药物，将其局部递送至肺部以治疗囊性纤维化或慢性阻塞性肺疾病（COPD）中的炎症可能非常有趣。通过调整 pH 值，从美洛昔康水溶液中优化喷雾干燥条件来制备可吸入干粉。进行了非多孔和大孔颗粒（LPP）之间的比较研究，以证明目标大尺寸（>5 µm）和低密度（<0.2 mg/cm）制剂的相关性。使用适量的致孔剂碳酸氢铵，LPP 表现出与较小但密度较高的颗粒相同的空气动力学直径和更高的沉积分数。LPP 的空气动力学评估表明，细颗粒分数（FPF）高达 65.8%，而发射分数（EF）高达 85.4%，均高于非多孔颗粒。稳定性测试表明，在储存 10 周后，制剂的空气动力学行为没有明显差异。据我们所知，这是首次报道从美洛昔康水溶液中获得具有增强空气动力学性能的大孔颗粒。
