Department of Pharmaceutical Technology, University of Szeged, Eötvös 6, H-6720 Szeged, Hungary.
J Pharm Biomed Anal. 2011 Sep 10;56(2):183-90. doi: 10.1016/j.jpba.2011.05.008. Epub 2011 May 17.
The crystal size, form, wettability and rate of dissolution of a drug are factors limiting its nasal or pulmonary administration. The aim of this work was to achieve an ideal crystal habit, good wettability and the rapid release of meloxicam (MEL), a poorly water-soluble non-steroidal anti-inflammatory drug. The structures of MEL and the carrier-based systems were analysed by differential scanning calorimetry, X-ray diffractometry and Fourier transform infrared spectroscopy. The particle size and morphology were investigated by laser diffraction and SEM analyses. The novelty of this work was the use of a co-spray-drying technique, which resulted in mannitol-based crystalline microcomposites (1-6 μm) containing MEL microcrystals (1-5 μm). The particle size and form of the MEL microcrystals were adjusted by a top-down method. The presence of mannitol (with a MEL:mannitol mass ratio of 1:1) with additives ensured the homogeneous distribution of MEL in the microcomposites with good wettability and rapid release (100% MEL within 5 min).
药物的晶体大小、形态、润湿性和溶解速率是限制其鼻内或肺部给药的因素。本工作的目的是获得理想的晶体形态、良好的润湿性和快速释放美洛昔康(MEL),一种水溶性差的非甾体抗炎药。通过差示扫描量热法、X 射线衍射和傅里叶变换红外光谱分析了 MEL 和基于载体的系统的结构。通过激光衍射和 SEM 分析研究了粒径和形态。这项工作的新颖之处在于使用共喷雾干燥技术,得到了含有 MEL 微晶体(1-5μm)的甘露醇基结晶微复合材料(1-6μm)。通过自上而下的方法调整了 MEL 微晶体的粒径和形态。甘露醇(MEL:甘露醇质量比为 1:1)的存在以及添加剂的存在确保了 MEL 在微复合材料中的均匀分布,具有良好的润湿性和快速释放(5 分钟内 100%释放 MEL)。