Tajber L, Corrigan D O, Corrigan O I, Healy A M
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.
Int J Pharm. 2009 Feb 9;367(1-2):79-85. doi: 10.1016/j.ijpharm.2008.09.030. Epub 2008 Sep 25.
The objective of this work was to examine the physicochemical properties of spray dried budesonide, formoterol fumarate and their mixtures at two different weight ratios: 100:6 and 400:6 of budesonide and formoterol fumarate, respectively. A comparison of the thermal properties, crystalline/amorphous nature and particle size of the starting micronised as well as processed materials was carried out. The micronised drugs on their own and the physical mixtures were crystalline in contrast to the spray dried counterparts which were shown to be amorphous. The glass transition temperatures (T(g)s) of the processed actives were determined and appeared at 89.5 and 88 degrees C for budesonide and formoterol fumarate, respectively. As for the spray dried composites, an indication of miscibility and/or interactions between the components was indicated by differential scanning calorimetry and infrared analysis. The spray drying in all cases resulted in smooth, spherical microparticles of sizes suitable for inhalation.
这项工作的目的是研究喷雾干燥的布地奈德、富马酸福莫特罗及其两种不同重量比混合物的物理化学性质，布地奈德与富马酸福莫特罗的重量比分别为100:6和400:6。对起始微粉化材料以及加工后材料的热性质、晶态/非晶态性质和粒径进行了比较。微粉化药物本身和物理混合物是晶态的，而喷雾干燥后的对应物显示为非晶态。测定了加工后活性成分的玻璃化转变温度（Tg），布地奈德和富马酸福莫特罗的玻璃化转变温度分别为89.5℃和88℃。对于喷雾干燥的复合材料，差示扫描量热法和红外分析表明了各组分之间的混溶性和/或相互作用。在所有情况下，喷雾干燥均产生了尺寸适合吸入的光滑球形微粒。
