Adebisi Adeola O, Kaialy Waseem, Hussain Tariq, Al-Hamidi Hiba, Nokhodchi Ali, Conway Barbara R, Asare-Addo Kofi
Department of Pharmacy, University of Huddersfield, Huddersfield, HD1 3DH, UK.
School of Pharmacy, University of Wolverhampton, Faculty of Science and Engineering, Wolverhampton, WV1 1LY, UK.
Colloids Surf B Biointerfaces. 2016 Oct 1;146:841-51. doi: 10.1016/j.colsurfb.2016.07.032. Epub 2016 Jul 16.
This work explores the use of both spray drying and d-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging were also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM. XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5μm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5nC/g for untreated material and -7.5 versus 3.1nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1-0.3nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.
本研究探索了喷雾干燥法以及使用盐酸氨基葡萄糖（GLU）作为亲水性载体来提高吡罗昔康（PXM）的溶解速率，同时研究与喷雾干燥过程相关的静电荷。制备并表征了喷雾干燥的PXM:GLU固体分散体（X射线粉末衍射、差示扫描量热法、扫描电子显微镜）。还进行了溶出度和摩擦起电测试。结果表明，单独喷雾干燥的PXM（不含GLU）产生了一些PXM II型（差示扫描量热法结果），相对于母体PXM，其溶解度没有提高。X射线粉末衍射结果还表明，喷雾干燥过程降低了GLU和所制备固体分散体的结晶度。GLU的存在提高了PXM的溶解速率。喷雾干燥的PXM:GLU比例为2:1时，溶出度改善最为显著。喷雾干燥过程通常产生约2.5μm的PXM-GLU球形颗粒，这可能有助于提高溶出度。与载体GLU相比，PXM表现出更高的带电倾向（未处理材料分别为-3.8和0.5nC/g，喷雾干燥材料分别为-7.5和3.1nC/g）。喷雾干燥的PXM和喷雾干燥的GLU分别显示出比未处理的PXM和未处理的GLU更高的电荷密度。无论PXM:GLU比例如何，所有喷雾干燥的PXM:GLU固体分散体的电荷密度都可忽略不计（净CMR：0.1 - 0.3nC/g）。喷雾干燥PXM:GLU固体分散体可用于生产几乎不带电的制剂粉末，从而改善PXM的处理性能以及溶出行为。
