Saveyn Pieter, Cocquyt Ellen, Zhu Wuxin, Sinnaeve Davy, Haustraete Katrien, Martins José C, Van der Meeren Paul
Particle and Interfacial Technology Group, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Gent, Belgium.
Phys Chem Chem Phys. 2009 Jul 14;11(26):5462-8. doi: 10.1039/b822327k. Epub 2009 Apr 16.
The solubilization of the poorly water soluble anti-inflammatory drug flurbiprofen in non-ionic Tween 20 surfactant micellar solutions was studied by both (19)F and (1)H NMR spectroscopy in an acidic environment. These non-destructive techniques allowed us to investigate the effect of temperature cycling in situ. Using (19)F NMR, an increased solubilisation capacity was observed as the temperature increased. This effect became more pronounced above the cloud point, which was reduced by more than 30 degrees C in the presence of an excess of flurbiprofen. Upon clouding, peak splitting was observed in the (19)F spectrum, which indicates that two pools of solubilised flurbiprofen exist that are in slow exchange on the NMR frequency timescale. The clouding and solubilization processes were found to be reversible, albeit with slow kinetics. Based on chemical shift differences of both Tween 20 and flurbiprofen, as well as NOESY experiments, the flurbiprofen was found to be accumulated within the palisade layer of the Tween 20 micelles.
在酸性环境中,通过¹⁹F和¹H核磁共振光谱法研究了难溶性抗炎药物氟比洛芬在非离子吐温20表面活性剂胶束溶液中的增溶作用。这些无损技术使我们能够原位研究温度循环的影响。使用¹⁹F核磁共振,观察到随着温度升高增溶能力增强。在浊点以上这种效应变得更加明显,在过量氟比洛芬存在下浊点降低了30多摄氏度。在浊化时,¹⁹F光谱中观察到峰分裂,这表明存在两个溶解的氟比洛芬池,它们在核磁共振频率时间尺度上进行缓慢交换。发现浊化和增溶过程是可逆的,尽管动力学较慢。基于吐温20和氟比洛芬的化学位移差异以及核Overhauser效应光谱实验,发现氟比洛芬聚集在吐温20胶束的栅栏层内。