Sancho Matias I, Russo Marcos G, Moreno M Sergio, Gasull Estela, Blanco Sonia E, Narda Griselda E
§Instituto Balseiro, Centro Atómico Bariloche, San Carlos de Bariloche 8400, Argentina.
J Phys Chem B. 2015 May 7;119(18):5918-25. doi: 10.1021/acs.jpcb.5b01742. Epub 2015 Apr 27.
The characterization of the inclusion complex between 2-hydroxybenzophenone (2OHBP) and β-cyclodextrin (βCD) in the solid state was performed using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and transmission electron microscopy (TEM). The apparent formation constant of the complex was determined by phase solubility diagrams and liquid chromatography (HPLC) at different temperatures. The formation of the inclusion complex induced slight shifts in the FTIR spectrum while by PXRD a new crystalline phase was observed. TEM studies revealed that the complex forms aggregates of nanometric size. The inclusion complex showed a higher solubility in the tested dissolution media than free 2OHBP. Moreover, the freeze-dried solid complex exhibits a higher thermal stability than the solid free drug. The thermodynamic analysis allowed us to conclude that the encapsulation process is endothermic in water and exothermic in methanol-water.
采用傅里叶变换红外光谱(FTIR)、粉末X射线衍射(PXRD)、差示扫描量热法(DSC)、热重分析(TGA)和透射电子显微镜(TEM)对固态下2-羟基二苯甲酮(2OHBP)与β-环糊精(βCD)之间的包合物进行了表征。通过不同温度下的相溶解度图和液相色谱(HPLC)测定了该配合物的表观形成常数。包合物的形成在FTIR光谱中引起了轻微的位移,而通过PXRD观察到了一个新的晶相。TEM研究表明,该配合物形成了纳米尺寸的聚集体。包合物在测试的溶出介质中的溶解度高于游离的2OHBP。此外,冻干的固体配合物比固体游离药物表现出更高的热稳定性。热力学分析使我们得出结论,包封过程在水中是吸热的,在甲醇-水中是放热的。