Mura P, Adragna E, Rabasco A M, Moyano J R, Pérez-Martìnez J I, Arias M J, Ginés J M
Department of Pharmaceutical Sciences, Firenze University, Italy.
Drug Dev Ind Pharm. 1999 Mar;25(3):279-87. doi: 10.1081/ddc-100102172.
The effect of cyclodextrin (Cd) complexation on ibuproxam (IBUX) dissolution properties was studied by evaluating both the influence of Cd cavity size and the preparation method used for obtaining solid inclusion complexes. Binary systems of IBUX with natural Cds, prepared using different techniques (kneading, sealed-heating, spray-drying), were studied by differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and their dissolution behavior was evaluated according to the dispersed amount method. The nature and the dissolution performance of the end product appeared to be related to both steric factors of host molecule and preparation method of the solid system. The alpha Cd cavity size was less suitable for accommodating the IBUX molecule, whereas spray-drying and sealed-heating methods led to a true inclusion complex of IBUX in the beta Cd and gamma Cd cavity. In contrast, the kneading method did not lead in any case to a real inclusion complex. Spray-dried systems with beta Cd and gamma Cd were the most effective in achieving the enhancement of the IBUX dissolution rate.
通过评估环糊精（Cd）的空腔大小以及用于获得固体包合物的制备方法的影响，研究了环糊精（Cd）络合对异丁普生（IBUX）溶解性能的影响。采用不同技术（捏合、密封加热、喷雾干燥）制备的IBUX与天然环糊精的二元体系，通过差示扫描量热法（DSC）、热台显微镜（HSM）、傅里叶变换红外（FTIR）光谱、扫描电子显微镜（SEM）进行研究，并根据分散量法评估其溶解行为。最终产物的性质和溶解性能似乎与主体分子的空间因素以及固体体系的制备方法有关。α-环糊精的空腔大小不太适合容纳IBUX分子，而喷雾干燥和密封加热方法导致IBUX在β-环糊精和γ-环糊精空腔中形成真正的包合物。相比之下，捏合法在任何情况下都不会形成真正的包合物。含有β-环糊精和γ-环糊精的喷雾干燥体系在提高IBUX溶解速率方面最为有效。
