Salústio P J, Feio G, Figueirinhas J L, Pinto J F, Cabral Marques H M
iMed.UL (Research Institute for Medicines and Pharmaceutical Sciences), Faculdade de Farmácia da Universidade de Lisboa, P-1649-003 Lisboa, Portugal.
Eur J Pharm Biopharm. 2009 Feb;71(2):377-86. doi: 10.1016/j.ejpb.2008.09.027. Epub 2008 Oct 17.
The work aims to prove the complexation of two model drugs (ibuprofen, IB and indomethacin, IN) by beta-cyclodextrin (betaCD), and the effect of water in such a process, and makes a comparison of their complexation yields. Two methods were considered: kneading of a binary mixture of the drug, betaCD, and inclusion of either IB or IN in aqueous solutions of betaCD. In the latter method water was removed by air stream, spray-drying and freeze-drying. To prove the formation of complexes in final products, optical microscopy, UV spectroscopy, IR spectroscopy, DSC, X-ray and NMR were considered. Each powder was added to an acidic solution (pH=2) to quantify the concentration of the drug inside betaCD cavity. Other media (pH=5 and 7) were used to prove the existence of drug not complexed in each powder, as the drugs solubility increases with the pH. It was observed that complexation occurred in all powders, and that the fraction of drug inside the betaCD did not depend neither on the method of complexation nor on the processes of drying considered.
这项工作旨在证明两种模型药物（布洛芬，IB和吲哚美辛，IN）与β-环糊精（βCD）的络合作用，以及水在该过程中的影响，并比较它们的络合产率。考虑了两种方法：将药物、βCD的二元混合物捏合，以及将IB或IN包合在βCD的水溶液中。在后一种方法中，通过气流、喷雾干燥和冷冻干燥除去水。为了证明最终产品中络合物的形成，考虑了光学显微镜、紫外光谱、红外光谱、差示扫描量热法、X射线和核磁共振。将每种粉末加入酸性溶液（pH = 2）中以量化βCD腔内药物的浓度。由于药物溶解度随pH值增加，因此使用其他介质（pH = 5和7）来证明每种粉末中未络合的药物的存在。观察到所有粉末中都发生了络合作用，并且βCD内药物的比例既不取决于络合方法，也不取决于所考虑的干燥过程。
