Uekama K, Imai T, Maeda T, Irie T, Hirayama F, Otagiri M
J Pharm Sci. 1985 Aug;74(8):841-5. doi: 10.1002/jps.2600740808.
The inclusion behavior of methylated beta-cyclodextrins, heptakis(2,6-di-O-methyl)-beta-cyclodextrin and heptakis-(2,3,6-tri-O-methyl)-beta-cyclodextrin in solution and the solid state was compared with that of natural beta-cyclodextrin using an anti-inflammatory drug, flurbiprofen, as a guest molecule. Stability constants were determined by the solubility method at various temperatures, and the thermodynamic parameters were calculated for inclusion complex formation in aqueous solution. The solid complexes were obtained in a molar ratio of 1:1, and their dissolution behavior and release from suppository bases were examined. The data suggest that the inclusion mode of the complex with 3 is somewhat different from that of the complexes with 1 and 2. From a practical point of view, 2 seems to be particularly useful for improving the pharmaceutical properties of flurbiprofen in various dosage forms.
以抗炎药物氟比洛芬作为客体分子，将甲基化β-环糊精、七（2,6-二-O-甲基）-β-环糊精和七（2,3,6-三-O-甲基）-β-环糊精在溶液和固态中的包合行为与天然β-环糊精的包合行为进行了比较。通过溶解度法在不同温度下测定了稳定常数，并计算了在水溶液中形成包合物的热力学参数。以1:1的摩尔比获得了固体配合物，并研究了它们的溶解行为和从栓剂基质中的释放情况。数据表明，与3形成的配合物的包合模式与与1和2形成的配合物的包合模式略有不同。从实际角度来看，2似乎对改善氟比洛芬在各种剂型中的药物性质特别有用。
