Uekama K, Hirayama F, Fujise A, Otagiri M, Inaba K, Saitô H
J Pharm Sci. 1984 Mar;73(3):382-4. doi: 10.1002/jps.2600730323.
A solid complex of prostaglandin F2 alpha (dinoprost) with gamma-cyclodextrin in a molar ratio of 1:1 was obtained on the basis of the BS-type phase solubility diagram. The mode of interaction in the solid state was studied by powder X-ray diffractometry, thermal analysis, and carbon-13 cross polarization/magic angle spinning nuclear magnetic resonance (13C-CP/MAS-NMR) spectrometry. The X-ray diffraction and NMR data suggested that prostaglandin F2 alpha is included in the cylindrical channels formed by coaxial alignment of gamma-cyclodextrin molecules to give a channel type structure. Dissolution and thermal behaviors of the prostaglandin F2 alpha-gamma-cyclodextrin complex were examined and compared with the drug itself. The result indicated that the gamma-cyclodextrin complex may have great utility as a rapidly dissolving form of prostaglandin F2 alpha with improved thermal stability.
基于BS型相溶解度图，获得了摩尔比为1:1的前列腺素F2α（地诺前列素）与γ-环糊精的固体复合物。通过粉末X射线衍射法、热分析和碳-13交叉极化/魔角旋转核磁共振（13C-CP/MAS-NMR）光谱法研究了固态下的相互作用模式。X射线衍射和核磁共振数据表明，前列腺素F2α包含在由γ-环糊精分子同轴排列形成的圆柱形通道中，形成通道型结构。研究了前列腺素F2α-γ-环糊精复合物的溶解和热行为，并与药物本身进行了比较。结果表明，γ-环糊精复合物作为前列腺素F2α的快速溶解形式，具有改善的热稳定性，可能具有很大的实用性。
