Improvement of some pharmaceutical properties of nocloprost by β- and γ-Cyclodextrin Complexation |
| |
Authors: | Masahiko Kurihara Fumitoshi Hirayama Kaneto Uekama Masaki Yamasaki |
| |
Affiliation: | (1) Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, 862 Kumamoto, Japan;(2) Department of Biochemistry, Medical School, Kumamoto University, 2-2-1 Honjo, 860 Kumamoto, Japan |
| |
Abstract: | Inclusion complexation of nocloprost, a potent antiulcer prostaglandin derivative, with -, -, and -cyclodextrins (CyDs) in aqueous solutions has been studied by the solubility method and13C-NMR spectroscopy. The steric requirement of host-guest interaction was reflected in the magnitude of the stability constants and the thermodynamic parameters of the inclusion complexes. Solid complexes of nocloprost with - and -CyDs in a molar ratio of 1 : 2 were obtained on the basis of aBs-type phase solubility diagram. The X-ray diffraction data suggested that nocloprost is included in the cylindrical channel formed by coaxial alignment of -CyD molecules to give a channel type structure. Release and thermal behavior of the solid complexes was examined and compared with nocloprost itself. The results indicated that the -CyD complex may have great utility among the three CyDs, being a rapid dissolving form of nocloprost with improved thermal stability. |
| |
Keywords: | Nocloprost cyclodextrin inclusion complex stability constant thermodynamic parameter solubility release rate |
本文献已被 SpringerLink 等数据库收录! |
|