Improving the aqueous stability of prostaglandin E2 and prostaglandin A2 by inclusion complexation with methylated-beta-cyclodextrins.

作者: Fumitoshi Hirayama , Masahiko Kurihara , Kaneto Uekama

DOI: 10.1248/CPB.32.4237

关键词: Beta-CyclodextrinsProstaglandin E2Chemical stabilityOrganic chemistryReaction rate constantMedicinal chemistryProstaglandinAqueous solutionChemistryReaction rateIsomerization

摘要: The effects of two methylated-β-cyclodextrins, heptakis (2, 6-di-O-methyl)-β-cyclodextrin (DM-β-CyD) and 3, 6-tri-O-methyl)-β-cyclodextrin (TM-β-CyD), on the dehydration rate prostaglandin E2 (PGE2) isomerization A2 (PGA2) in aqueous alkaline solution were investigated comparison with natural β-cyclodextrin (β-CyD). In contrast to acceleration effect β-CyD, both DM-β-CyD TM-β-CyD significantly retarded reaction rates. stabilizing was larger than that TM-β-CyD. Stability constants complexes kinetically determined basis 1 : inclusion complex formation. data suggest is useful stabilization PGEs PGAs solution.

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