摘要
利用氟脲嘧啶(5-Fu)和呋氟脲嘧啶(FT-207)与β-环糊精(β-CD)形成主—客包合物后^(19)F化学位移的变化研究了这些包合物的组成和稳定常数。5-Fu和FT-207均与β-CD形成1:1包合物,包合物的稳定常数在40℃分别为17.0±1.7mol^(-1)·L和9.0±0.1mol^(-1)·L。研究结果还表明,与β-CD形成包合物后,5-Fu和FT-207的^(19)F化学位移的变化有较明显的差异,提示了它们分子中的氟脲嘧啶环在β-CD疏水性内腔中的位置是不同的。
The composition and stability constants of the host-guest inclusion complexes of β-cyclodextrin (β-CD)with fluorouracil (5-Fu) and ftorafur (FT-207) were studied by ^(19)F NMR. The ^(19)F chemical shift changes (△) of 5-Fu and FT-207 on complexation with β-CD were used to determine the stoichiometry of these inclusion complexes by Job plot. It was shown that both 5-Fu and FT-207 formed 1: 1 inclusion complexes with β-CD. The stability constants (K_c) of their complexes with β-CD, calculated from the slope of linear relation between △/C_(CD)~0 and △(C_(CD)~0 being the initial concentration of β-CD) were found to be 17.0±1.7 mol^(-1)·L and 9.0±0.1 mol^(-1)·L at 40℃ respectively. The ^(19)F chemical shifts of these complexes relative to their free forms were also obtained and discussed in terms of the structures of these β-CD inclusion complexes in aqueous solution.
出处
《药学学报》
CAS
CSCD
北大核心
1990年第5期345-348,共4页
Acta Pharmaceutica Sinica
关键词
氟脲嘧啶
呋氟脲嘧啶
核磁共振
Fluorouracil (5-Fu)
Ftorafur (FT-207) β-Cyclodextrin (β-CD)
Host-guest inclusion complex
^(19)F NMR
