手性药物对映体的环糊精手性流动相、手性固定相HPLC法拆分

使用β-环糊精(CD)作为手性流动相添加剂或手性固定相,采用反相高效液相色谱法首次拆分了抗胆碱能药物盐酸戊乙奎醚、盐酸苯环壬酯和盐酸卡马特灵。结果表明,3个手性药物4对对映体完全达到基线分离。求得其包络常数、包络比和分离度,并结合其他结构类似的化合物,从结构—分离因子关系的角度研究了其拆分机理。详细研究了影响容量因子和分离度的各种因素。

CHIRAL RECOGNITION OF CYCLODEXTRIN SUPRAMOLECULAR SYSTEM——CHIRAL SEPARATION OF ENANTIOMER DRUGS BY REVERSED PHASE HPLC WITH CYCLODEXTRIN AS A MOBILE PHASE AND STATIONARY PHASE

Three new drugs, penequinine, bencynonate and kemadrine, have been baseline separated by reversed phase-HPLC using β-cyclodextrin as chiral mobile phase additive, whereas HPLC with β-cyclodextrin chiral stationary phase can only be used to baseline separate bencynonate. Binding constants, stoichiometry ratios and separation factors have been used to evaluate chiral recognition mechanism. Analyte retention mechanism is consistent with β-cyclodextrin inclusion hydrophobic models of interaction. Adding triethylamine to the mobile phase and decreasing pH can improve peak symmetry and reduce retention. Structural factors affecting chiral recognition and separation of β-cyclodextrin for 8 multi ring compounds have been discussed.