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磷脂膜色谱用于评价药物与有序磷脂膜的相互作用 被引量:8
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作者 孙进 程刚 +1 位作者 何仲贵 王淑君 《药学学报》 CAS CSCD 北大核心 2003年第9期702-706,共5页
目的 使用磷脂膜色谱考察药物与有序磷脂膜的相互作用。方法 使用磷脂膜色谱测定药物与有序磷脂膜的相互作用强度 ,表示为药物的膜亲和性参数 (lgkIAM)。使用正辛醇 水系统测定药物的疏水性参数(lgDO W ,7 4 )。结果 在有机调节剂百... 目的 使用磷脂膜色谱考察药物与有序磷脂膜的相互作用。方法 使用磷脂膜色谱测定药物与有序磷脂膜的相互作用强度 ,表示为药物的膜亲和性参数 (lgkIAM)。使用正辛醇 水系统测定药物的疏水性参数(lgDO W ,7 4 )。结果 在有机调节剂百分比 ( φ) 0~ 30 %范围内 ,容量因子对数值 (lgk′IAM)与 φ呈现良好线性关系 ;对于 3种有机调节剂 (甲醇、乙醇和乙腈 ) ,lgk′IAM 与 φ间曲线截距相同 ,但斜率有显著差别。从对羟基苯甲酸甲酯到丁酯 ,每增加一个CH2 对测定的亲脂性参数差值 (ΔlgkIAM 和ΔlgDO W ,7 4 )具有相似的影响 ,但是从对羟基苯甲酸到甲酯的差值却明显偏离这个规律。结论 磷脂膜色谱是一个简便。 展开更多
关键词 磷脂色谱系统 有序磷脂膜的相互作用 亲脂性 正辛醇/水系统
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Interactions Mode of Amphoteric Molecules with Ordered Phospholipid Membrane
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作者 SUNJin CHENGGang HEZhong-gui WANGshu-jun CHENJi-min 《Journal of Chinese Pharmaceutical Sciences》 CAS 2003年第1期26-30,共5页
Aim To explore interaction mode between amphoteric molecules with the orderedphospholipid membrane. Methods Membrane interactions were determined by immobilized artificialmembrane (IAM) chromatography and solutes'... Aim To explore interaction mode between amphoteric molecules with the orderedphospholipid membrane. Methods Membrane interactions were determined by immobilized artificialmembrane (IAM) chromatography and solutes' hydrophobicity was measured by n-octanol/buffer system.Results The ampholytes, similar to bases, generally exhibited higher membrane affinity than expectedfrom their hydrophobicity, resulting from the attractive polar interaction with phospholipidmembrane. Furthermore, the strength of additional polar interaction with membrane (Δlg k_(IAM)) wasthen calculated. The Δlg k_(IAM) values were far greater for bases and ampholytes ranging from0.50 - 1.39, than those for acids and neutrals with the scope from - 0.55 - 0.44. ConclusionConsidering the microspecies distribution of amphoteric molecules, it was assumed that not onlyneutral and positive but also zwitterionic microspecies are capable of partitioning into orderedamphoteric lipid membrane with complementarily conformational and energetically favorableinteractions. 展开更多
关键词 membrane interactions amphoteric molecules polar extra-interaction immobilized artificial membrane chromatography
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