Aim To compare lipophilicity measuring scale stemmed from immobilized artificial membrane chromatography and n octanol/buffer systems. Methods A test set consisted of 27 structurally diverse compounds. The lipophilici...Aim To compare lipophilicity measuring scale stemmed from immobilized artificial membrane chromatography and n octanol/buffer systems. Methods A test set consisted of 27 structurally diverse compounds. The lipophilicity of these were evaluated by both immobilized artificial memberane chromatography (IAMC) and n octanol/buffer systems, which were expressed as lg k IAM and lg D O/W,7 4 , respectively. Results With regard to each individual group, good correlation coefficient ( r 2) over 0 81 was obtained (0 82 for acid, 0 88 for neutral, 0 81 for base and 0 92 for ampholyte, respectively). However, a smaller r 2 (0 62) was acquired for all compounds studied than that of each individual group. Conclusion IAMC and n octanol/buffer systems were shown to be different in lipophilicity.展开更多
The thermodynamic partitioning behavior of solutes into immobilized artificial membrane(IAM) and n-octanol/water systems was investigated, including acidic,basic,and amphoteric substances.In an n-octanol/buffer system...The thermodynamic partitioning behavior of solutes into immobilized artificial membrane(IAM) and n-octanol/water systems was investigated, including acidic,basic,and amphoteric substances.In an n-octanol/buffer system,partitioning process was entropy-dominated for the most studied drugs,while partitioning of oxolinic and nalidixic acids into n-octanol phase was enthalpy-driven.In IAM chromatography,partitioning into membrane for the studied solutes was enthalpy-driven and an exothermal process.In conclusion,there is a significant difference of solutes′ partitioning mechanism into either IAM or an n-octanol phase,therefore,presenting the theoretical basis for differing lipophilicity measuring scale.展开更多
文摘Aim To compare lipophilicity measuring scale stemmed from immobilized artificial membrane chromatography and n octanol/buffer systems. Methods A test set consisted of 27 structurally diverse compounds. The lipophilicity of these were evaluated by both immobilized artificial memberane chromatography (IAMC) and n octanol/buffer systems, which were expressed as lg k IAM and lg D O/W,7 4 , respectively. Results With regard to each individual group, good correlation coefficient ( r 2) over 0 81 was obtained (0 82 for acid, 0 88 for neutral, 0 81 for base and 0 92 for ampholyte, respectively). However, a smaller r 2 (0 62) was acquired for all compounds studied than that of each individual group. Conclusion IAMC and n octanol/buffer systems were shown to be different in lipophilicity.
文摘The thermodynamic partitioning behavior of solutes into immobilized artificial membrane(IAM) and n-octanol/water systems was investigated, including acidic,basic,and amphoteric substances.In an n-octanol/buffer system,partitioning process was entropy-dominated for the most studied drugs,while partitioning of oxolinic and nalidixic acids into n-octanol phase was enthalpy-driven.In IAM chromatography,partitioning into membrane for the studied solutes was enthalpy-driven and an exothermal process.In conclusion,there is a significant difference of solutes′ partitioning mechanism into either IAM or an n-octanol phase,therefore,presenting the theoretical basis for differing lipophilicity measuring scale.