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固定相对使用反相色谱系统测定β受体阻滞剂亲脂性的影响。

The effect of stationary phase on lipophilicity determination of beta-blockers using reverse-phase chromatographic systems.

作者信息

Welerowicz Tomasz, Buszewski Boguslaw

机构信息

Department of Environmental Chemistry and Ecoanalytics, Faculty of Chemistry, Nicolas Copernicus University, Gagarin Street 7, PL-87100 Torun, Poland.

出版信息

Biomed Chromatogr. 2005 Dec;19(10):725-36. doi: 10.1002/bmc.507.

DOI:10.1002/bmc.507
PMID:15856476
Abstract

Evaluation of lipophilicity parameters for basic compounds using different chromatographic stationary phases is presented. An HPLC method for determination of lipophilic molecule-stationary phase interactions was based on gradient analysis. Differences in correlation between the lipophilicity of compounds and experimental chromatographic results obtained in pseudo-membrane systems showed a strong influence of stationary phase structure and physico-chemical properties. beta-Blocker drugs with varying lipophilicity and bio-activity were chosen as test compounds. The stationary phases used for the study were monolithic rod-structure C18 and silica gel octadecyl phase SG-C18 as reference material. The second group was silica gel-based polar-embedded alkylamide and cholesterolic phases. The mobile phase was composed of acetonitrile or methanol with ammonium acetate, and a linear gradient of methanol and acetonitrile in mobile phase was performed. A linear correlation of plots of log k(g) = f(log P) was observed, especially for polar-embedded phases, and this allowed log P(HPLC) to be calculated. The behavior of stationary phases in methanol and acetonitrile buffer showed differences between obtained log P(HPLC) values.

摘要

介绍了使用不同色谱固定相对碱性化合物亲脂性参数的评估。一种用于测定亲脂性分子与固定相相互作用的高效液相色谱法基于梯度分析。在伪膜系统中,化合物亲脂性与实验色谱结果之间的相关性差异显示出固定相结构和物理化学性质的强烈影响。选择具有不同亲脂性和生物活性的β受体阻滞剂药物作为测试化合物。用于该研究的固定相是整体棒状结构的C18和硅胶十八烷基相SG-C18作为参考材料。第二组是基于硅胶的极性嵌入烷基酰胺和胆固醇相。流动相由乙腈或甲醇与醋酸铵组成,并在流动相中进行甲醇和乙腈的线性梯度洗脱。观察到log k(g) = f(log P)图的线性相关性,特别是对于极性嵌入相,这使得可以计算log P(HPLC)。固定相在甲醇和乙腈缓冲液中的行为表明所获得的log P(HPLC)值之间存在差异。

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