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首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >Relation between retention factors of immunosuppressive drugs in microemulsion electrokinetic chromatography with biosurfactants and octanol-water partition coefficients.
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Relation between retention factors of immunosuppressive drugs in microemulsion electrokinetic chromatography with biosurfactants and octanol-water partition coefficients.

机译:微乳液电动色谱中具有生物表面活性剂的免疫抑制药物的保留因子与辛醇-水分配系数之间的关系。

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Retention (capacity) factors (k' values) of immunosuppressive drugs were determined in microemulsion electrokinetic chromatography (MEEKC) systems as a tool for the indirect estimation of partition coefficients (P(OW)) between 1-octanol and water. The microemulsions were based on phosphatidylcholine (PC) and bile acids (BAs) as biosurfactants and isopropyl myristate (IPM) as oil. Immunosuppressants were azathioprine (AZA), mycophenolate mofetil (MMF), tacrolimus (FK506) and cyclosporine A (CyA). Capacity factors of the analytes were determined from electrophoretic mobilities using an aqueous phosphate buffer (20 mM; pH 7.5) for all the systems. Retention was compared with that in the most commonly used microemulsion based on sodium dodecyl sulphate (SDS). logP(OW) versus logk' calibration lines were constructed using reference compounds with known P(OW). In addition, data of logP(OW) of the immunosuppressants were determined by partitioning between octanol and water, and were calculated by the aid of computer program. A different sequence of logP(OW) for two analytes was found in the biosurfactant-based systems compared with the SDS-containing one. Excellent agreement was observed between the logP(OW) values derived from the microemulsions containing deoxycholate compared with the data determined by partitioning between octanol and water. It was concluded that the retention factors in the systems with biosurfactants are good estimators for the partitioning in biological systems.
机译:在微乳液电动色谱(MEEKC)系统中确定了免疫抑制药物的保留(容量)因子(k'值),作为间接估算1-辛醇和水之间分配系数(P(OW))的工具。微乳液基于磷脂酰胆碱(PC)和胆汁酸(BAs)作为生物表面活性剂,以及肉豆蔻酸异丙酯(IPM)作为油。免疫抑制剂为硫唑嘌呤(AZA),霉酚酸酯(MMF),他克莫司(FK506)和环孢霉素A(CyA)。对于所有系统,使用磷酸盐水溶液(20 mM; pH 7.5)通过电泳迁移率确定分析物的容量因子。将保留率与最常用的基于十二烷基硫酸钠(SDS)的微乳液的保留率进行了比较。使用具有已知P(OW)的参考化合物构建logP(OW)与logk'校准线。另外,通过在辛醇和水之间分配来确定免疫抑制剂的logP(OW)数据,并借助计算机程序进行计算。与基于SDS的系统相比,在基于生物表面活性剂的系统中发现了两种分析物的logP(OW)序列不同。与通过辛醇和水分配确定的数据相比,在包含脱氧胆酸盐的微乳液中得到的logP(OW)值之间观察到极好的一致性。结论是具有生物表面活性剂的系统中的保留因子是生物系统中分配的良好估计。

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