Odović Jadranka, Karljiković-Rajić Katarina, Trbojević-Stanković Jasna, Stojimirović Biljana, Vladimirov Sote
Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
Iran J Pharm Res. 2012 Summer;11(3):763-70.
In this assay, the evaluation of lipophilicity of four ACE-inhibitors and hydrochlorothiazide (HCTZ) with RP-TLC on cellulose layers was described using three binary solvent systems. The selected ACE inhibitors had sufficiently different structures which can indicate the method suitability for their lipophilicity evaluation as the model substances in comparison with HCTZ. In addition, the linear relationship between the RM-values and composition of mobile phases was established in the current study. From the regression data of the plots, the hydrophobicity parameters, R(0) M and m, were determined and C0 parameter was calculated. The correlations between the experimentally obtained hydrophobicity parameters and calculated log p values were studied. Furthermore, the obtained results were compared with those previously obtained on RP-18 modified silica gel. Very good correlation (r = 0.91; water-ethanol solvent system) between the chromatographically obtained hydrophobicity parameters and calculated log p values confirmed the selection of ACE inhibitors since lisinopril and quinapril were on the opposite sites of linear relationship. The results indicate that cellulose as an easily available sorbent can be successfully used for the lipophilicity investigation of examined substances with RP-TLC.
在本试验中，使用三种二元溶剂系统描述了在纤维素层上用反相薄层色谱法（RP-TLC）对四种血管紧张素转换酶抑制剂（ACE抑制剂）和氢氯噻嗪（HCTZ）的亲脂性进行评估。所选的ACE抑制剂具有足够不同的结构，与HCTZ相比，可作为模型物质表明该方法对其亲脂性评估的适用性。此外，本研究建立了比移值（RM值）与流动相组成之间的线性关系。根据图谱的回归数据，确定了疏水性参数R(0)M和m，并计算了C0参数。研究了实验获得的疏水性参数与计算得到的log P值之间的相关性。此外，将所得结果与先前在反相18改性硅胶上获得的结果进行了比较。色谱法获得的疏水性参数与计算得到的log P值之间具有很好的相关性（r = 0.91；水-乙醇溶剂系统），这证实了ACE抑制剂的选择是合理的，因为赖诺普利和喹那普利处于线性关系的相反位置。结果表明，纤维素作为一种容易获得的吸附剂，可成功用于用RP-TLC对被测物质进行亲脂性研究。
