Abstract

One of the priority tasks of the pharmaceutical industry is to manufacturing high-quality, effective, and safe medicines. Thus, the interest in for searching biologically active compounds perspective for the creation of new drugs is growing. The aim of this work was to study the chromatographic behavior of benzimidazole and its firstly synthesized derivatives by reversed-phase–HPLC (RP-HPLC). The sorption of benzimidazole and its five derivatives from liquid solutions of various qualitative composition on octadecyl silica gel was studied by the method of RP HPLC. Mobile phases contained ionic liquids (IL) as an additive: 1-butyl-2,3-dimethylimidazolium tetrafluoroborate ([BdMIM] [BF₄]) and 1-butyl-3 methylimidazolium bromide ([BMIM] [Br]). The effect of eluent’s and ILs’ nature on benzimidazoles’ retention from six compositions of mobile phases at a ratio of H₂O (or aqueous solution of IL)/organic modifier (acetonitrile or methanol) of 50/50 vol.% was studied. The standard changes in the enthalpy of the benzimidazoles’ transition from the aqueous-organic eluent to the octadecyl silica gel layer and the entropy components of the process were calculated based on the temperature dependences of the retention factors. A comparative analysis of the enthalpies’ and entropy components’ values of the sorption process for the studied benzimidazoles was carried out. Also the enthalpy–entropy dependences were considered.

摘要

制药行业的首要任务之一是生产高质量，有效和安全的药物。因此，对于寻找生物活性化合物的观点以产生新药物的兴趣正在增长。这项工作的目的是通过反相HPLC（RP-HPLC）研究苯并咪唑及其首次合成的衍生物的色谱行为。采用反相高效液相色谱法研究了各种定性组成的液体溶液中苯并咪唑及其五种衍生物在十八烷基硅胶上的吸附性能。流动相包含离子液体（IL）作为添加剂：1-丁基-2,3-二甲基咪唑四氟硼酸酯（[BdMIM] [BF ₄]）和1-丁基-3甲基咪唑鎓溴化物（[BMIM] [Br]）。研究了在H ₂ O（或IL的水溶液）/有机改性剂（乙腈或甲醇）的体积比为50/50％的情况下，六种流动相组成对洗脱液和IL的性质对苯并咪唑保留的影响。基于保留因子的温度依赖性，计算了苯并咪唑从水性有机洗脱液到十八烷基硅胶层的焓变的标准变化以及该过程的熵成分。对所研究的苯并咪唑的吸附过程的焓和熵成分值进行了比较分析。还考虑了焓-熵的依赖性。