色谱法在质子泵抑制剂药物对映体分离分析中的应用进展  

Application advances of chromatography in separation and determination of PPIs enantiomers

作　　者：关瑾[1] 刘芷含[1] 丁爽[1] 董西鑫 何传昌[1] 阎峰[1] 石爽[1] 

机构地区：[1]沈阳化工大学应用化学学院,沈阳110142

出　　处：《药物分析杂志》2014年第7期1143-1148,共6页Chinese Journal of Pharmaceutical Analysis

基　　金：辽宁省自然基金项目(20092055);辽宁省教育厅科学研究一般项目(L2012150)

摘　　要：手性药物的生物活性与其立体构型密切相关。目前新药研究的一个发展趋势是研制和生产光学纯的药物。质子泵抑制剂包括泰妥拉唑、泮托拉唑、兰索拉唑、雷贝拉唑和奥美拉唑,主要作用于胃壁细胞的H+/K+-ATP酶而抑制胃酸的分泌,用于治疗与胃酸分泌有关的疾病。质子泵抑制剂具有相似的结构特征,分子中存在1个手性硫原子中心,此类药物的药效学和药动学表现出对映体差异性。色谱法是对映体分离分析主要方法之一,本文综述了超临界色谱法、高效液相色谱法、毛细管电泳法等色谱法在拉唑类药物手性分离分析中的应用进展,对该领域的发展前景进行了展望。The bioactivity of chiral drugs is closely related to the stereostructures. Nowadays,production of optically pure drugs has been the trend of new drug development. Tenatoprazole and several related benzimidazoles including pantoprazole,lansoprazole,rabeprozole and omeprazole are a group of drugs- proton pump inhibitors（ PPIs）,whose main action is a pronounced and long- lasting reduction of gastric acid production. They bind to the proton pump（ H＋/K＋- ATPase） at the surface of gastric parietal cells and inhibit the final step in secretion of the H＋ions into the gastric lumen. The PPIs exist as a pair of enantiomers which may potentially exhibit different pharmacokinetic and pharmacodynamic profiles. Chiral chromatography method is one of the most powerful tools available for analyzing enantiomeric mixtures. This review summarizes the application progress of chromatographic techniques,including supercritical fluid chromatography,high performance liquid chromatography and capillary electrophoresis in the chiral separation of PPIs,and prospects the future development in this field.

关 键 词：质子泵抑制剂 泰妥拉唑 泮托拉唑 兰索拉唑 雷贝拉唑 奥美拉唑 手性分离 超临界色谱法 高效液相色谱法 毛细管电泳法 综述 

分 类 号：R917[医药卫生—药物分析学] O657.7[医药卫生—药学]