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Enantioselective Separation of Antiretroviral Drug Combinations on Immobilized Polysaccharide CSPs Under Subcritical Conditions Using Supercritical Fluid Chromatography Apparatus
Chromatographia ( IF 1.7 ) Pub Date : 2021-01-15 , DOI: 10.1007/s10337-021-04004-3
Thirupathi Choppari , Srinivasu Gunnam , Lakshmi Narayana Chennuru , Chandra Sekhara Rao Boddala , C. P. Murthy , M. V. N. Kumar Talluri

A stereoselective method has been developed for the chiral separation of the enantiomers of eight antiretroviral (ARV) drugs under subcritical conditions using a supercritical fluid chromatography apparatus. The ARVs: abacavir, tenofovir alafenamide, lamivudine, efavirenz, atazanavir, emtricitabine, dolutegravir and darunavir, are used to treat the human immunodeficiency virus (HIV). The antiretroviral therapy has been planned to manage and control the severity of HIV and prolong the patient’s life. The use of multiple drugs that act on different viral targets is known as highly active antiretroviral therapy, which slows down the development of AIDS and prevents opportunistic infections that often lead to death. The immobilized meta-substituted polysaccharide-derived carbamate columns (CSPs) have been chosen for chiral SFC separation of selected ARVs. The ARVs enantioseparation was achieved on CSPs by using different alcohol co-solvents (methanol, ethanol and isopropyl alcohol) with diethylamine (DEA) as an additive to the mobile phase. These CSPs exhibit an exceptional level of complementary chiral recognition characteristics by applying different screening and method optimization strategies. The cellulose tris(3,5-dichlorophenylcarbamate) immobilized on silica gel was found to be useful for the chiral SFC analysis of abacavir, lamivudine, efavirenz combination ARV analysis, and the method was optimized by studying the effects of different mobile phase additives, column temperatures and flow rates. The amylose tris(3-chloro, 5-methylphenyl carbamate) immobilized on silica gel was found to be useful for the chiral SFC analysis of emtricitabine, abacavir and dolutegravir combination ARV drugs.

中文翻译:

使用超临界流体色谱仪在亚临界条件下对固定化多糖 CSP 上的抗逆转录病毒药物组合进行对映选择性分离

开发了一种立体选择性方法,用于使用超临界流体色谱仪在亚临界条件下手性分离八种抗逆转录病毒 (ARV) 药物的对映异构体。ARVs:阿巴卡韦、替诺福韦艾拉酚胺、拉米夫定、依法韦仑、阿扎那韦、恩曲他滨、多替拉韦和达芦那韦,用于治疗人类免疫缺陷病毒 (HIV)。抗逆转录病毒疗法已计划用于管理和控制 HIV 的严重程度并延长患者的生命。使用多种作用于不同病毒靶点的药物被称为高效抗逆转录病毒疗法,可减缓艾滋病的发展并防止经常导致死亡的机会性感染。已选择固定化的间位取代多糖衍生氨基甲酸酯柱 (CSP) 用于选定 ARV 的手性 SFC 分离。通过使用不同的醇共溶剂(甲醇、乙醇和异丙醇)和二乙胺 (DEA) 作为流动相的添加剂,在 CSP 上实现 ARV 对映分离。通过应用不同的筛选和方法优化策略,这些 CSP 表现出卓越水平的互补手性识别特征。发现固定在硅胶上的三(3,5-二氯苯基氨基甲酸酯)纤维素可用于阿巴卡韦、拉米夫定、依法韦仑组合 ARV 分析的手性 SFC 分析,并通过研究不同流动相添加剂、色谱柱的影响来优化方法温度和流速。直链淀粉三(3-氯,
更新日期:2021-01-15
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