溶液环境和静电因素对厄贝沙坦互变异构体结晶的影响。
The effect of solution environment and the electrostatic factor on the crystallisation of desmotropes of irbesartan.
作者信息
Araya-Sibaja Andrea M, Urgellés Mariola, Vásquez-Castro Felipe, Vargas-Huertas Felipe, Vega-Baudrit José Roberto, Guillén-Girón Teodolito, Navarro-Hoyos Mirtha, Cuffini Silvia L
机构信息
Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE 1174-1200 Pavas San José Costa Rica.
Centro de Investigación y Extensión en Materiales, Escuela de Ciencia e Ingeniería de los Materiales, Tecnológico de Costa Rica Cartago 159-7050 Costa Rica.
出版信息
RSC Adv. 2019 Feb 11;9(9):5244-5250. doi: 10.1039/c8ra10146a. eCollection 2019 Feb 5.
The experimental conditions necessary for stabilising irbesartan (IBS) tautomers in solution and selectively obtaining the desmotropic crystal forms are presented herein. 1H and 2H tautomers were stabilized in specific solution conditions and the 2H-tetrazole⋯imidazole interaction was confirmed by solution-state NMR. The results showed that highly polar and polarisable solvents (higher values of the electrostatic factor (EF)) lead to the crystallisation of IBS form B. Furthermore, the variations of pH in methanol, in turn, determined the crystallisation of desmotropes A and/or B.
本文介绍了在溶液中稳定厄贝沙坦（IBS）互变异构体并选择性获得反位晶体形式所需的实验条件。1H和2H互变异构体在特定溶液条件下得以稳定，并且通过溶液态核磁共振证实了2H-四唑⋯咪唑相互作用。结果表明，高极性和可极化溶剂（静电因子（EF）值较高）会导致IBS B型结晶。此外，甲醇中pH值的变化进而决定了反位异构体A和/或B的结晶。
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