Department of Chemistry, School of Sciences, National and Kapodistrian University of Athens, 15784 Athens, Greece.
Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, 15784 Athens, Greece.
Molecules. 2022 Apr 8;27(8):2421. doi: 10.3390/molecules27082421.
Losartan potassium salt (LSR) is a well-known antihypertensive drug with proven beneficial effects on human health. Its formulation with the non-toxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) could improve its pharmacological profile. Thus, its molecular interactions are studied using a combination of Differential Scanning Calorimetry (DSC), Nuclear Magnetic Resonance (NMR) and Molecular Dynamics (MD). First, its complexation is shown through Differential Scanning Calorimetry as lyophilization provided distinct thermal properties in comparison to the mixture. The complexation is further proved by utilizing the chemical shift changes in the complexation and T1 values. Furthermore, the reversible favorable complexation was shown by MD calculations. Such physical chemical properties provide evidence that this formulation must be further explored through biological experiments.
氯沙坦钾盐(LSR)是一种著名的降压药物,对人类健康有明确的有益作用。其与无毒的 2-羟丙基-β-环糊精(2-HP-β-CD)的配方可以改善其药理学特性。因此,使用差示扫描量热法(DSC)、核磁共振(NMR)和分子动力学(MD)的组合研究了其分子相互作用。首先,通过差示扫描量热法显示其络合作用,与混合物相比,冻干提供了明显的热特性。通过络合和 T1 值的化学位移变化进一步证明了络合作用。此外,MD 计算表明了这种可逆的有利络合作用。这些物理化学性质证明,这种配方必须通过生物实验进一步探索。