Losartan Interactions with 2-Hydroxypropyl-β-CD

氯沙坦与 2-羟丙基-β-环糊精的相互作用

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作者:Vasiliki Palli, Georgios Leonis, Nikoletta Zoupanou, Nikitas Georgiou, Maria Chountoulesi, Nikolaos Naziris, Demeter Tzeli, Costas Demetzos, Georgia Valsami, Konstantinos D Marousis, Georgios A Spyroulias, Thomas Mavromoustakos

Abstract

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.

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