Abstract
Venlafaxine (VFX) is a modern antidepressant from the serotonin and norepinephrine reuptake inhibitor (SNRI) class. It is a chiral substance used in therapy as a racemate, but differences between the pharmacological properties of the two enantiomers have been reported. The current article presents the development of a simple capillary electrophoresis (CE) method for the rapid chiral separation of VFX enantiomers. A complex cyclodextrin (CD) screening at four different pH levels was carried out to establish the optimum chiral selector; carboxymethyl-β-CD (CM-β-CD) at pH 2.5 was selected for further method development. An initial “one factor at time” (OFAT) screening strategy was used to establish the influence of analytical parameters on the separation, followed by a face centered central composite design (FCCD) for the optimization process. The analytical performances of the newly developed method were verified in terms of accuracy, linearity, precision, repeatability, and sensitivity. The method was used for the determination of VFX enantiomer ratio in pharmaceutical forms. Finally, computer modelling of VFX-CD complexes was undertaken to characterize host–guest chiral recognition.
Highlights
Chirality plays an important role in modern drug research, as chiral drug enantiomers can exhibit different pharmacokinetic and pharmacodynamic properties
R,S-Venlafaxine hydrochloride was acquired from Ercros Pharmaceuticals (Barcelona, Spain)
Migration times of VFX decreased in an achiral system with the increase of the background electrolyte (BGE) pH value; at pH above 5.0 where electroosmotic flow (EOF)
Summary
Chirality plays an important role in modern drug research, as chiral drug enantiomers can exhibit different pharmacokinetic and pharmacodynamic properties. Examples of chiral pharmaceuticals with differences between enantiomers activity can be found in many pharmaceutical classes: β-blockers, calcium channel blockers, proton pump inhibitors, H1 antihistamines, anticoagulants, angiotensin converting enzyme inhibitors, and others [2,3,4]. Among these substances one of the most interesting and intriguing class of chiral pharmaceuticals are the one of modern antidepressants, represented by selective serotonin reuptake inhibitors (SSRIs) and serotonin and norepinephrine reuptake inhibitors (SNRIs) [5]. A bicyclic phenylethylamine derivative with asymmetric carbon atom its structure, which leads to the existence of two enantiomers, S-VFX and.
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