article · Chirality
A capillary electrophoresis strategy has been developed for the chiral enantioseparation of several pharmaceutical compounds with diverse acidic and basic properties. The method tests two anti-Alzheimer treatments, donepezil and rivastigmine, alongside four antifungal drugs, ketoconazole, itraconazole, fluconazole, and sertaconazole. The workflow uses an initial screening phase followed by an experimental design optimisation step. Testing evaluated various modified cyclodextrins as chiral selectors under initial conditions of 15 kilovolts, 25 degrees Celsius, and a phosphate-triethanolamine buffer at pH 2.5. A full factorial design examined the effects of pH and cyclodextrin concentration across nine experimental runs. While highly sulfated gamma-cyclodextrin achieved the highest resolution for five of the compounds, sulfobutyl ether beta-cyclodextrin successfully resolved all six drug racemates within a ten-minute runtime. Regression analysis indicated that linear models were insufficient, revealing complex interactions among experimental factors.
Many drugs exist as mirror-image molecules called enantiomers, which can differ significantly in their therapeutic effects and safety profiles. Developing fast, generic laboratory methods to separate and analyse these different forms across multiple drug classes helps analytical chemists assess drug purity more efficiently without having to invent entirely new separation conditions for each individual therapeutic molecule.
This work represents early-stage analytical method development relevant to quality control and formulation laboratories within the pharmaceutical industry. The rapid ten-minute separation protocol could enable testing facilities to streamline chiral purity screening for specific antifungal and anti-Alzheimer formulations. However, the abstract describes laboratory-scale method optimisation and does not indicate formal analytical validation or an immediate pathway to commercial implementation.
AI-generated from the published abstract. Always read the original work before citing.
The present study describes a generic strategy using capillary electrophoretic (CE) method for chiral enantioseparation of anti-Alzheimer drugs, namely, donepezil (DON), rivastigmine (RIV), and antifungal drugs, namely, ketoconazole (KET), Itraconazole (ITR), fluconazole (FLU), and sertaconazole (SRT) in which these drugs have different basic and acidic properties. Several modified cyclodextrins (CDs) were applied for enantioseparation of racemates such as highly sulfated α, γ CDs, hydroxyl propyl-β-CD, and Sulfobutyl ether-β-CD. The starting screening conditions consist of 50-mM phosphate-triethanolamine buffer at pH 2.5, an applied voltage of 15 kV, and a temperature of 25°C. The CE strategy implemented in the separation starts by screening prior to the optimization stage in which an experimental design is applied. The design of experiment (DOE) was based on a full factorial design of the crucial two factors (pH and %CD) at three levels, to make a total of nine (3<sup>2</sup> ) experiments with high, intermediate, and low values for both factors. Evaluation of the proposed strategy pointed out that best resolution was obtained at pH 2.5 for five racemates using low percentages of HS-γ-CD, while SBE-β-CD was the most successful chiral selector offering acceptable resolution for all the six racemates, with the best separation at low pH values and at higher %CD within 10-min runtime. Regression study showed that the linear model shows a significant lack of fit for all chiral selectors, anticipating that higher orders of the factors are most likely to be present in the equation with possible interactions.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.1002/chir.22777
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
