Abstract
A normal phase enantioselective high performance liquid chromatographic method was developed for enantiomeric resolution of Ezetimibe it reduces the overall delivery of cholesterol to the liver. The enantiomers of Ezetimibe were resolved on a Chiral Pak AS-H (250 × 4.6 mm, 5 um) column using a mobile phase system containing n-Hexane, etha-nol, 2-Propanol and Trifloroacetic acid (84:12:4:0.1 v/v). The resolution between enantiomers was found to be more than 2.0. The limit of detection and limit of quantification of (R)-enantiomer were found to be 0.2 ug/mL and 0.5 ug/mL, respectively, for 10 uL injection volume. The sample solution and mobile phase were found to be stable for at least 48 h. The final optimized method was successfully applied to separate (R)-enantiomer from Ezetimibe and was proven to be reproducible and accurate for the quantitative determination of (R)-enantiomer in bulk drugs.
Highlights
Enantiomers of racemic drugs often show different behaviors in pharmacological action and metabolic process
There was an indication of separation on Chiralpak AS-H (250 × 4.6 mm, 5 μm) column using a mobile phase consisting of n-hexane, ethanol, 2-propanol and trifluoroacetic acid acid (84:12:4:0.1 v/v)
The HPLC condition of the final method was evaluated for its specificity, limit of detection (LOD), limit of Quantification (LOQ), linearity, accuracy, precision, robustness and stability
Summary
Enantiomers of racemic drugs often show different behaviors in pharmacological action and metabolic process. It is not uncommon for one enantiomer to be active while other isomer is toxic in biological systems. The development of the methods for the quantitative analysis of Chiral compounds and for the assessment of enantiomeric purity is extremely challenging, because the same physical and chemical properties of the two enantiomers make discriminating and separating them very difficulty [4]. Ezetimibe selectively prevents the absorption of cholesterol from dietary and biliary sources by blocking the transport of cholesterol through the intestinal wall. The developed chiral HPLC method was reproducible and accurate for the quantitative determination of (R)-enantiomer in Ezetimibe
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