Enantioresolution of (RS)‐baclofen by liquid chromatography: A review

Abstract

Baclofen is a commonly used racemic drug and has a simple chemical structure in terms of the presence of only one stereogenic center. Since the desirable pharmacological effect is in only one enantiomer, several possibilities exist for the other enantiomer for evaluation of the disposition of the racemic mixture of the drug. This calls for the development of enantioselective analytical methodology. This review summarizes and evaluates different methods of enantioseparation of (RS)-baclofen using both direct and indirect approaches, application of certain chiral reagents and chiral stationary phases (though very expensive). Methods of separation of diastereomers of (RS)-baclofen prepared with different chiral derivatizing reagents (under microwave irradiation at ease and in less time) on reversed-phase achiral columns or via a ligand exchange approach providing high-sensitivity detection by the relatively less expensive methods of TLC and HPLC are discussed. The methods may be helpful for determination of enantiomers in biological samples and in pharmaceutical formulations for control of enantiomeric purity and can be practiced both in analytical laboratories and industry for routine analysis and R&D activities.

Bioassay, determination and separation of enantiomers of atenolol by direct and indirect approaches using liquid chromatography: A review

“…Both direct and indirect approaches of separation of enantiomers (using LC) have their own advantages and limitations depending upon the situation, particularly, in terms of the source and amount of sample availability, chemical structure of the analyte and the ease of availability of laboratory facilities. Various reviews on separation of enantiomers of ( RS )‐baclofen (Batra & Bhushan, ), ( RS )‐bupropion (Batra & Bhushan, ), ( RS )‐Naproxen (Batra & Bhushan, ) and dl ‐penicillamine (Bhushan & Kumar, ), have discussed various issues related to ‘direct’ and ‘indirect’ (modes of) enantioseparation; therefore, such general aspects are not being discussed in this paper.…”

Stereochemical facets of clinical β‐blockers: An overview

“…Recently, Batra and Bhushan reported a comprehensive review of the LC enantioseparation of atenolol and propranolol . Both direct and indirect methods for enantiomeric resolution have been discussed using HPLC.…”

Liquid chromatographic enantioseparation, determination, bioassay and isolation of enantiomers of Ketorolac: A review

“…Both the approaches have their own advantages and limitations and choice of method would depend upon source and amount of sample available, chemical structure of the analyte and the ease of availability of laboratory facilities. Different reviews and monographs on enantiomeric resolution [10][11][12][13] including those on separation of enantiomers of different active pharmaceutical ingredients (APIs) of a variety of racemic drugs [14][15][16] have discussed various issues related to 'direct' and 'indirect' (modes of) enantioseparation, therefore, such general aspects are not being discussed in this paper. Literature reveals that there has been no attempt to review methods of LC enantioseparation of Ket in spite of its pharmaceutical applications in modern clinical therapy and the importance of enantioseparation.…”