R-besifloxacin hydrochloride is used in clinics as a consequence of its higher antibacterial activity. KeywordsEnantioseparation-Ofloxacin enantiomers-Bivalent ion-Ligand exchange chromatographyīesifloxacin hydrochloride is a novel chiral broad-spectrum fluoroquinolone developed for the treatment of bacterial conjunctivitis.
The separation method was used to analyze the ofloxacin enantiomers in different commercial medicines. L-isoleucine and 0.6mmoldm−3 Cu2+, room temperature), baseline separation of the two enantiomers was obtained with resolution of 1.32 in less than 30min.
Under the optimum conditions (methanol/water 20:80 v/v, containing 2.5mmoldm−3 On enantioseparation were evaluated the results showed that enantioselectivity was strongly affected by the ligand concentration The effect of different kinds and concentrations of ligands, bivalent ligand ions, and organic modifier, and temperature A C18 column was used with the mobile phase consisting of a methanol–water solution (containing different concentrations of l-isoleucine and copper sulfate) at flow rate of 0.5cm3min−1. The small resolution caused by complex formation is not perfect with the concentration of L-isoleucine and copper (II).ĪbstractThe enantioseparation conditions of ligand exchange chromatography were examined using ofloxacin enantiomers. We obtained the resolution of this separtion about 0.98. This research resulted 47 fractions which four of early fractions have correspond with the standard of (-)-ofloxacin and 43 other factions do not. Then the fractions were compared with the standard and the purity was tested by HPLC. Samples injected into the column and eluted by the mobile phase (consisting a mixture of water-methanol (88:12) and solution of L-isoleusine 4 mM and copper (II) sulfate 9 mM).
This study aims to separate mixture of ofloxacin enantiomers by forming diastereoisomeric with L-isoleusine and copper (II) into compound (-)-ofloxacin and (+)-ofloxacin and also to identify the optimum condition of separation using HPLC with preparative liquid chromatography column. Separation of enantiomers using chiral column is not quite economical separation, but the separation of enantiomers using a chiral column by converting the enantiomeric mixture into a diastereoisomeric form is the right solution. Enantiomers of drugs have different pharmacology and toxicology effects that need to be separated before it used to get the molecule target. Ofloxacin is an antibiotic with a broad range of uses in human and veterinary medicine to prevent or treat bacterial infections which has an enantiomeric mixture structure of (-)-ofloxacin and (+)-ofloxacin.
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