Enantioseparation method for montelukats by capillary electrophoresis applied to quality control

FLOR S; CONTIN M.; MARTINEFSKI M.,; ESTEVEZ PABLO; SCIOSCIA S.,; GARCIA BECERRA C.; TRIPODI V.,; LUCANGIOLI S.

Rosario

Encuentro; RICiFA 2012: 2ª Reunión Internacional de Ciencias Farmacéuticas; 2012

Ricifa

In the field of optical isomerism, pharmaceutical industry has become vital importance in recent years, since about 60% of the drugs included in the pharmacopoeias are racemates composed of equimolar mixtures of two enantiomers. The importance is that the enantiomers are chemical entities independent with different pharmacokinetic, pharmacodynamic and toxicological properties.Montelukast is a drug used in the treatment of chronic asthma, in preventing exercise-induced bronchospasm and in allergic rhinitis. Asthma is an inflammatory disorder of the respiratory tract characterized by reversible obstruction associated with bronchial hyperresponsiveness. The main inflammatory mediators involved in this process are the leukotrienes. Therefore, various leukotrienes modulatory agents have been developed like montelukats (1).Montelukast is a molecule with a chiral carbon in its chemical structure that confers optical isomerism. It has two enantiomers, R-isomer, which corresponds to properly montelukast and S-isomer, its principal synthesis impurity. Capillary electrophoresis using cyclodextrins as pseudoestationary phases is one of the analytical methods of choice for chiral analysis due to its high separation efficiency, resolution, versatility, low sample consumption and short analysis times (2). The aim of this work was to develop a selective analytical method for determining the S-isomer as well as its main related impurities at very low concentrations in both raw material and finished product of montelukast.