Isolation and Characterization of S-Enantiomer in Montelukast

Maddala, Vijaya Lakshmi; Kakumani, Kishore Kumar; Chimalakonda, Kameswara Rao; Srinivasulu, Polisetty; Ray, Purna Chandra

doi:10.4236/ajac.2013.41008

Cited by 6 publications

(4 citation statements)

References 4 publications

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“…The International Conference of Harmonization (ICH) Q7 guiding principal mandates strict control of the S-enantiomer content in montelukast sodium bulk drug 15 . Moreover, literature has shown that montelukast sodium, as an LTD4 receptor antagonist, is superior to its S-enantiomer in both in-vitro and in-vivo studies 16 .…”

Section: Discussionmentioning

confidence: 99%

In-Vitro Comparative Study of Levocetirizine Dihydrochloride and Montelukast Sodium Release Profiles in Xyzal M Suspension and Other Marketed Syrup Formulations

Joshi,

Veligandla,

Rathod

et al. 2023

J. Drug Delivery Ther.

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Objectives: In-vitro comparative analysis of the release profile of levocetirizine dihydrochloride and montelukast sodium in Xyzal M Suspension and three commercially available syrup formulations. Method: The active components and their impurities were initially assayed in all formulations using a validated HPLC method. The enantiomeric impurities of montelukast sodium in different pH media were determined using the HPLC method specified in the United State Pharmacopoeia (USP) monograph. Additionally, dissolution studies and the soluble fractions of the components were evaluated in pH media that mimic the conditions of the gastrointestinal tract. The particle size was also analyzed using microscopic analysis. All parameters were examined in fresh, stressed, and aged samples of each formulation. Results: The assay results indicate the claimed potency of formulations. The total and enantiomeric impurities meet the limits set by the Indian Pharmacopoeia (<2%) and USP monograph (<0.2%), respectively. The particle size analysis demonstrated that montelukast remained suspended throughout the Xyzal M suspension. Levocetirizine in all formulations exhibited a soluble fraction of >70% after 1 and 24 hours in various pH media. For montelukast, the soluble fraction exceeded 50% in all syrup formulations. However, in Xyzal M suspension, montelukast was found to be 100% insoluble in all pH media after 1 and 24 hours, except in simulated intestinal fluid (~40-45%) after 24 hours. The absence of S-enantiomer, even in simulated intestinal fluid, indicates its presence in the pharmacologically active form. Conclusion: Xyzal M suspension is a promising dosage formulation for achieving desired pharmacological action, outperforming the syrup formulations. Keywords: Levocetirizine dihydrochloride, Montelukast sodium, Release profile, Suspension, Syrup, S-enantiomer

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Section: Discussionmentioning

confidence: 99%

In-Vitro Comparative Study of Levocetirizine Dihydrochloride and Montelukast Sodium Release Profiles in Xyzal M Suspension and Other Marketed Syrup Formulations

Joshi,

Veligandla,

Rathod

et al. 2023

J. Drug Delivery Ther.

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“…Analyst® TF 1.6 soware was used for data acquisition and data processing. The ion spray voltage for the DuoSpray™ ion source in ESI mode 19,20 was maintained at 4500 V and the temperature was set at 450 C. The auxiliary gas and curtain gas used were high purity nitrogen. Zero air was used as the nebulizer gas.…”

Section: Lc/ms/msmentioning

confidence: 99%

Isolation and identification of a potential unknown impurity in montelukast drug substance resulting from photolytic degradation

et al. 2016

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“…5). 35 The enantioseparation of chlorinated drugs [36][37][38] is of interest because, along with fluorine, the chlorine atom is also incorporated in several biologically active compounds. Indeed, it is considered to be isosteric and isolipophilic with the methyl group, able to alter the metabolism and is effective in inhibiting metabolic oxidation.…”

Section: Drugsmentioning

confidence: 99%

Liquid Chromatography Enantioseparations of Halogenated Compounds on Polysaccharide‐Based Chiral Stationary Phases: Role of Halogen Substituents in Molecular Recognition

2015

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Halogenated chiral molecules have become important in several fields of science, industry, and society as drugs, natural compounds, agrochemicals, environmental pollutants, synthetic products, and chiral supports. Meanwhile, the perception of the halogen moiety in organic compounds and its role in recognition processes changed. Indeed, the recognition of the halogen bond as an intermolecular interaction occurring when the halogen acts as a Lewis acid had a strong impact, particularly in crystal engineering and medicinal chemistry. Due to this renewed interest in the potentialities of chiral organohalogens, here we focus on selected recent applications dealing with enantioseparations of halogenated compounds on polysaccharide-based chiral stationary phases (CSPs), widely used in liquid chromatography (LC). In particular, recently the first case of halogen bonding-driven high-performance LC (HPLC) enantioseparation was reported on a cellulose-based CSP. Along with enantioseparations performed under conventional HPLC, representative applications using supercritical fluid chromatography (SFC) are reported.

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Isolation and Characterization of S-Enantiomer in Montelukast

Cited by 6 publications

References 4 publications

In-Vitro Comparative Study of Levocetirizine Dihydrochloride and Montelukast Sodium Release Profiles in Xyzal M Suspension and Other Marketed Syrup Formulations

In-Vitro Comparative Study of Levocetirizine Dihydrochloride and Montelukast Sodium Release Profiles in Xyzal M Suspension and Other Marketed Syrup Formulations

Isolation and identification of a potential unknown impurity in montelukast drug substance resulting from photolytic degradation

Liquid Chromatography Enantioseparations of Halogenated Compounds on Polysaccharide‐Based Chiral Stationary Phases: Role of Halogen Substituents in Molecular Recognition

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