Abstract
Two sensitive and validated methods were developed for determination of a racemic mixture citalopram and its enantiomer S-(+) escitalopram. The first method was based on direct measurement of the intrinsic fluorescence of escitalopram using sodium dodecyl sulfate as micelle enhancer. This was further applied to determine escitalopram in spiked human plasma, as well as in the presence of common and co-administrated drugs. The second method was TLC densitometric based on various chiral selectors was investigated. The optimum TLC conditions were found to be sensitive and selective for identification and quantitative determination of enantiomeric purity of escitalopram in drug substance and drug products. The method can be useful to investigate adulteration of pure isomer with the cheap racemic form.
Highlights
Citalopram (Fig. 1) a selective serotonine re-uptake inhibitor (SSRI), has been used for the treatment of depression, social anxiety disorder, panic disorder and obsessive-compulsive disorder.[1,2,3] Citalopram is sold as a racemic mixture, consisting of 50% R-(−)-citalopram and 50% S-(+)-citalopram
In this study we develop two simple, economic and validated methods for determination of escitalopram and enantioseparation of its racemic mixture in drug substance and drug products
In this work a simple method was used for isolation of escitalopram from its drug product rather than the published procedure.[24]
Summary
Citalopram (Fig. 1) a selective serotonine re-uptake inhibitor (SSRI), has been used for the treatment of depression, social anxiety disorder, panic disorder and obsessive-compulsive disorder.[1,2,3] Citalopram is sold as a racemic mixture, consisting of 50% R-(−)-citalopram and 50% S-(+)-citalopram. As the S-(+) enantiomer has the desired antidepressant effect[4] it is marketed under the generic name of escitalopram. It has been shown that the R-enantiomer present in citalopram counteracts the activity of escitalopram. Citalopram and escitalopram have demonstrated different pharmacological and clinical effects.[5]. A number of techniques including spectrophotometric,[6,7] fluorimetric,[8,9] electrochemical,[10] chromatography[11,12] and capillary electrophoresis[13,14] have been developed for the determination of enantiomeric citalopram. Several chiral methods including LC15–20 and CE21,22 are available for separation of racemic citalopram, there is no report concerning enantiomeric separation of citalopram using thin layer chromatography (TLC)
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