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Cyclodextrine screening for the chiral separation of carvedilol by capillary electrophoresis.

Hancu G, Cârje A, Iuga I, Fülöp I, Szabó ZI - Iran J Pharm Res (2015)

Bottom Line: Carvedilol is administered as a racemic mixture of the R(+)- and S(-)-enantiomers, although it was demonstrated that the two enantiomers exhibit different pharmacological effects and stereoselective pharmacokinetics.The aim of this study was the evaluation of several native and derivatized cyclodextrines as chiral selectors for the separation of carvedilol enantiomers.The effects of CD concentration, pH value and composition of the background electrolyte, capillary temperature, running voltage and injection parameters have been investigated.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Târgu Mureş, Romania.

ABSTRACT
Carvedilol is administered as a racemic mixture of the R(+)- and S(-)-enantiomers, although it was demonstrated that the two enantiomers exhibit different pharmacological effects and stereoselective pharmacokinetics. The aim of this study was the evaluation of several native and derivatized cyclodextrines as chiral selectors for the separation of carvedilol enantiomers. Stereoselective interactions were observed with four cyclodextrines (β-CD, hydroxypropyl-β-CD, randomly methylated β-CD and sulfobuthyl ether- β-CD). The effects of CD concentration, pH value and composition of the background electrolyte, capillary temperature, running voltage and injection parameters have been investigated. The method was validated for precision of peak-area response, linearity range and limits of detection and quantification. An efficient stereoselective capillary zone electrophoretic method was developed for the determination of carvedilol enantiomers using a simple 25 mM phosphate buffer at a pH = 2.5 and 10 mM β-CD as chiral selector, resulting in baseline separation of the two enantiomers with sharp peaks and relatively short analysis time. Highly satisfactory results were obtained from the analysis of carvedilol from tablets, indicating that the method is suitable for routine analysis of carvedilol in pharmaceutical products.

No MeSH data available.


Related in: MedlinePlus

Effect of CD concentration on the chiral resolution (electrophoretic conditions: BGE 25 mM phosphoric acid, pH = 2.5, voltage + 20 kV, temperature 20 ˚C, hydrodinamic injection 50 mbar/3 s., UV detection 242 nm).
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Figure 2: Effect of CD concentration on the chiral resolution (electrophoretic conditions: BGE 25 mM phosphoric acid, pH = 2.5, voltage + 20 kV, temperature 20 ˚C, hydrodinamic injection 50 mbar/3 s., UV detection 242 nm).

Mentions: If complexation was observed but insuficient resolution was achieved, we increased the concentration of the chiral selector (5-40 mM) until satisfactory separation was obtained. When using β-CD as chiral selector the maximum concentration was 20 mM, due to its poor solubility in aqueous solutions. Resolution of the enantiomers was calculated and the optimal concentration for the separation was determined. Figure 2 shows the effect of chiral selector concentrations on the carvedilol enantiomers separation.


Cyclodextrine screening for the chiral separation of carvedilol by capillary electrophoresis.

Hancu G, Cârje A, Iuga I, Fülöp I, Szabó ZI - Iran J Pharm Res (2015)

Effect of CD concentration on the chiral resolution (electrophoretic conditions: BGE 25 mM phosphoric acid, pH = 2.5, voltage + 20 kV, temperature 20 ˚C, hydrodinamic injection 50 mbar/3 s., UV detection 242 nm).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4403058&req=5

Figure 2: Effect of CD concentration on the chiral resolution (electrophoretic conditions: BGE 25 mM phosphoric acid, pH = 2.5, voltage + 20 kV, temperature 20 ˚C, hydrodinamic injection 50 mbar/3 s., UV detection 242 nm).
Mentions: If complexation was observed but insuficient resolution was achieved, we increased the concentration of the chiral selector (5-40 mM) until satisfactory separation was obtained. When using β-CD as chiral selector the maximum concentration was 20 mM, due to its poor solubility in aqueous solutions. Resolution of the enantiomers was calculated and the optimal concentration for the separation was determined. Figure 2 shows the effect of chiral selector concentrations on the carvedilol enantiomers separation.

Bottom Line: Carvedilol is administered as a racemic mixture of the R(+)- and S(-)-enantiomers, although it was demonstrated that the two enantiomers exhibit different pharmacological effects and stereoselective pharmacokinetics.The aim of this study was the evaluation of several native and derivatized cyclodextrines as chiral selectors for the separation of carvedilol enantiomers.The effects of CD concentration, pH value and composition of the background electrolyte, capillary temperature, running voltage and injection parameters have been investigated.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Târgu Mureş, Romania.

ABSTRACT
Carvedilol is administered as a racemic mixture of the R(+)- and S(-)-enantiomers, although it was demonstrated that the two enantiomers exhibit different pharmacological effects and stereoselective pharmacokinetics. The aim of this study was the evaluation of several native and derivatized cyclodextrines as chiral selectors for the separation of carvedilol enantiomers. Stereoselective interactions were observed with four cyclodextrines (β-CD, hydroxypropyl-β-CD, randomly methylated β-CD and sulfobuthyl ether- β-CD). The effects of CD concentration, pH value and composition of the background electrolyte, capillary temperature, running voltage and injection parameters have been investigated. The method was validated for precision of peak-area response, linearity range and limits of detection and quantification. An efficient stereoselective capillary zone electrophoretic method was developed for the determination of carvedilol enantiomers using a simple 25 mM phosphate buffer at a pH = 2.5 and 10 mM β-CD as chiral selector, resulting in baseline separation of the two enantiomers with sharp peaks and relatively short analysis time. Highly satisfactory results were obtained from the analysis of carvedilol from tablets, indicating that the method is suitable for routine analysis of carvedilol in pharmaceutical products.

No MeSH data available.


Related in: MedlinePlus