Enantioselective liquid chromatographic-electrospray mass spectrometric assay of β-adrenergic blockers: application to a pharmacokinetic study of sotalol in human plasma

• Published in: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences Vol. 796; no. 1; pp. 45 - 54
• Main Authors: Badaloni, Elena, D’Acquarica, Ilaria, Gasparrini, Francesco, Lalli, Silvana, Misiti, Domenico, Pazzucconi, Franco, Sirtori, Cesare R
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 25.10.2003; Elsevier Science
• Subjects: Adrenergic beta-Antagonists - blood; Adrenergic beta-Antagonists - pharmacokinetics; Analysis; Biological and medical sciences; Chromatography, High Pressure Liquid - methods; Enantiomer separation; General pharmacology; Humans; Medical sciences; Pharmacokinetics; Pharmacology. Drug treatments; Reference Values; Reproducibility of Results; Sensitivity and Specificity; Sotalol; Sotalol - blood; Sotalol - pharmacokinetics; Spectrometry, Mass, Electrospray Ionization - methods; Stereoisomerism; β-Adrenergic blockers; Pharmacokinetics; β-Adrenergic blockers; Enantiomer separation; Sotalol; Human; Drug; Biological fluid; HPLC chromatography; Liquid chromatography; Electrospray; Teicoplanin; Blood plasma; β-Adrenergic receptor; Glycopeptide; Enantiomer; Antagonist; Mass spectrometry; Quantitative analysis; Beta blocking agent
• ISSN: 1570-0232; 1873-376X
• DOI: 10.1016/j.jchromb.2003.07.001

An enantioselective high performance liquid chromatographic-electrospray ionization mass spectrometric (HPLC-ESI-MS) method for the direct determination of several β-adrenergic blockers was developed and validated. The method is based on the direct separation of the enantiomers of drugs on a laboratory-made chiral stationary phase (CSP) containing covalently bonded teicoplanin (TE) as chiral selector. Detection of the effluent was performed by electrospray ionization mass spectrometry, run in the selected-ion recording (SIR) mode. The method was applied to the pharmacokinetic monitoring of sotalol (STL) in the plasma of five young healthy volunteers, dosed with racemic drug. The limits of quantitation (LOQ) reached 4 ng/ml for both sotalol enantiomers. Such a method, fully validated, offers a novel, fast and very efficient tool for the direct determination of sotalol enantiomers in human plasma, and can be generally applied to the β-adrenergic blockers stereoselective pharmacokinetics.