Analysis of carvedilol enantiomers in human plasma using chiral stationary phase column and liquid chromatography with tandem mass spectrometry |
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Authors: | Poggi Josiane Cristófani Da Silva Flávia Garcez Coelho Eduardo Barbosa Marques Maria Paula Bertucci Carlo Lanchote Vera Lucia |
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Affiliation: | 1. Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeir?o Preto, Universidade de S?o Paulo, Ribeir?o Preto, SP, Brazil;2. Departamento de Clínica Médica, Faculdade de Medicina de Ribeir?o Preto, Universidade de S?o Paulo, Ribeir?o Preto, SP, Brazil;3. Dipartimento di Scienze Farmaceutiche, University of Bologna, Bologna, Italy |
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Abstract: | Carvedilol is an antihypertensive drug available as a racemic mixture. (?)‐(S)‐carvedilol is responsible for the nonselective β‐blocker activity but both enantiomers present similar activity on α1‐adrenergic receptor. To our knowledge, this is the first study of carvedilol enantiomers in human plasma using a chiral stationary phase column and liquid chromatography with tandem mass spectrometry. The method involves plasma extraction with diisopropyl ether using metoprolol as internal standard and direct separation of the carvedilol enantiomers on a Chirobiotic T® (Teicoplanin) column. Protonated ions [M + H]+ and their respective ion products were monitored at transitions of 407 > 100 for the carvedilol enantiomers and 268 > 116 for the internal standard. The quantification limit was 0.2 ng ml?1 for both enantiomers in plasma. The method was applied to study enantioselectivity in the pharmacokinetics of carvedilol administered as a single dose of 25 mg to a hypertensive patient. The results showed a higher plasma concentration of (+)‐(R)‐carvedilol (AUC0–∞ 205.52 vs. 82.61 (ng h) ml?1), with an enantiomer ratio of 2.48. Chirality, 2012. © 2012 Wiley Periodicals, Inc. |
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Keywords: | carvedilol pharmacokinetics enantiomers LC‐MS/MS chiral stationary phase |
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