A capillary electrophoresis method using cyclodextrins as the chiral selectors was developed for the determination of carvedilol enantiomers in serum. Several types of cyclodextrins were evaluated. The effect of cyclodextrin concentration on enantiomer resolution was investigated. Best results were obtained using 10 mM hydroxypropyl-beta-cyclodextrin in the run buffer. The effect of voltage on efficiency was assessed. Other electrophoretic conditions were optimized. The method was validated for carvedilol enantiomers in serum. Linearity of detection was assessed over the concentration range of 50-4000 ng/ml of each enantiomer in serum. Intra- and inter-assay variability obtained were under 8% for both enantiomers.
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http://dx.doi.org/10.1016/s0731-7085(00)00468-4 | DOI Listing |
Br J Clin Pharmacol
September 2024
Center for Pharmacometrics and Systems Pharmacology, College of Pharmacy, University of Florida, Orlando, FL, USA.
Aims: A population-based pharmacokinetic (PK) modeling approach (PopPK) was used to investigate the impact of Roux-en-Y gastric bypass (RYGB) on the PK of (R)- and (S)-carvedilol. We aimed to optimize carvedilol dosing for these patients utilizing a pharmacokinetic/pharmacodynamic (PK/PD) link model.
Methods: PopPK models were developed utilizing data from 52 subjects, including nonobese, obese, and post- RYGB patients who received rac- carvedilol orally.
Circulation
November 2023
From the Departments of Medicine (K.S., Y.Y., A.K., M.K., S.Y., Y.H., Q.W., M.V.P., M.T.W., V.N.P., E.A.A.), Stanford University School of Medicine, CA.
J Pharmacol Exp Ther
January 2024
Department of Biotechnology and Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, Pomona, California
The chemical warfare agent sulfur mustard and its structural analog nitrogen mustard (NM) cause severe vesicating skin injuries. The pathologic mechanisms for the skin injury following mustard exposure are poorly understood; therefore, no effective countermeasure is available. Previous reports demonstrated the protective activity of carvedilol, a US Food and Drug Administration (FDA)-approved -blocker, against UV radiation-induced skin damage.
View Article and Find Full Text PDFChirality
October 2023
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, "Iuliu Hațieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania.
Carvedilol, a highly protein-bound beta-blocker, is used in therapy as a racemic mixture of its two enantiomers that exhibit different pharmacological activity. The aim of this study was to evaluate the stereoselective nature of its binding to the two major plasma proteins: albumin and alpha-1-acid glycoprotein. The determination of the plasma protein-binding degree for carvedilol and its enantiomers was achieved using ultrafiltration for the separation of the free fraction, followed by LC-MS/MS quantification, using two different developed and validated methods in terms of stationary phase: achiral C18 type and chiral ovomucoid type.
View Article and Find Full Text PDFBMC Chem
March 2023
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo, 11562, Egypt.
Enantioseparation of five β-adrenergic blockers was studied using two mobile phases on a cellulose tris(3-chloro-4-methylphenylcarbamate) (Lux-Cellulose-2) chiral column in normal phase mode. The first mobile phase composed of n-hexane: ethanol: diethylamine 60: 40: 0.1 by volume has successfully resolved the chromatographic peaks of three pairs of β-adrenergic blockers namely, bisoprolol, carvedilol and atenolol.
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