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A chiral LC–MS/MS method for the stereospecific determination of efonidipine in human plasma.
- Source :
-
Journal of Pharmaceutical & Biomedical Analysis . Apr2016, Vol. 122, p35-41. 7p. - Publication Year :
- 2016
-
Abstract
- Efonidipine hydrochloride is a new generation dihydropyridine Ca 2+ channel blocker designed to inhibit both T-type and L-type Ca 2+ channels. Efonidipine possesses a chiral carbon and is clinically administered as a racemate. In the present study, an enantioselective and sensitive LC–MS/MS method of determining efonidipine enantiomers in human plasma was developed and validated to characterize the stereoselective pharmacokinetics. Plasma samples were processed by liquid-liquid extraction (LLE). Chiral separation was optimized on a CHIRALPAK ® ID column using an isocratic mobile phase of acetonitrile/water (60:40, v/v). Detection was using MS in multiple reaction monitoring (MRM) mode, using the transitions of m/z 632.3 → 91.1 for efonidipine enantiomers, and m/z 493.3 → 117.2 for cilnidipine (internal standard). The calibration curves were linear over 0.100–20.0 ng/mL for each enantiomer. The lower limit of quantification (LLOQ) for each enantiomer was established at 0.100 ng/mL. Intra- and inter-day precisions were less than 12.1% for each enantiomer in terms of relative standard deviation (RSD), and accuracies were between −5.0% and 5.0% in terms of relative error (RE) for each enantiomer. No chiral inversion was observed during sample storage, preparation procedure and analysis. The validated method was successfully applied to a stereoselective pharmacokinetic study of efonidipine in healthy subjects after oral administration of 40 mg (20 mg × 2) efonidipine hydrochloride tablets. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 07317085
- Volume :
- 122
- Database :
- Academic Search Index
- Journal :
- Journal of Pharmaceutical & Biomedical Analysis
- Publication Type :
- Academic Journal
- Accession number :
- 113188321
- Full Text :
- https://doi.org/10.1016/j.jpba.2016.01.039