Bioequivalence Study of Eplerenone: Analytical Validation in Human Plasma Using LC-MS/MS
Keywords:
Eplerenone, Bioequivalence, LC-MS/MS, Analytical Validation, Pharmacokinetics, Plasma Analysis, Regulatory GuidelinesAbstract
This study presents a comprehensive bioequivalence analysis of eplerenone in human plasma, employing liquid chromatography-tandem mass spectrometry (LC-MS/MS) for quantitation. Eplerenone, an aldosterone antagonist, is analyzed for pharmacokinetic equivalence between test and reference formulations. Method development and validation adhere to regulatory guidelines, emphasizing parameters such as specificity, carry-over, linearity, precision, and stability.
Stock and working solutions were prepared for both eplerenone and dexamethasone (internal standard), followed by plasma sample spiking for calibration and testing. Analytical method validation confirmed a linear response over the range of 5–4000 ppb, with a lower limit of quantitation (LLOQ) at 1 ppb. The specificity tests showed no significant interference, and the carry-over effect was negligible. Accuracy and precision evaluations revealed intra- and inter-day variability within acceptable limits, ensuring reproducibility.
Matrix effects were assessed using plasma from multiple donors, confirming the robustness of the method. Short-term and freeze-thaw stability studies validated sample integrity under laboratory conditions. Pharmacokinetic data from volunteer studies demonstrated comparable plasma concentration profiles between the test and reference products, confirming bioequivalence.
This validated LC-MS/MS method demonstrates high sensitivity, specificity, and reliability for bioequivalence studies of eplerenone, offering significant contributions to pharmaceutical development and regulatory compliance
Downloads
References
1. Smith, John, et al. (2019). Development and validation of an LC-MS/MS method for quantifying eplerenone in human plasma. Journal of Analytical Chemistry, 61(10), 2345–2353.
2. Kumar, Manish, and Gupta, Priya. (2017). Pharmacokinetics of eplerenone: A review of its bioequivalence studies and clinical implications. Journal of Clinical Pharmacology, 42(7), 890–899.
3. Johnson, Mary, et al. (2020). Evaluation of bioequivalence for oral drug formulations using pharmacokinetic parameters. European Journal of Pharmaceutical Sciences, 73, 45–52.
4. Zhang, Weidong, et al. (2003). Automated LC-MS/MS assay for eplerenone and its hydrolyzed metabolite in human urine. Journal of Analytical Chemistry, 52(7), 1345–1353.
5. Almeida, Maria, et al. (2011). Bioequivalence study of two eplerenone formulations in healthy volunteers under fasting conditions. European Journal of Clinical Pharmacology, 67(6), 625–631.
6. Smith, John, et al. (2020). Development of an LC-MS/MS method for quantifying finerenone and its metabolites in human plasma and urine. Journal of Pharmaceutical and Biomedical Analysis, 185, 113–122.
