Validation and Greenness assessment of UPLC Method for bioanalysis of Bilastine in mice PK study
Keywords:Bilastine, Solid Phase Extraction, UPLC, Validation, Antihistamine, Pharmacokinetics
Bilastine, is a second-generation antihistamine drug which is used in the treatment of allergic rhinoconjunctivitis and urticaria. It exerts its effect as a selective histamine H1 receptor antagonist. In this study, an ultra-high-performance liquid chromatography (UPLC) method was developed to measure the concentrations of Bilastine in mouse blood, and the method was applied in measuring the pharmacokinetics of the analyte after oral and intravenous administration. The analyte was extracted by solid phase extraction method. A UPLC BEH C18 column (2.1 mm × 100 mm, 1.8 ?m particle size) was used for chromatographic separation by gradient elution using acetonitrile-water (0.1% formic acid) as the mobile phase at a flow rate of 0.4 mL/min. Bilastine was administered to the mice orally at 2 mg/kg and intravenously at 0.05 mg/kg. Blood was collected at various time intervals, and the blood samples were processed after collection and analyzed by UPLC. The intra-day and inter-day accuracy of Bilastine were 91%-103% and 85%-107%, respectively, and the precision (RSD, %) was less than 15% for both intra-day and inter-day measurements. The matrix effect ranged from 95% to 108%, and the recovery was higher than 70%. The half-life of bilastine in plasma was found to be 7.02 ± 5.21h. Bilastine has a good linear relationship in the range of 10-500 ng/mL, and the lower limit of quantification was 10 ng/mL. The precision, accuracy, extraction recovery, matrix effect, and stability meet the requirements of the guiding principles. A robust and reliable UPLC method was fully optimized and developed to detect the blood concentration of bilastine in mice and the samples were analyzed by Empower software.
Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A (2005). "Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: Receptor selectivity and in vitro antihistaminic activity". Drugs in R&D 6 (6): 371–84.
Bachert, C.; Kuna, P.; Zuberbier, T. (1 June 2010). "Bilastine in allergic rhinoconjunctivitis and urticaria". Allergy. 65: 1–13 .
Jáuregui I, Bartra J, del Cuvillo A, Dávila I, Ferrer M, Montoro J, Mullol J, Sastre J, Valero A (2011). "Bilastine and quality of life". Journal of Investigational Allergology and Clinical Immunology. 21 Suppl 3: 16–23.
Jáuregui I, Ramaekers JG, Yanai K, Farré M, Redondo E, Valiente R, Labeaga L. Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving. Expert Opin Drug Saf. 2016 Jan;15(1):89-98.
Silva ATD, Brabo GR, Marques ID, Bajerski L, Malesuik MD and Paim CS: UV Spectrophotometric method for quantitative determination of Bilastine using experimental design for robustness Drug Anal Res 2017; 01(2): 38-43.
Motta, P. R., dos Santos Porto, D., Martini, P. R. R., Bajerski, L., Azeredo, J. B., Paula, F. R., & Paim, C. S. (2020). Bilastine: Quantitative determination by LC with fluorescence detection and structural elucidation of the degradation products using HRMS. Journal of AOAC International, 103(6), 1451–1460.
Ouarezki, R., Guermouche, S., & Guermouche, M.-H. (2020). Degradation kinetics of Bilastine determined by RP-HPLC method and identification of its degradation product in oxidative condition. Chemical Papers, 74(4), 1133–1142.
Pardeshi, P., Gaware, V., & Dhamak, K. (2020). Development and Validation of RP-HPLC Method for the Estimation of Bilastine from bulk and Formulation. Asian Journal of Pharmaceutical Analysis, 10(2).
Khushbu K. Patel, Arati M. Patel, C. N. Patel. A new simple RP-HPLC Method development, Validation and Forced degradation studies of Bilastine. Asian Journal of Pharmaceutical Analysis. 2021; 11(3):183-7.
Katta R, Murty NNVVSSN, Ramasrinivas and Rao GN: Stability indicating method development and validation for the determination of bilastine and its impurities by UPLC method. Int J Pharm Sci & Res 2020; 11(3): 1312-21. doi: 10.13040/IJPSR.0975-8232.11(3).1312-21.
Terzic J, Popovic I, Stajic A, Tumpa A and Jancic-Stojanovic B: Application of analytical quality by design concept for bilastine and its degradation impurities determination by hydrophilic interaction liquid chromato-graphic method. J Pharm Biomed Anal 2016; 125: 385-93.
Zuberbier T, Oanta A, Bogacka E, Medina I, Wesel F and Uhl P: Comparison of the efficacy and safety of Bilastine 20 mg vs. levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-center, double-blind, randomized, placebo-controlled study. Allergy 2010; 65(4): 516-28.
Berrueta LA, Fernandez-Armentia M, Bakkali A, Gonzalo A, Lucero ML and Orjales A: Matrix solid-phase dispersion technique for the determination of a new antiallergic drug, Bilastine, in rat faeces. J Chromatogr B 2001; 760: 185-90.
Lasseter KC, Sologuren A, La Noce A and Dilzer SC: Evaluation of the single-dose pharmacokinetics of Bilastine in subjects with various degrees of renal insufficiency. Clin Drug Investi 2013; 33: 665-73.
Food and Drug Administration. Guidance for Industry: Bioanalytical Method Validation Center for Drug Evaluation and Research. Silver Springs, MD: FDA; 2001.
ICH guideline M10 on bioanalytical method validation and study sample analysis EMA/CHMP/ICH/172948/2019.
Pereira, P. F.; Wojnowski, W.; Tobiszewski, M. AGREE - Analytical GREEnness Metric Approach and Software. Anal Chem. 2020, 92(14):10076–82.
Ga?uszka, A.; Migaszewski, Z. M.; Konieczka, P.; Namie?nik, J. Analytical Eco-Scale for assessing the greenness of analytical procedures. TrAC - Trends Anal Chem. 2012;37(July):61–72.
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