PHARMACOKINETIC INVESTIGATION OF REMOGLIFLOZIN IN RAT PLASMA SAMPLES BY HIGH-THROUGHPUT HPLC-MS-MS
DOI:
https://doi.org/10.22159/ijap.2022v14i6.45700Keywords:
Bio-analytical, Empagliflozin, HPLC-MS-MS, Internal standard, Remogliflozin, Wistar male ratAbstract
Objective: Remogliflozin (REMO), a selective inhibitor of the renal sodium-dependent glucose transporter 2 channel, which could increase urine glucose excretion and lower plasma glucose in humans. To establish a simple, sensitive and completely validated HPLC-MS-MS approach for the analysis of Remogliflozin in rat plasma samples.
Methods: The method was developed after simple step protein precipitation by acetonitrile and Empagliflozin (EMPA) was used as internal standard. Separation was done on an CORTECS C18, 90 Å, 2.7 µm, 4.6 mm X 150 mm with an isocratic mobile phase consisting of 0.1% Formic acid: acetonitrile (20:80%, v/v) and pumped at a flow stream of 0.8 ml/min at ambient temperature.
Results: The approach developed showed fine calibration curve in the quantity range of 5-1000 pg/ml with correlation coefficient (r2) of ≥ 0.9997 and the intra-run accuracy and precision was 99.91 to 109.07% and 0.17 to 1.34, inter-run accuracy and precision was 99.8 to 101.54 and 0.17 to 1.66 according to FDA guidelines.
Conclusion: The newly designed and validated approach was simple, fast and applied effectively for single-dose oral pharmacokinetic investigation in Wistar male rats for the quantification of REMO in biological matrix.
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References
Garcia Ropero A, Badimon JJ, Santos Gallego CG. The pharmacokinetics and pharmacodynamics of SGLT2 inhibitors for type 2 diabetes mellitus: the latest developments. Expert Opin Drug Metab Toxicol. 2018;14(12):1287-302. doi: 10.1080/17425255.2018.1551877, PMID 30463454.
Neal B, Perkovic V, Mahaffey KW, de Zeeuw D, Fulcher G, Erondu N. Canagliflozin and cardiovascular and renal events in type 2 diabetes. N Engl J Med. 2017;377(7):644-57. doi: 10.1056/NEJMoa1611925, PMID 28605608.
Tang H, Cui W, Li D, Wang T, Zhang J, Zhai S. Sodium-glucose co-transporter 2 inhibitors in addition to insulin therapy for management of type 2 diabetes mellitus: A meta-analysis of randomized controlled trials. Diabetes Obes Metab. 2017;19(1):142-7. doi: 10.1111/dom.12785, PMID 27598833.
Wiviott SD, Raz I, Bonaca MP, Mosenzon O, Kato ET, Cahn A. Dapagliflozin and cardiovascular outcomes in type 2 diabetes. N Engl J Med. 2019;380(4):347-57. doi: 10.1056/NEJMoa1812389, PMID 30415602.
Zinman B, Wanner C, Lachin JM, Fitchett D, Bluhmki E, Hantel S. Empagliflozin, cardiovascular outcomes, and mortality in type 2 diabetes. N Engl J Med. 2015;373(22):2117-28. doi: 10.1056/NEJMoa1504720, PMID 26378978.
Zelniker TA, Wiviott SD, Raz I, Im K, Goodrich EL, Bonaca MP. SGLT2 inhibitors for primary and secondary prevention of cardiovascular and renal outcomes in type 2 diabetes: a systematic review and meta-analysis of cardiovascular outcome trials. Lancet. 2019;393(10166):31-9. doi: 10.1016/S0140-6736(18)32590-X, PMID 30424892.
Santos Gallego CG, Garcia Ropero A, Mancini D, Pinney SP, Contreras JP, Fergus I. Rationale and design of the EMPA-TROPISM trial (ATRU-4): are the ”cardiac benefits” of empagliflozin independent of its hypoglycemic activity? Cardiovasc Drugs Ther. 2019;33(1):87-95. doi: 10.1007/s10557-018-06850-0, PMID 30675708.
Santos Gallego CG, Requena Ibanez JA, San Antonio R, Ishikawa K, Watanabe S, Picatoste B, Flores E, Garcia Ropero A, Sanz J, Hajjar RJ, Fuster V, Badimon JJ. Empagliflozin ameliorates adverse left ventricular remodeling in nondiabetic heart failure by enhancing myocardial energetics. J Am Coll Cardiol. 2019;73(15):1931-44. doi: 10.1016/j.jacc.2019.01.056, PMID: 30999996.
Flores E, Santos Gallego CG, Diaz Mejia N, Badimon JJ. Do the SGLT-2 inhibitors offer more than hypoglycemic activity? Cardiovasc Drugs Ther. 2018;32(2):213-22. doi: 10.1007/s10557-018-6786-x, PMID 29679303.
Mikhail N. Remogliflozin etabonate: a novel SGLT2 inhibitor for treatment of diabetes mellitus. Expert Opin Investig Drugs. 2015;24(10):1381-7. doi: 10.1517/13543784.2015.1061501, PMID 26288025.
Tammisetty MR, Challa BR, Puttagunta SB. A novel analytical method for the simultaneous estimation of remogliflozin and metformin hydrochloride by UPLC/PDA in bulk and formulation application to the estimation of product traces. Turk J Pharm Sci. 2021;18(3):296-305. doi: 10.4274/tjps.galenos.2020.39699. PMID 34157819.
Attimarad M, Elgorashe REE, Subramaniam R, Islam MM, Venugopala KN, Nagaraja S. Development and validation of rapid RP-HPLC and green second-derivative UV spectroscopic methods for simultaneous quantification of metformin and remogliflozin in formulation using experimental design. Separations. 2020;7(4):59. doi: 10.3390/separations7040059.
Attimarad M, Nair AB, Nagaraja S, Aldhubiab BE, Venugopala KN, Pottathil S. Smart UV derivative spectrophotometric methods for simultaneous determination of metformin and remogliflozin: development, validation and application to the formulation. Indian J Pharm Educ Res. 2021;55(1s):s293-302. doi: 10.5530/ijper.55.1s.62.
Attimarad M, Nair AB, Sreeharsha N, Al-Dhubiab BE, Venugopala KN, Shinu P. Development and validation of green UV derivative spectrophotometric methods for simultaneous determination metformin and remogliflozin from formulation: evaluation of greenness. Int J Environ Res Public Health. 2021;18(2):448. doi: 10.3390/ijerph18020448, PMID 33429964.
Vidhi D, Patel P. Method development and validation of UV spectrophotometric estimation of remogliflozin etabonate in bulk and its tablet dosage form. Res J Pharm Technol. 2021;14(4):2042-4. doi: 10.52711/0974-360X.2021.00362.
Shah DA, Gondalia II, Patel VB, Mahajan A, Chhalotiya UK. Stability indicating liquid chromatographic method for the estimation of remogliflozin etabonate. J Chem Metrol. 2020;14(2):125-32. doi: 10.25135/jcm.46.20.07.1734.
Shah DA, Gondalia II, Patel VB, Mahajan A, Chhalotiya U, Nagda DC. Stability indicating thin-layer chromatographic method for estimation of antidiabetic drug Remogliflozin etabonate. Futur J Pharm Sci. 2021;7(1):83. doi: 10.1186/s43094-021-00230-6.
Venkata Sakuntala MS, Lakshmana Rao A, Carey MW. Simultaneous estimation of ivacaftor and tezacaftor in rat plasma by liquid chromatography coupled with tandem-mass-spectrometry: application to pharmacokinetic studies. Thai J Pharm Sci. 2021;45(6):451-60.
U.S. Food and Drug Administration guidance for industry: bioanalytical method validation 2018. U.S. Department of Health and Human Services, Food and Drug Administration; 2018.
U.S. Food and Drug Administration guidance for industry: bioavailability and bioequivalence studies for orally administered drug products-general considerations 2002. U.S. Department of Health and Human Services, Food and Drug Administration; 2002.
U.S. Food and Drug Administration guidance for industry: food-effect bioavailability and fed bio equivalence studies 2002. U.S. Department of Health and Human Services, Food and Drug Administration; 2002.
Inturi S, Avula PR. A sensitive bioanalytical method development and validation of cabozantinib in human plasma by LC-ESI-MS/MS. Braz J Pharm Sci. 2018;54(2):e17163. doi: 10.1590/s2175-97902018000217163.
Ponnuru VS, Challa BR, Nadendla R. Quantification of desloratadine in human plasma by LC-ESI-MS/MS and application to a pharmacokinetic study. J Pharm Anal. 2012;2(3):180-7. doi: 10.1016/j.jpha.2012.01.008. PMID 29403740.
Harahap Y, Maysyarah I. Analytical validation of clopidogrel in human plasma through ultrahighperformance liquid chromatography-tandem mass spectrometry. Int J App Pharm 2017;9(1):79-86. doi: 10.22159/ijap.2017.v9s1.79_86.
IS, A PR. Development and validation of liquid chromatography coupled with tandem mass spectrometry method for estimation of lenvatinib in human plasma. Asian J Pharm Clin Res 2017;10(7):182-7. doi: 10.22159/ajpcr.2017.v10i7.18287.
Agbokponto JE, Yemoa LA, Assanhou AG, Liu R, Ganfon H, Ding L. Liquid chromatography tandem mass spectrometry determination method of bencycloquidium bromide: application to drug interaction study in Human. Int J Pharm Pharm Sci. 2021;13(10):43-6. doi: 10.22159/ijpps.2021v13i10.5791.
Halder D, Das S, Ghosh B, Biswas E, Roy S, Bose A. An LC-MS/MS based Bioanalytical approach to resolve pharmacokinetic investigation of acotiamide hydrochloride and its application to bioequivalence study. Int J Pharm Pharm Sci. 2020;12(10):76-84. doi: 10.22159/ Ijpps.2020v12i10.38410.
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