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Current Analytical Chemistry

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ISSN (Print): 1573-4110
ISSN (Online): 1875-6727

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Research Article

New Analytical Method for Simultaneous Analysis of Losartan and E-3174 by HPLC in Human Plasma: Application in Pharmaceutical Science

Author(s): Edgar Alejandro de Leon-Diaz de Leon, Antonio Gordillo-Moscoso*, Úrsula Medina, Ángel Antonio Vertiz Hernández, Rafael Almendra-Pegueros and Juan M. López Quijano

Volume 16, Issue 8, 2020

Page: [979 - 987] Pages: 9

DOI: 10.2174/1573411015666191209111221

Price: $65

Abstract

Background: Losartan, one of the most frequently used drugs in Heart Failure (HF) treatment, could be modified for its bioavailability (BA) by generic formulations and other factors. Hence, the importance of therapeutic drug monitoring.

Objective: Development and validation of a simplified analytical method using HPLC for simultaneous quantification of losartan and E-3174 in human plasma samples. The method was tested for determining the pharmacokinetics parameters of HF patients.

Methods: Analytical conditions were optimized using a C18 column (4.6 X 50 mm, 3 μm. Thermo Scientific) at 25ºC. Conditions of mobile phase: a phosphate buffer (0.01M), adjusted to pH 2.5 with phosphoric acid (1M) and Acetonitrile (60:40 v/v). The flow rate was maintained at 1.2 mL/min, on a running time of 5 min and a sample injection volume of 50 μL. Absorbance for measurement of losartan and E-3174 was 200 nm. Pharmacokinetics profiles were determined with Phoenix Win- Nonlin 8.1 software in a non-compartmental model.

Results: Analytical method developed and validated in this work is precise and accurate for simultaneous determination of losartan and E-3174 in human plasma samples in a range of 0.02 -10 μg/mL. In HF subjects, lower Tmax and higher Cmax for losartan and E-3174 patent than generic formulation were observed, which can be translated into less biological effect and more time to present it by the generic drug.

Conclusion: The pharmacokinetic profile is dependent on the type of formulation studied (generic/ patent) hence the importance of conducting evaluations in our patients to ensure that the expected therapeutic effect is achieved with treatment administered.

Keywords: E-3174, heart failure, losartan, method validation, pharmacokinetic, UV/VIS HPLC.

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[1]
Kannel, W.B.; Belanger, A.J. Epidemiology of heart failure. Am. Heart J., 1991, 121(3 Pt 1), 951-957.
[http://dx.doi.org/10.1016/0002-8703(91)90225-7] [PMID: 2000773]
[2]
Parmley, W.W. Pathophysiology of congestive heart failure. Am. J. Cardiol., 1985, 55(2), 9A-14A.
[http://dx.doi.org/10.1016/0002-9149(85)90790-8] [PMID: 3966410]
[3]
Kim, D.H.; Chien, F.J.; Eisen, H.J. Pharmacologic Management for heart failure and emerging therapies. Curr. Cardiol. Rep., 2017, 19(10), 94.
[http://dx.doi.org/10.1007/s11886-017-0899-x] [PMID: 28840572]
[4]
MacIntyre, K.; Capewell, S.; Stewart, S.; Chalmers, J.W.T.; Boyd, J.; Finlayson, A.; Redpath, A.; Pell, J.P.; McMurray, J.J. Evidence of improving prognosis in heart failure: Trends in case fatality in 66 547 patients hospitalized between 1986 and 1995. Circulation, 2000, 102(10), 1126-1131.
[http://dx.doi.org/10.1161/01.CIR.102.10.1126] [PMID: 10973841]
[5]
Mosterd, A.; Hoes, A.W. Clinical epidemiology of heart failure. Heart, 2007, 93(9), 1137-1146.
[http://dx.doi.org/10.1136/hrt.2003.025270] [PMID: 17699180]
[6]
Bredy, C.; Ministeri, M.; Kempny, A.; Alonso-Gonzalez, R.; Swan, L.; Uebing, A.; Diller, G.P.; Gatzoulis, M.A.; Dimopoulos, K. New York Heart Association (NYHA) classification in adults with congenital heart disease: relation to objective measures of exercise and outcome. Eur. Heart J. Qual. Care Clin. Outcomes, 2018, 4(1), 51-58.
[http://dx.doi.org/10.1093/ehjqcco/qcx031] [PMID: 28950356]
[7]
Miller-Davis, C.; Marden, S.; Leidy, N.K. The New York Heart Association Classes and functional status: What are we really measuring? Heart Lung, 2006, 35(4), 217-224.
[http://dx.doi.org/10.1016/j.hrtlng.2006.01.003] [PMID: 16863893]
[8]
Naveiro-Rilo, J.C.; Diez-Juárez, D.; Flores-Zurutuza, M.L.; Molina Mazo, R.; Alberte Pérez, C.; Arias Cobos, V. The appropriate use of pharmacological treatment in patients with chronic heart failure. A perspective from Primary Care. Semergen, 2013, 39(4), 183-190.
[http://dx.doi.org/10.1016/j.semerg.2012.08.006] [PMID: 23726729]
[9]
Dávila, D.F.; Núñez, T.J.; Odreman, R.; de Dávila, C.A. Mechanisms of neurohormonal activation in chronic congestive heart failure: pathophysiology and therapeutic implications. Int. J. Cardiol., 2005, 101(3), 343-346.
[http://dx.doi.org/10.1016/j.ijcard.2004.08.023] [PMID: 15907399]
[10]
Sica, D.A.; Gehr, T.W.; Ghosh, S. Clinical pharmacokinetics of losartan. Clin. Pharmacokinet., 2005, 44(8), 797-814.
[http://dx.doi.org/10.2165/00003088-200544080-00003] [PMID: 16029066]
[11]
Weber, M.A.; Byyny, R.L.; Pratt, J.H.; Faison, E.P.; Snavely, D.B.; Goldberg, A.I.; Nelson, E.B. Blood pressure effects of the angiotensin II receptor blocker, losartan. Arch. Intern. Med., 1995, 155(4), 405-411.
[http://dx.doi.org/10.1001/archinte.1995.00430040081010] [PMID: 7848024]
[12]
Stearns, R.A.; Chakravarty, P.K.; Chen, R.; Chiu, S.H. Biotransformation of losartan to its active carboxylic acid metabolite in human liver microsomes. Role of cytochrome P4502C and 3A subfamily members. Drug Metab. Dispos., 1995, 23(2), 207-215.
[PMID: 7736913]
[13]
Krieter, P.A.; Colletti, A.E.; Miller, R.R.; Stearns, R.A. Absorption and glucuronidation of the angiotensin II receptor antagonist losartan by the rat intestine. J. Pharmacol. Exp. Ther., 1995, 273(2), 816-822.
[PMID: 7752085]
[14]
Simpson, K.L.; McClellan, K.J. Losartan: a review of its use, with special focus on elderly patients. Drugs Aging, 2000, 16(3), 227-250.
[http://dx.doi.org/10.2165/00002512-200016030-00006] [PMID: 10803861]
[15]
Goldberg, L.R.; Jessup, M.; Stage, B. Stage B heart failure: Management of asymptomatic left ventricular systolic dysfunction. Circulation, 2006, 113(24), 2851-2860.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.105.600437] [PMID: 16785351]
[16]
Farthing, D.; Sica, D.; Fakhry, I.; Pedro, A.; Gehr, T.W. Simple high-performance liquid chromatographic method for determination of losartan and E-3174 metabolite in human plasma, urine and dialysate. J. Chromatogr. B Biomed. Sci. Appl., 1997, 704(1-2), 374-378.
[http://dx.doi.org/10.1016/S0378-4347(97)00489-1] [PMID: 9518174]
[17]
Jalalizadeh, H.; Souri, E.; Farsam, H.; Ansari, M. A high-performance liquid chromatographic assay for the determination of losartan in plasma. IJPT, 2003, 2(1), 18-21.
[18]
del Rosario Brunetto, M.; Contreras, Y.; Clavijo, S.; Torres, D.; Delgado, Y.; Ovalles, F.; Ayala, C.; Gallignani, M.; Estela, J.M.; Martin, V.C. Determination of losartan, telmisartan, and valsartan by direct injection of human urine into a column-switching liquid chromatographic system with fluorescence detection. J. Pharm. Biomed. Anal., 2009, 50(2), 194-199.
[http://dx.doi.org/10.1016/j.jpba.2009.04.015] [PMID: 19446420]
[19]
Bienert, A.; Brzezińiski, R.; Szałek, E.; Dubai, V.; Grześkowiak, E.; Dyderski, S.; Drobnik, L.; Wolc, A.; Olejniczak-Rabinek, M. Bioequivalence study of two losartan formulations administered orally in healthy male volunteers. Arzneimittelforschung, 2006, 56(11), 723-728.
[PMID: 17220048]
[20]
Singh, J. International conference on harmonization of technical requirements for registration of pharmaceuticals for human use. J. Pharmacol. Pharmacother., 2015, 6(3), 185-187.
[http://dx.doi.org/10.4103/0976-500X.162004] [PMID: 26312010]
[21]
Q2 (R1) validation of analytical procedure, test and methodology Proceedings of the International Conference on Harmonization, Geneva, Switzerland , 2005.
[22]
Furtek, C.I.; Lo, M.W. Simultaneous determination of a novel angiotensin II receptor blocking agent, losartan, and its metabolite in human plasma and urine by high-performance liquid chromatography. J. Chromatogr. A, 1992, 573(2), 295-301.
[http://dx.doi.org/10.1016/0378-4347(92)80132-A] [PMID: 1601963]
[23]
Shokraneh, F.; Dabirsiaghi, A.; Adib, N. A new HPLC method for determination of Losartan in Human Plasma and its aplication in bioequivalence studies. Orient. J. Chem., 2012, 28(1), 237-241.
[http://dx.doi.org/10.13005/ojc/280128]
[24]
Dos pasos Maio, V.M.; Dias, C.L.; Bergold, A.M. Validation of an Isocratic HPLC Assay of losartan potassium in pharmaceutical formulations and stress test for stability evaluation of drug substance. Lat. Am. J. Pharm., 2005, 24(2), 250-255.
[25]
Ohtawa, M.; Takayama, F.; Saitoh, K.; Yoshinaga, T.; Nakashima, M. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br. J. Clin. Pharmacol., 1993, 35(3), 290-297.
[http://dx.doi.org/10.1111/j.1365-2125.1993.tb05696.x] [PMID: 8471405]
[26]
Perez, M.; Ramirez, G.; Perez, M.; Restrepo, P. Validation of an analytical method for the determination of valsartan in human plasma by HPLC/UV with addition standard using losartan as an internal standard. Colom. Med., 2007, 38(1), 13-20.
[27]
Burnier, M.; Wuerzner, G. Pharmacokinetic evaluation of losartan. Expert Opin. Drug Metab. Toxicol., 2011, 7(5), 643-649.
[http://dx.doi.org/10.1517/17425255.2011.570333] [PMID: 21417956]
[28]
Amini, H.; Ahmadiani, A.; Moazenzadeh, M. Pharmacokinetics of losartan and its active metabolite EXP3174 in healthy iranian subjects. Clin. Drug Investig., 2004, 24(10), 619-623.
[http://dx.doi.org/10.2165/00044011-200424100-00008] [PMID: 17523724]
[29]
Lo, M.W.; Toh, J.; Emmert, S.E.; Ritter, M.A.; Furtek, C.I.; Lu, H.; Colucci, W.S.; Uretsky, B.F.; Rucinska, E. Pharmacokinetics of intravenous and oral losartan in patients with heart failure. J. Clin. Pharmacol., 1998, 38(6), 525-532.
[http://dx.doi.org/10.1002/j.1552-4604.1998.tb05790.x] [PMID: 9650542]
[30]
Dorado, P.; Machín, E.; de Andrés, F.; Naranjo, M.E.; Peñas-Lledó, E.M.; Llerena, A. Development of a HPLC method for the determination of losartan urinary metabolic ratio to be used for the determination of CYP2C9 hydroxylation phenotypes. Drug Metabol. Drug Interact., 2012, 27(4), 217-233.
[http://dx.doi.org/10.1515/dmdi-2012-0018] [PMID: 23093260]
[31]
Furtek, C.I.; Lo, M.W. Simultaneous determination of a novel angiotensin II receptor blocking agent, losartan, and its metabolite in human plasma and urine by high-performance liquid chromatography. J. Chromatogr. A, 1992, 573(2), 295-301.
[32]
Yeung, P.K.F.; Jamieson, A.; Smith, G.J.; Fice, D.; Pollak, P.T. Determination of plasma concentrations of losartan in patients by HPLC using solid phase extraction and UV detection. Int. J. Pharm., 2000, 204(1-2), 17-22.
[http://dx.doi.org/10.1016/S0378-5173(00)00453-1] [PMID: 11011981]
[33]
Furtek, C.I.; Lo, M.W. Simultaneous determination of a novel angiotensin II receptor blocking agent, losartan, and its metabolite in human plasma and urine by high-performance liquid chromatography. J. Chromatogr. A, 1992, 573(2), 295-301.
[34]
World Medical Association Declaration of Helsinki. Ethical principles for medical research involving human subjects. JAMA, 2013, 310(20), 2191-2194.
[http://dx.doi.org/10.1001/jama.2013.281053] [PMID: 24141714]
[35]
Reglamento de la Ley General de Salud en Materia de Investigación para la Salud. Publicado en el Diario Oficial de la Federación el día 06 de enero de 1987.

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