Development of a rapid HPLC method for determination of famotidine in human plasma using a monolithic column

Zarghi, Afshin; Shafaati, Alireza; Foroutan, Seyed Mohsen; Khoddam, Arash

doi:10.1016/j.jpba.2005.03.029

Cited by 49 publications

(33 citation statements)

References 10 publications

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“…Approximately 1 mL of whole blood collected from untreated rats was infused via the femoral artery at 0.25, 1, and 4 h to replace the blood loss due to blood sampling. Each blood sample was centrifuged at 16 810×g for 5 min, and 200 μL of each plasma sample was stored at -40 °C until HPLC analysis of losartan and EXP-3174 was performed [11] .…”

Section: Chemicalsmentioning

confidence: 99%

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Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats

Yang

Cho

2011

Acta Pharmacol Sin

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npg IntroductionLosartan (DuP 753,, an angiotensin II receptor antagonist, has a low side-effect profile and is approved for the treatment of hypertension, alone or in combination with other agents [1] . After oral administration, losartan is almost completely absorbed and extensively metabolized to a carboxylic acid derivative, EXP-3174, mainly by cytochrome P450 (CYP) 2C9 and 3A4 [2] . EXP-3174 is a major active metabolite in both rats and humans and is a more potent inhibitor of angiotensin II receptor than losartan, with high-affinity receptor specificity [3] . Losartan has also been reported to be a substrate of P-glycoprotein (P-gp) [4] . Considering that losartan is a substrate of both CYP enzymes and P-gp, the modulation of CYP and P-gp activities may cause significant changes in the pharmacokinetic profiles of losartan and its active metabolite, EXP-3174.Ticlopidine, a potent antiplatelet agent induced by adenosine diphosphate, is used for the treatment of a variety of platelet-dependent disease states [5] . Several papers recommend ticlopidine as a valuable alternative when patients cannot tolerate aspirin [6,7] . It has been reported that ticlopidine causes significant inhibition of several drugs metabolized by the hepatic CYP enzyme system [8,9] .Clinically, losartan and ticlopidine can be prescribed concomitantly for the prevention or therapy of cardiovascular diseases. However, the pharmacokinetic interaction between ticlopidine and losartan in vivo has not yet been reported. Therefore, the present study aimed to evaluate the effect of ticlopidine on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats. The effects of ticlopidine on P-gp, CYP2C9, and 3A4 activities were also evaluated. Materials and methods ChemicalsLosartan, EXP-3174, L-158.809 (internal standard), acetonitrile, methanol, and tert-butylmethylether were purchased from Merck Corporation (Darmstadt, Germany). Ticlopidine was purchased from Sigma-Aldrich Corporation (St Louis, MO, USA). All other chemicals were of reagent grade, and all solvents were of HPLC grade. Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in ratsSi-hyung YANG 1 , Young-ah CHO 2 , Jun-shik CHOI 3, * Aim: Losartan and antiplatelet agent ticlopidine can be prescribed concomitantly for prevention or therapy of cardiovascular diseases. Hence, the effects of ticlopidine on the pharmacokinetics of losartan and its active metabolite EXP-3174 were evaluated in rats. Methods: Ticlopidine (4 or 10 mg/kg po) was administered 30 min before administration of losartan (9 mg/kg po or 3 mg/kg iv). The activity of human CYP2C9 and 3A4 were measured using the CYP inhibition assay kit. The activity of P-gp was evaluated using rhodamine-123 retention assay in MCF-7/ADR cells. Results: Ticlopidine (10 mg/kg) significantly increased the areas under the plasma concentration-time curves (AUCs) and peak plasma concentration (C max ) of oral losartan (9 mg/kg), as well as the AUCs of the active metabolite EXP-3174. Ticlopid...

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Section: Chemicalsmentioning

confidence: 99%

“…Plasma concentrations of losartan were determined using an HPLC assay, which was modified from the reported method [11] . Briefly, a 50 μL aliquot of L-158.809 (internal standard, 5 μg/mL dissolved in methanol) and a 0.5 mL aliquot of acetonitrile were added to a 0.2 mL aliquot of the plasma sample in a 2.0 mL polypropylene microtube.…”

Section: Hplc Assaymentioning

confidence: 99%

Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats

Yang

Cho

2011

Acta Pharmacol Sin

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“…A literature survey retrieved a large number of references reporting analytical methods for the determination of these compounds. Mainly separation techniques such as Gas Chromatography (GC) [2], High Performance Thin Layer Chromatography (HPTLC) [3][4][5][6][7][8][9][10], Capillary Electrophoresis (CE) [11][12][13][14][15][16][17] and High Performance Liquid Chromatography (HPLC) [18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34] have been used, with the latter being the predominant technique for the determination of these compounds in a variety of matrices, utilizing different methods of sample pretreatment and detection modes. HPLC with ultra-violet (UV) detection, employing reversed phase particle packed columns, is most frequently used for the analysis of these drugs in pharmaceutical preparations and biological fluids.…”

Section: Introductionmentioning

confidence: 99%

Use of a monolithic column for the development and validation of a HPLC method for the determination of famotidine, cimetidine and nizatidine in biological fluids

Κοντού¹,

Zotou²

2017

J Appl Bioanal

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A simple and selective HPLC method, using a monolithic column, was developed for the simultaneous determination of the histamine H 2 -receptor antagonists: famotidine, cimetidine and nizatidine, in the presence of sulfadimethoxine as internal standard. The separation was performed on a Chromolith Performance RP-18 column (100 mm x 4.6 mm i.d.) with an isocratic mobile phase consisting of 0.05 mol/L acetate buffer (adjusted to pH 6.5 with triethylamine)/methanol/ acetonitrile (85:10:5, v/v/v). The wavelength was set at 230 nm. Linearity was obtained for concentrations between 0.2 to 50 μg/mL and limits of detection were in the range 0.07-0.17 μg/mL. Full validation with respect to linearity, selectivity, detection and quantification limits, accuracy, precision and robustness, the latter using the Youden's test, was carried out. The method was successfully applied to the determination of the drugs in human serum and urine following solid phase extraction. Average recoveries between 88.0 to 104.4% and 88.0 to 108.0% in serum and urine samples, respectively, were obtained.

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“…It is often used in the treatment of Helicobacter infection, inflammatory bowel disease, canine parvovirus, ingestion of a toxin that could be ulcerating, any disease involving protracted vomiting, or chronically in combination with medications which may have stomach irritating properties 1 . Various analytical methods such as high performance liquid chromatography [2][3][4] , fluorimetry 5 , capillary electrophoresis 6 , polarography 7 , voltammetry 8 , and potentiometry 9 have been reported for the determination of famotidine. However, these methods are expensive and not available at most quality control laboratories.…”

Section: Introduction Famotidine 3-[[[2-[(aminoiminomethyl)amino]-4-mentioning

confidence: 99%

Spectrophotometric Methods for the Determination of Famotidine in Drug Formulations.

Araujo

Perdomo²,

Montiel³

et al. 2012

Int J of Adv in Phar Ana

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This paper describes two sensitive and simple spectrophotometric methods for determination of famotidine in pharmaceutical preparations. The first method is based on the hydrolisis of famotidine with sodium hydroxide assisted with microwave radiation, whereby the sulfide ion is produced. The sulfide was allowed to react with N, N -diethyl -p -phenylendiamine oxalate and Fe (III), and the blue color produced was measured at 671 nm. Beer's law was fulfilled in the concentration range 0.6 -52.8 µg/ml, with a detection limit of 0.2 µg/ml. The second method is based upon the formation of a ternary complex between lead (II), eosin and famotidine in the presence of methyl cellulose as a surfactant. The ternary complex showed an absorption maximum at 541 nm. The method obeys Beer's law over concentration range of 7.4-100.0 µg/ml. The methods are simple, sensitive and accurate. The proposed method was applied on the famotidine determination in tablets and intravenous solution, shows recoveries in the range of 97.9-104.2 %. The results obtained by proposed methods were statistically validated.

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Development of a rapid HPLC method for determination of famotidine in human plasma using a monolithic column

Cited by 49 publications

References 10 publications

Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats

Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats

Use of a monolithic column for the development and validation of a HPLC method for the determination of famotidine, cimetidine and nizatidine in biological fluids

Spectrophotometric Methods for the Determination of Famotidine in Drug Formulations.

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