Novel liquid chromatographic methods for the determination of varenicline tartrate

El‐Bagary, Ramzia I.; Abo-Talib, Nisreen F.; Mohamed, Marwa A. El-Wahab

doi:10.1016/j.talanta.2015.07.077

Cited by 9 publications

(8 citation statements)

References 25 publications

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“… 33 , 34 A forced degradation study on VRC solution reported complete degradation of VRC under the presence of hydrogen peroxide (30%, w/v) by heating in a water bath at 90°C for 4 hours, whereas relatively mild degradation of VRC was observed in strong alkaline and acidic conditions; that is, 10% and 14% of VRC was degraded by 5 N NaOH and 5 N HCl at 90°C for 9 hours, respectively, and in comparison, the degradation was found to be 0.29% and 0.31% after alkaline hydrolysis (0.1 N NaOH for 2 hours in a boiling water bath) and acid hydrolysis (0.1 N HCl for 2 hours in a boiling water bath), respectively. 33 However, VRC was stable to boiling (solution refluxed for 2 hours in a boiling water bath), UV irradiation (powder exposed to UV light for 72 hours), and oxidation (solution with 30% hydrogen peroxide at 25°C for 2 hours), as no degradation products were observed in the HPLC chromatograms. 34 These results confirmed that VRC-S in tablet formulations could be sufficiently stable in the accelerated condition.…”

Section: Resultsmentioning

confidence: 99%

Immediate release tablet formulation of varenicline salicylate and comparative pharmacokinetic study in human volunteers

Kwak¹,

Lee²,

Yoon³

et al. 2018

DDDT

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PurposeTo develop an immediate release-type tablet containing varenicline salicylate (VRC-S), a smoking cessation agent, formulation and stability studies were performed. The in vitro dissolution and in vivo pharmacokinetic (PK) behavior of the tablets were compared with those of the commercial product (Champix) as a reference.Materials and methodsThe characteristics of the powder were investigated by particle morphology, size distribution, solubility, hygroscopicity, differential scanning calorimetry, and powder X-ray diffraction. Based on the drug–excipient compatibility test, different VRC-S tablets were prepared with the selected excipients through direct compression or wet granulation method and subjected to a dissolution test. The stability of the most promising VRC-S tablet (F4) was evaluated under accelerated conditions (40°C and 75% relative humidity). Further, the dissolution and human pharmacokinetic profiles of the F4 tablet and Champix were compared.ResultsVRC-S showed a positively skewed unimodal size distribution with a specific surface area of 2.02 m2/g, single endothermic peak of 225.2°C in differential scanning calorimetry, crystalline internal structure in powder X-ray diffraction, aqueous solubility of 244.7 mg/mL, and hygroscopicity of 0.256 mg/g. The wet granulation method was preferred for tablet preparation and employed the following excipients: microcrystalline cellulose and anhydrous dibasic calcium phosphate as diluents, croscarmellose sodium as a disintegrant, and colloidal silicon dioxide and magnesium stearate as lubricants. The F4 tablet was stable for 6 months under accelerated conditions. The dissolution of VRC was pH independent, revealing f2 values of 76.49 and 68.38 at pH 1.2 and pH 6.8, respectively. After the oral administration of F4 tablet and Champix to healthy human volunteers, pharmacokinetic parameters, including time to reach the maximum plasma concentration (Tmax), maximum plasma concentration (Cmax), and area under the curve from 0 to infinity (AUCinf), were compared. The values of 90% CI were 0.972–1.035 for Cmax and 0.982–1.075 for AUCinf, which was indicative of the bioequivalence of both products.ConclusionVRC-S–containing F4 tablet might be a good candidate for smoking cessation treatment.

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Section: Resultsmentioning

confidence: 99%

Immediate release tablet formulation of varenicline salicylate and comparative pharmacokinetic study in human volunteers

Kwak¹,

Lee²,

Yoon³

et al. 2018

DDDT

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“…Although the light absorption characteristics of VAR are available in literature [9,12], we recorded the UV-absorption spectrum in methanol in order to select the appropriate analytical wavelength, while simultaneously verifying available data. As shown in Figure 1, VAR has three absorption maxima at 237, 269 and 320 nm which were considered in further analysis.…”

Section: Resultsmentioning

confidence: 99%

“…Available clinical-trial data support its use as an effective and generally well-tolerated therapy for smoking cessation in healthy adult smokers [6]. High performance liquid chromatography (HPLC) is the predominant method used for varenicline analysis [7][8][9][10][11][12][13][14]. Other analytical techniques are used sporadically, including mainly spectroscopic techniques [10,15,16].…”

Section: Development and Validation Of The Hplc Methods For Vareniclinmentioning

confidence: 99%

“…Varenicline has been analyzed using UV-VIS spectrophotometry [15], fluorimetry [16], nuclear magnetic resonance spectroscopy (1H NMR and 13C NMR) [10], mass spectrometry (MS) [10,13,14] and Fourier-transform infrared spectroscopy (FTIR) [10]. Most frequently, papers refer to the quantification of varenicline in its pharmaceutical preparations [7][8][9][10][11][12]15,16]. Quality control of varenicline-containing preparations using a simple, sensitive, precise and accurate HPLC methods is necessary due to the fact that these preparations are often imported and are often exposed to different transport conditions [9].…”

Section: Development and Validation Of The Hplc Methods For Vareniclinmentioning

confidence: 99%

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Development and validation of the HPLC method for varenicline determination in pharmaceutical preparation

Pietraś

Szymańska

Kondej

et al. 2017

Current Issues in Pharmacy and Medical Sciences

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A simple and accurate reverse phase HPLC method has been developed and validated for quantification of varenicline in bulk drug and pharmaceutical dosage forms. Herein, an isocratic LC analysis was carried out on a Chromolith Performance RP18e column with methanol-buffer solution pH 3.5 (a buffer solution containing sodium benzoate (0.5 mmol/l) adjusted to pH 3.5 with trifluoroacetic acid (20 mmol/l) (55:45, V/V)) at a flow rate of 1.2 ml/min. The detection wavelength was set at 320 nm. The calibration curve was linear (r = 0.9999) in the studied range of concentration (0.2-10 μg/ml). The selectivity and sensitivity of the elaborated method were satisfactory, and the limits of detection and quantification was less than 20% of the specification level. Moreover, the inter-and intra-day precisions was found to be less than 3% (RSD), while the recovery values expressing inter-and intra-day accuracy was varied from 99.73 to 101.23. The varenicline solution was stable over a period of 3 days on storage under refrigeration. The utility of the developed method was examined by analysing the tablets containing VAR. As a result, the method was found to be selective, sensitive, precise and accurate.

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“…Some papers deal with the analysis of this drug and/or its (bio) degradation products in different matrices—dosage forms, tissues, blood, plasma, serum or human urine. Most of them are dedicated to the chromatographic methods such as HPLC, UHPLC with conventional UV or advanced MS detection . To our best knowledge, only four papers describe CE methods for the separation of VAR and only one of them is associated with the analysis of VAR in complex biological matrices such as human urine .…”

Section: Introductionmentioning

confidence: 99%

Comparison of hydrodynamically closed two-dimensional capillary electrophoresis coupled with ultraviolet detection and hydrodynamically open capillary electrophoresis hyphenated with mass spectrometry in the bioanalysis of varenicline

et al. 2017

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Two capillary electrophoresis methods for monitoring renally excreted varenicline, a highly effective drug prescribed for smoking cessation, in human urine were developed and compared. A method combining capillary electrophoresis with mass spectrometry was proposed for the fast analysis of varenicline (analysis time up to 7 min). Here, mass spectrometry was a prerequisite for achieving high sensitivity and selectivity of the analysis suitable for the quantification of a 15 ng/mL level of varenicline in un-pretreated urine matrices. An alternative approach, two-dimensional (column-coupled) capillary electrophoresis with enhanced sample load capacity and ultraviolet detection, was proposed as a low-cost alternative to capillary electrophoresis with mass spectrometry. The isotachophoresis on-line sample treatment included simple elimination of the major matrix constituents and stacking of the sample in a large volume so that threefold lower quantitation limits could be easily achieved in comparison to the capillary electrophoresis with mass spectrometry. On the other hand, longer analysis time (ca. 4.5-fold) and more complex electrolyte system in the coupled zone electrophoresis step (including two additives enhancing separation selectivity, i.e. isopropanol and cyclodextrin) were prerequisites for the complete separation of varenicline from the sample matrix. Anyway, both the developed methods were validated according to the Food and Drug Administration guidelines showing favorable performance parameters, suitable for their routine biomedical use.

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Novel liquid chromatographic methods for the determination of varenicline tartrate

Cited by 9 publications

References 25 publications

Immediate release tablet formulation of varenicline salicylate and comparative pharmacokinetic study in human volunteers

Immediate release tablet formulation of varenicline salicylate and comparative pharmacokinetic study in human volunteers

Development and validation of the HPLC method for varenicline determination in pharmaceutical preparation

Comparison of hydrodynamically closed two-dimensional capillary electrophoresis coupled with ultraviolet detection and hydrodynamically open capillary electrophoresis hyphenated with mass spectrometry in the bioanalysis of varenicline

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