Bioanalysis of antimalarials using liquid chromatography

Wahajuddin,; Raju, K. Kanaka; Taneja, Isha

doi:10.1016/j.trac.2012.09.014

Cited by 12 publications

(3 citation statements)

References 135 publications

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“…Artemether ( Figure 1 ) is a lipophilic drug and a methyl ether derivative of artemisinin ( Liu et al, 2011 ; Raju and Taneja, 2013 ), having a logP value of 3.5 ( Matsa et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Estimation of dihydroartemisinin in human plasma using a highly sensitive LTQ Orbitrap mass spectrometer with Xcalibur software

et al. 2023

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Background: Artemether (ARM), the O-methyl ether prodrug of dihydroartemisinin (DHA), is considered a first-line antimalarial agent. Artemether is extensively metabolized in vivo to its active metabolite DHA, and therefore its determination offers considerable difficulties. In the present study, DHA identification and estimation were accurately performed by the mass spectrometric analysis, using a high-resolution liquid chromatography/electrospray ionization-mass spectrometry (LC/ESI-MS) LTQ Orbitrap hybrid mass spectrometer.Methods: The plasma samples were taken from healthy volunteers, and the spiked plasma was extracted by adding 1 mL of a mixture of dichloromethane and tert.-methyl butyl ether (8:2 v/v) to 0.5 mL of plasma. The internal standard solution (artemisinin 500 ng/mL) was added to the plasma samples. After vertexing and centrifugation, the organic layer was separated and transferred into another tube and dried under nitrogen. The residue was reconstituted in 100 μL of acetonitrile and was injected onto the LC-MS system for analysis. Measurement of standards and samples was carried out isocratically on a Surveyor HPLC system combined with an LTQ Orbitrap mass spectrometer using an ACE 5 C18-PFP column. Mobile phase A consisted of 0.1% v/v formic acid in water, Mobile phase B consisted of acetonitrile only, and isocratic elution was carried out with A:B 20:80, v/v. The flow rate was 500 μL/min. The ESI interface was operated in a positive ion mode with a spray voltage of 4.5 kV.Results: Artemether is not a very biologically stable compound and is immediately metabolized to its active metabolite dihydroartemisinin, so no clear peak was observed for artemether. Both artemether and DHA after ionization undergo neutral losses of methanol and water, respectively, in the source of the mass spectrometer. The ions observed were (MH-H2O) m/z 267.15 for DHA and (MH-m/z 283.15 for internal standard artemisinin. The method was validated according to international guidelines.Discussion: The validated method was applied successfully for the determination and quantification of DHA in plasma samples. This method works well for the extraction of drugs, and the Orbitrap system with the help of Xcalibur software accurately and precisely determines the concentration of DHA in spiked as well as volunteer’s plasma.

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“…Artemether ( Figure 1 ) is a lipophilic drug and a methyl ether derivative of artemisinin ( Liu et al, 2011 ; Raju and Taneja, 2013 ), having a logP value of 3.5 ( Matsa et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Estimation of dihydroartemisinin in human plasma using a highly sensitive LTQ Orbitrap mass spectrometer with Xcalibur software

et al. 2023

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“…Lumefantrine (LUME) (previously known as benflumetol) was synthesized in the 1970s by the Academy of Military Medical Sciences in Beijing, China. It is a racemic fluorene derivative, named 2-dibutylamino-1-[2,7-dichloro-9-(4-chlorobenzylidene)- 9H-fluoren-4-yl]-ethanol [ 2 , 3 ]. It is the long-acting partner drug of the artemisinin derivative artemether, in this ACT.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous quantification of proposed anti-malarial combination comprising of lumefantrine and CDRI 97–78 in rat plasma using the HPLC–ESI-MS/MS method: application to drug interaction study

Wahajuddin

Singh

Taneja

et al. 2015

Malar J

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BackgroundLumefantrine is the mainstay of anti-malarial combination therapy in most endemic countries presently. However, it cannot be used alone owing to its long onset time of action. CDRI 97–78 is a promising trioxane-derivative anti-malarial candidate that is currently being investigated as a substitute for artemisinin derivatives owing to their emerging resistance.MethodsIn the present study, a sensitive, simple and rapid high-performance liquid chromatography coupled with positive ion electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method was developed for the simultaneous determination of lumefantrine and CDRI 97-78’s metabolite, 97–63, in rat plasma using halofantrine as an internal standard. Lumefantrine and 97–63 were separated on a Waters Atlantis C18 (4.6 × 50 mm, 5.0 μm) column under isocratic condition with mobile phase consisting of acetonitrile: methanol (50:50, v/v) and ammonium formate buffer (10 mM, pH 4.5) in the ratio of 95:5 (v/v) at a flow rate of 0.65 mL/min.ResultsThe method was accurate and precise within the linearity range 3.9-500 ng/mL for both lumefantrine and 97–63 with a correlation coefficient (r2) of ≥0.998. The intra- and inter-day assay precision ranged from 2.24 to 7.14% and 3.97 to 5.90%, and intra- and inter-day assay accuracy was between 94.93 and 109.51% and 96.87 and 108.38%, respectively, for both the analytes. Upon coadministration of 97–78, the relative bioavailability of lumefantrine significantly decreased to 64.41%.ConclusionsA highly sensitive, specific and reproducible high-throughput LC-ESI-MS/MS assay was developed and validated to quantify lumefantrine and CDRI 97–78. The method was successfully applied to study the effect of oral co-administration of lumefantrine on the pharmacokinetics of 97–78 in male Sprague–Dawley rats and vice versa. Co-administration of 97–78 significantly decreased the systemic exposure of lumefantrine.Electronic supplementary materialThe online version of this article (doi:10.1186/s12936-015-0684-5) contains supplementary material, which is available to authorized users.

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“…A literature survey revealed few liquid chromatography (LC) assay methods that have been reported for the determination of Arterolane in bulk dug and pharmaceutical dosage forms, but there are no reported methods for simultaneous estimation of Arterolane maleate and Piperaquin phosphate in combined pharmaceutical dosage forms [3][4][5][6][7][8][9][10][11] . The present International Conference on Harmonization (ICH) drug stability guidelines suggest that stress studies should be conducted on the drug product to establish its inherent stability characteristics, and the analytical method should able to separate all degradation impurities formed under stress studies to prove its stability-indicating power.…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of a Stability Indicating Liquid Chromatographic Method for Simultaneous Estimation of Arterolane Maleate and Piperaquine Phosphate in Combined Dosage Form

Reddy¹,

Reddy²,

Reddy.L³

2013

Orient. J. Chem

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A novel stability indicating isocratic, reversed phase-liquid-chromatographic method has been developed for the simultaneous quantitative determination of Arterolane maleate And Piperaquine phosphate in combined-dosage form. A thermo hypersil BDS C18 (250*4.6*5µ) column with mobile phase containing water pH 2.8 adjusted with ortho phosphoric acid: methanol in the ratio of (60: 40, v/v) was used. The flow rate was 1.0 mL/min, column temperature was 30°C and effluents were monitored at 241 nm. The retention times of Arterolane Maleate and Piperaquine Phosphate were 1.864min and 3.047min, respectively. Correlation co-efficient for Arterolane Maleate and Piperaquine Phosphate was found to be 0.99 and 0.99, respectively. The proposed method was validated with respect to linearity, accuracy, precision, specificity, and robustness. Recovery of Arterolane Maleate and Piperaquine Phosphate in formulations was found to be in the range of 97-103% and 97-103% respectively confirms the non-interferences of the excipients in the formulation. Arterolane Maleate and Piperaquine Phosphate were exposed to stress conditions like acidic hydrolysis, basic hydrolysis, oxidative, photolytic, humidity and thermal conditions. Due to its simplicity, rapidness and high precision, the method was successfully applied to the estimation of Arterolane Maleate and Piperaquine Phosphate in combined dosage form.Key words: Arterolane Maleate, Piperaquine Phosphate, Method validation, Forced degradation.Plasmodium falciparum is responsible for half of these cases. Fixed dose combination of arterolane maleate (150 mg) and piperaquine phosphate (750 mg) has been recently approved by FDA as a once-a day therapy for three days for the treatment of acute, uncomplicated Plasmodium falciparum malaria 3 .

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Bioanalysis of antimalarials using liquid chromatography

Cited by 12 publications

References 135 publications

Estimation of dihydroartemisinin in human plasma using a highly sensitive LTQ Orbitrap mass spectrometer with Xcalibur software

Estimation of dihydroartemisinin in human plasma using a highly sensitive LTQ Orbitrap mass spectrometer with Xcalibur software

Simultaneous quantification of proposed anti-malarial combination comprising of lumefantrine and CDRI 97–78 in rat plasma using the HPLC–ESI-MS/MS method: application to drug interaction study

Development and Validation of a Stability Indicating Liquid Chromatographic Method for Simultaneous Estimation of Arterolane Maleate and Piperaquine Phosphate in Combined Dosage Form

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