Pharmacokinetic Comparison of Epinastine Using Developed Human Plasma Assays

Jeong, Seung‐Hyun; Jang, Ji-Hun; Cho, Hea-Young; Lee, Yong-Bok

doi:10.3390/molecules25010209

Cited by 3 publications

(1 citation statement)

References 18 publications

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“…The literature on EPI showed three stability-indicating HPLC methods for its determination in pharmaceuticals [10][11][12], where its stability was examined as a part of the validation procedure. At the same time, LC-MS methods from the literature were only used for quantifying EPI in human plasma [13,14]. As far as EME is concerned, a literature survey revealed one stability-indicating TLC method which enables estimation of chemical degradation of EME [15].…”

Section: Introductionmentioning

confidence: 99%

LC-UV and UPLC-MS/MS Methods for Analytical Study on Degradation of Three Antihistaminic Drugs, Ketotifen, Epinastine and Emedastine: Percentage Degradation, Degradation Kinetics and Degradation Pathways at Different pH

et al. 2020

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Evaluation of pH-dependent reactivity of drugs is an essential component in the pharmaceutical industry. Thus, the stability of three antihistaminic drugs, i.e., ketotifen, epinastine and emedastine, was tested, in solutions of five pH values, i.e., 1.0, 3.0, 7.0, 10.0 and 13.0, at high temperature (70 °C). LC-UV isocratic methods were developed to estimate percentage degradation as well as the kinetics of degradation. Generally, epinastine was shown to be the most stable compound with degradation below 14%. Emedastine was labile in all pH conditions, with degradation in the range 29.26–51.88%. Ketotifen was moderately stable at pH 1–7 (degradation ≤ 14.04%). However, at pH ≥ 10, its degradation exceeded 30%. The kinetics of degradation of ketotifen, epinastine and emedastine was shown as a pseudo-first-order reaction with the rate constants in the range 10−4–10−3 min−1 Finally, the UPLC-MS/MS method was applied to identify the main degradants and suggest degradation pathways. Degradation of ketotifen proceeded with oxidation and demethylation in the piperidine ring of the molecule. As far as epinastine was concerned, opening of the imidazole ring with formation of the amide group was observed. Unfortunately, no degradation products for emedastine were detected. The present results complete the literary data and may be important for both manufacturing of these drugs and their administration to patients.

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Section: Introductionmentioning

confidence: 99%

LC-UV and UPLC-MS/MS Methods for Analytical Study on Degradation of Three Antihistaminic Drugs, Ketotifen, Epinastine and Emedastine: Percentage Degradation, Degradation Kinetics and Degradation Pathways at Different pH

et al. 2020

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Simultaneous measurement of epinastine and its metabolite, 9,13b‐dehydroepinastine, in human plasma by a newly developed ultra‐performance liquid chromatography–tandem mass spectrometry and its application to pharmacokinetic studies

Jeong

Jang

Cho

et al. 2020

Biomedical Chromatography

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Epinastine is an antiallergic drug with high selectivity for histamine receptors. It has been reported that 9,13b‐dehydroepinastine is present as a metabolite in vivo in humans, but there was little information about their pharmacokinetics (PKs) in humans. Although several analytical methods have been reported for epinastine analysis in different matrices, none are available for its metabolite. Therefore, the purpose of this study was to develop an analytical method to simultaneously measure epinastine and its metabolite, 9,13b‐dehydroepinastine, in human plasma samples using an ultra‐performance liquid chromatography–tandem mass spectrometer. Analytes were separated on a C18 column. Quantification of this analysis was performed on a triple‐quadrupole mass spectrometer. Chromatograms showed high sensitivity, selectivity, and resolution with no interference with plasma constituents. Calibration curves for both epinastine and 9,13b‐dehydroepinastine in human plasma were 0.1–50 ng/ml and displayed excellent linearity with correlation coefficients (r2) >0.99. The developed analytical method satisfied the criteria of international guidance and was validated. The method could be successfully applied to pharmacokinetic studies of epinastine and, for the first time, the metabolite kinetics of epinastine to 9,13b‐dehydroepinastine in humans after oral administration of 20 mg epinastine hydrochloride tablets. Our study is expected to be useful in future studies such as dosage settings and clinical pharmacotherapy.

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Exploitation of metal-organic framework/ polyaniline composite as an efficient transducer for potentiometric determination of epinastine hydrochloride

Abdallah¹

2023

International Journal of Electrochemical Science

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Pharmacokinetic Comparison of Epinastine Using Developed Human Plasma Assays

Cited by 3 publications

References 18 publications

LC-UV and UPLC-MS/MS Methods for Analytical Study on Degradation of Three Antihistaminic Drugs, Ketotifen, Epinastine and Emedastine: Percentage Degradation, Degradation Kinetics and Degradation Pathways at Different pH

LC-UV and UPLC-MS/MS Methods for Analytical Study on Degradation of Three Antihistaminic Drugs, Ketotifen, Epinastine and Emedastine: Percentage Degradation, Degradation Kinetics and Degradation Pathways at Different pH

Simultaneous measurement of epinastine and its metabolite, 9,13b‐dehydroepinastine, in human plasma by a newly developed ultra‐performance liquid chromatography–tandem mass spectrometry and its application to pharmacokinetic studies

Exploitation of metal-organic framework/ polyaniline composite as an efficient transducer for potentiometric determination of epinastine hydrochloride

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