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A bioequivalence study of Allergostin compared to administration of Kestin in healthy volunteers
- Authors: Vasilyuk V.B.1,2, Faraponova M.V.1, Verveda A.B.1,3, Fomichev A.V.1, Syraeva G.I.1,4, Kovalenko A.L.5
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Affiliations:
- The Limited Liability Company “Research Center Eco-safety”
- North-Western State Medical University named after I.I. Mechnikov
- Research Institute of Industrial and Maritime Medicine of Federal Medical Biological Agency
- Academician I.P. Pavlov First St. Petersburg State Medical University
- Golikov Research Clinical Center of Toxicology
- Issue: Vol 20, No 2 (2023)
- Pages: 143-151
- Section: Original studies
- Submitted: 09.03.2023
- Accepted: 03.04.2023
- Published: 09.07.2023
- URL: https://rusalljournal.ru/raj/article/view/7525
- DOI: https://doi.org/10.36691/RJA7525
- ID: 7525
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Abstract
BACKGROUND: Ebastine is widely used in medical practice for treating urticaria and allergic rhinitis. This compound is an antiallergic drug that belongs to the second generation of H1 histamine receptor blockers. The effectiveness of ebastine can be observed when it is orally administered. As a part of the registration of the trade name Allergostin, a clinical study of its bioequivalence with Kestin was conducted involving 26 healthy volunteers.
AIM: To summarize the results of the clinical study of the comparative pharmacokinetics and bioequivalence, safety, and the tolerability of Allergostin (film-coated tablets, 20 mg; NTFF POLYSAN LLC, Russia) and Kestin (film-coated tablets, 20 mg; Almirall S.A., Spain) among healthy volunteers after a single oral dose on an empty stomach.
MATERIALS AND METHODS: To confirm bioequivalence, we conducted an open, randomized, two-period crossover study of comparative pharmacokinetics and bioequivalence of drugs with a single oral administration on an empty stomach in healthy male and female volunteers aged ≥18. During the study, blood plasma samples were collected from volunteers. Each sample was tested using a validated high-performance liquid chromatography with tandem mass spectrometry method, and the concentrations of ebastine and the active metabolite carabastin were determined. Based on the obtained data, pharmacokinetic and statistical analyses were carried out, and 90% confidence intervals were calculated for the ratio of the geometric mean values of the pharmacokinetic parameters Cmax and AUC0-72 for carabastin.
RESULTS: Based on the results of statistical analysis, the pharmacokinetic parameters of the test (Allergostin) and reference (Kestin) drugs were characterized by high similarity. For the estimated pharmacokinetic parameters of carabastin, the 90% confidence intervals ranged from 80% to 125% for AUC0-t and Cmax.
CONCLUSION: Therefore, in accordance with the applied criteria, the drugs are recognized as bioequivalent.
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About the authors
Vasiliy B. Vasilyuk
The Limited Liability Company “Research Center Eco-safety”; North-Western State Medical University named after I.I. Mechnikov
Email: vasilyuk_vb@ecosafety.ru
ORCID iD: 0000-0003-2503-4402
SPIN-code: 1459-5548
MD, Dr. Sci. (Med.), Professor
Россия, Saint Petersburg; Saint PetersburgMariia V. Faraponova
The Limited Liability Company “Research Center Eco-safety”
Author for correspondence.
Email: faraponova_mv@ecosafety.ru
ORCID iD: 0000-0003-4212-5453
SPIN-code: 9006-2074
Россия, 65 Yuri Gagarin avenue, 196143 Saint Petersburg
Aleksey B. Verveda
The Limited Liability Company “Research Center Eco-safety”; Research Institute of Industrial and Maritime Medicine of Federal Medical Biological Agency
Email: verveda_ab@ecosafety.ru
ORCID iD: 0000-0003-4029-3170
SPIN-code: 5448-0433
MD, Cand. Sci. (Med.)
Россия, Saint Petersburg; Saint PetersburgAleksey V. Fomichev
The Limited Liability Company “Research Center Eco-safety”
Email: fomichev_av@ecosafety.ru
ORCID iD: 0000-0002-9640-7168
SPIN-code: 8550-5610
MD, Cand. Sci. (Med.)
Россия, Saint PetersburgGulnara I. Syraeva
The Limited Liability Company “Research Center Eco-safety”; Academician I.P. Pavlov First St. Petersburg State Medical University
Email: syraeva_gi@ecosafety.ru
ORCID iD: 0000-0001-6635-9786
SPIN-code: 9650-5671
Россия, Saint Petersburg; Saint Petersburg
Aleksey L. Kovalenko
Golikov Research Clinical Center of Toxicology
Email: alleokov@mail.ru
ORCID iD: 0000-0003-3695-2671
SPIN-code: 7216-8364
Dr. Sci. (Biol.), Cand. Sci. (Chem.)
Россия, Saint PetersburgReferences
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