A bioequivalence study of Allergostin compared to administration of Kestin in healthy volunteers

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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

Russian Federation, Saint Petersburg; Saint Petersburg

Mariia 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
Russian Federation, 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.)

Russian Federation, Saint Petersburg; Saint Petersburg

Aleksey 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.)

Russian Federation, Saint Petersburg

Gulnara 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
Russian Federation, 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.)

Russian Federation, Saint Petersburg


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Supplementary files

Supplementary Files
1. Fig. 1. Average plots of the dependence of the concentration of the active metabolite of carabastin in blood plasma on time (drug sampling points) in volunteers after taking Allergostin (T) and Kestin (R) on a linear scale.

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2. Fig. 2. Average plots of the dependence of the concentration of the active metabolite of carabastin in blood plasma on time (drug sampling points) in volunteers after taking Allergostin (T) and Kestin (R) on a semi-logarithmic scale.

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