The study of bioequivalence of twо ezetimib drugs after single oral administration in healthy volunteers

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Abstract

Aim. To compare pharmacokinetics and bioavailability of ezetimib drugs - Otrio, 10 mg tablets (AKRIKhIN, Russia) and Esetrol®, 10 mg tablets (Schering-Plow Labo N.V., Belgium) after single dose under fasting conditions in healthy volunteers. The study was conducted in accordance with the standards of Good Clinical Practice and the legislation of the Russian Federation. Materials and methods. 64 healthy volunteers were enrolled in an open, randomized, crossover study. After overnight fasting drugs (tested and reference drug) were administered as a single dose, separated by two-weeks washout period. Blood sampling for the deterioration of ezetimibe was performed over 72 hours post dose. A validated HPLC-MS/MS method was used for quantification of ezetimibe in plasma. Pharmacokinetic parameters were determined. Results. The 90% confidence intervals of the ratio for the Ln-transformed AUC0-72 and Сmax ratios are within 80-125% according to existing guidelines. Conclusion. Otrio, 10 mg tablets (Akrikhin, Russia) is bioequivalent to Ezetrol®, 10 mg tablets (Schering-Plough Labo N.V., Belgium).

About the authors

Veronika V. Tolkacheva

People’s Friendship University of Russia

Email: tolkachevav@mail.ru
D. Sci. (Med.), Associate Professor of the Department of Internal Medicine with Cardiology and Functional Diagnostics course in V.S.Moiseyev academy 6, Miklukho-Maklaya st., Moscow, 117198, Russian Federation

Irina P. Malaya

Ascent CRS

Cand. Sci. (Med.), medical director 4, 1, block Б, entrance 7, floor 7, office 717Б, Business Park Rumyantsevo, 22nd km of the Kievskoe highway, housing estate, Moscow, 108811, Russian Federation*

Nazilia Kh. Bagmanova

People’s Friendship University of Russia

Cand. Sci. (Med.), Associate Professor of the Department of Internal Medicine with Cardiology and Functional Diagnostics Course in V.S.Moiseyev Academy 6, Miklukho-Maklaya st., Moscow, 117198, Russian Federation

Zhanna D. Kobalava

People’s Friendship University of Russia

D. Sci. (Med.), Prof., Head of the Department of Internal Medicine with Cardiology and Functional Diagnostics Course in V.S.Moiseyev Academy, People’s Friendship University of Russia, Head of the Department of Internal Medicine, Cardiology and Clinical Pharmacology 6, Miklukho-Maklaya st., Moscow, 117198, Russian Federation

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