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Urinary Excretion Kinetics of 9-(2-Diethylaminoethyl)-2-Phenylimidazo[1,2-a]Benzimidazole Dinitrate and Determination of the Main Metabolite in Blood Serum of Laboratory Animals

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Urinary excretion of 9-(2-diethylaminoethyl)-2-phenylimidazo[1,2-a]benzimidazole dinitrate after intragastric administration at a dose of 10 mg/kg has been studied in laboratory rats. The main metabolite in blood serum of rats was determined after a single intravenous injection at a dose of 10 mg/kg. The metabolite was determined in urine samples using HPLC. Its structure was established using HPLC-MS. According to the results, the drug substance was excreted unchanged in small amounts (~0.01% of the administered dose) because it was metabolized. The main metabolite was found in rat plasma as early as 3 min after intravenous injection at a dose of 10 mg/kg.

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Acknowledgments

The chemical part of the article was prepared with the assistance of Southern Federal University with financial support from the RF Ministry of Science and Higher Education [State Task for Scientific Activity, Southern Federal University, 2020, Project FENW-2020-0031 (0852-2020-0031)].

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Authors and Affiliations

  1. Pyatigorsk Medical and Pharmaceutical Institute, Branch of Volgograd State Medical University, 11 Kalinina Prosp., Pyatigorsk, 357500, Russia

    D. O. Mitrakova, M. V. Chernikov & I. P. Remezova

  2. State Scientific Center for Expert Evaluation of Medicinal Products, Ministry of Health of the Russian Federation, 8 Petrovskii Blvd., Moscow, 127051, Russia

    N. D. Bunyatyan

  3. Sechenov First Moscow State Medical University (Sechenov University), 8/2 Trubetskaya St., Moscow, 119991, Russia

    N. D. Bunyatyan

  4. State Institute of Medicines and Good Practices, 6 Lavrov Pereulok, Moscow, 109044, Russia

    A. V. Morozov

Authors
  1. D. O. Mitrakova
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  2. M. V. Chernikov
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  3. I. P. Remezova
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  4. N. D. Bunyatyan
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  5. A. V. Morozov
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Corresponding author

Correspondence to D. O. Mitrakova.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 56, No. 8, pp. 11 – 16, August, 2022.

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Mitrakova, D.O., Chernikov, M.V., Remezova, I.P. et al. Urinary Excretion Kinetics of 9-(2-Diethylaminoethyl)-2-Phenylimidazo[1,2-a]Benzimidazole Dinitrate and Determination of the Main Metabolite in Blood Serum of Laboratory Animals. Pharm Chem J 56, 1027–1032 (2022). https://doi.org/10.1007/s11094-022-02747-3

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  • DOI: https://doi.org/10.1007/s11094-022-02747-3

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