Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats

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Abstract

An important stage in the preclinical study of a new drug is the study of its pharmacokinetics: absorption, distribution, metabolism, and excretion of the drug compound.

The purpose of this study was to study the pharmacokinetics in healthy animals of a new analgesic based on hexaazaisowurtzitane (thiowurtzine).

Materials and methods. A technique for determining the concentration of thiowurtzine in the blood plasma and rat excreta has been developed and validated. Using high-performance liquid chromatography and tandem mass spectrometry, concentrations of thiowurtzine in plasma and rat excreta were determined after a single intragastric dose of 100 mg/kg.

Results. The peak concentration of thiowurtzine in the blood plasma of rats accounts for 2 hours, which is consistent with the pharmacodynamic data of the analgesic, the average retention time of the substance in the body reached 17.15 h after administration. Thiowurtzine is believed to be actively metabolized.

About the authors

Ksenya A. Lopatina

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Author for correspondence.
Email: k.lopatina@pharmso.ru

PhD, Senior Researcher of Oncopharmacology Laboratory

Russian Federation, Tomsk

Olga S. Bryushinina

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: k.lopatina@pharmso.ru

PhD, Researcher of Molecular and Clinical Physiology Laboratory

Russian Federation, Tomsk

Roman V. Gurto

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: roman.gurto@pharmso.ru

PhD, Leading Researcher of Molecular and Clinical Physiology Laboratory

Russian Federation, Tomsk

Svetlana G. Krylova

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: krylova5935@gmail.com

PhD, MD, Leading Researcher of Oncopharmacology Laboratory

Russian Federation, Tomsk

Yulia G. Zuzkova

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: roman.gurto@pharmso.ru

Junior Researcher of Molecular and Clinical Physiology Laboratory

Russian Federation, Tomsk

Darya A. Kulagina

Institute for Problems of Chemical and Energetic Technologies of the Siberian Branch оf the RAS

Email: imbiri@rambler.ru

PhD, Researcher of Medical Chemistry Laboratory

Russian Federation, Biysk

Elena A. Safonova

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: safonova_7@mail.ru

PhD, Researcher of Oncopharmacology Laboratory

Russian Federation, Tomsk

Elena P. Zueva

Tomsk National Research Medical Center of the RAS, Goldberg Research Institute of Pharmacology and Regenerative Medicine

Email: zep0929@mail.ru

PhD, MD, Head of Oncopharmacology Laboratory

Saint Helena, Ascension and Tristan da Cunha, Tomsk

Sergey V. Sysolyatin

Institute for Problems of Chemical and Energetic Technologies of the Siberian Branch оf the RAS

Email: imbiri@rambler.ru

PhD, MD, Head. Institute for Problems of Chemical and Energetic Technologies of the Siberian Branch оf the RAS

Russian Federation, Biysk

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Copyright (c) 2020 Lopatina K.A., Bryushinina O.S., Gurto R.V., Krylova S.G., Zuzkova Y.G., Kulagina D.A., Safonova E.A., Zueva E.P., Sysolyatin S.V.

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