Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats

Ksenya A. Lopatina; Olga S. Bryushinina; Roman V. Gurto; Svetlana G. Krylova; Yulia G. Zuzkova; Darya A. Kulagina; Elena A. Safonova; Elena P. Zueva; Sergey V. Sysolyatin

doi:10.17816/RCF17451-56

Reviews on Clinical Pharmacology and Drug Therapy ›› 2019, Vol. 17 ›› Issue (4) : 51 -56. DOI: 10.17816/RCF17451-56

Original study articles

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Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats

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

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

PhD, Senior Researcher of Oncopharmacology Laboratory

PhD, Researcher of Molecular and Clinical Physiology Laboratory

PhD, Leading Researcher of Molecular and Clinical Physiology Laboratory

PhD, MD, Leading Researcher of Oncopharmacology Laboratory

Junior Researcher of Molecular and Clinical Physiology Laboratory

PhD, Researcher of Medical Chemistry Laboratory

PhD, Researcher of Oncopharmacology Laboratory

PhD, MD, Head of Oncopharmacology Laboratory

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

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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.

Keywords

pharmacokinetics / mass spectrometry / thiowurtzine / preclinical studies

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Ksenya A. Lopatina, Olga S. Bryushinina, Roman V. Gurto, Svetlana G. Krylova, Yulia G. Zuzkova, Darya A. Kulagina, Elena A. Safonova, Elena P. Zueva, Sergey V. Sysolyatin. Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats. Reviews on Clinical Pharmacology and Drug Therapy, 2019, 17(4): 51-56 DOI:10.17816/RCF17451-56

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