Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats
- Authors: Lopatina K.A.1, Bryushinina O.S.1, Gurto R.V.1, Krylova S.G.1, Zuzkova Y.G.1, Kulagina D.A.2, Safonova E.A.1, Zueva E.P.1, Sysolyatin S.V.2
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Affiliations:
- 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
- Issue: Vol 17, No 4 (2019)
- Pages: 51-56
- Section: Original study articles
- URL: https://journals.rcsi.science/RCF/article/view/13498
- DOI: https://doi.org/10.17816/RCF17451-56
- ID: 13498
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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.
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##article.viewOnOriginalSite##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, TomskOlga 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, TomskRoman 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, TomskSvetlana 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, TomskYulia 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, TomskDarya 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, BiyskElena 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, TomskElena 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, TomskSergey 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, BiyskReferences
- Мирошниченко И.И. Основы фармакокинетики. – М.: ГЭОТАР-МЕД, 2002. – 192 с. [Miroshnichenko II. Osnovy farmakokinetiki. Moscow: GEOTAR-MED; 2002. 192 p. (In Russ.)]
- Руководство по проведению доклинических исследований лекарственных средств / Под ред. А.Н. Миронова. Ч. 1. – М.: Гриф и К, 2013. – 944 с. [Rukovodstvo po provedeniyu doklinicheskikh issledovaniy lekarstvennykh sredstv. Ed. by A.N. Mironov. Part 1. Moscow: Grief and K; 2013. 944 p. (In Russ.)]
- Сергиенко В.И., Джеллифф Р., Бондарева И.Б. Прикладная фармакокинетика: основные положения и клиническое применение. – М.: Издательство РАМН, 2003. – 208 с. [Sergienko VI, Jellyff R, Bondareva IB. Prikladnaya farmakokinetika: osnovnye polozheniya i klinicheskoe primenenie. Moscow: Izdatel’stvo RAMN; 2003. 208 p. (In Russ.)]
- Каркищенко Н.Н., Хоронько В.В., Сергеева С.А., Каркищенко В.Н. Фармакокинетика. – Ростов-на-Дону: Феникс, 2001. – 384 с. [Karkishchenko NN, Khoron’ko VV, Sergeeva SA, Karkishchenko VN. Farmakokinetika. Rostov-na-Donu: Phoenix; 2001. 384 p. (In Russ.)]
- Лебедев А.Т. Масс-спектрометрия в органической химии. – М.: БИНОМ. Лаборатория знаний, 2003. – 493 с. [Lebedev AT. Mass-spektrometriya v organicheskoy khimii. Moscow: BINOM. Laboratoriya znaniy; 2003. 493 p. (In Russ.)]
- Niessen W.M.A. MS–MS and MSn. Encyclopedia of Spectroscopy and Spectrometry. 3rd ed. Ed. by J.C. Lindon, G.E. Tranter, D. Koppenaal. Academic Press; 2016. P. 936-941.
