scholarly journals Some pharmacokinetics aspects of new analgetics from hexaazaisiowuritsitane class in rats

2020 ◽  
Vol 17 (4) ◽  
pp. 51-56 ◽  
Author(s):  
Ksenya A. Lopatina ◽  
Olga S. Bryushinina ◽  
Roman V. Gurto ◽  
Svetlana G. Krylova ◽  
Yulia G. Zuzkova ◽  
...  

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.

2021 ◽  
Vol 15 (4) ◽  
pp. 43-50
Author(s):  
A. I. Varlamova ◽  
V. E. Abramov ◽  
I. A. Arkhipov

The purpose of the research is to develop a methodology for the quantitative determination of fenbendazole (FBZ) and its metabolites in organs and tissues of sheep by high performance liquid chromatography tandem mass-spectrometry (HPLC-MS/MS).Materials and methods. The method for determining of FBZ and its metabolites after the administration of the supramolecular complex of fenbendazole was validated in accordance with international guidelines for the following indicators: linearity, recovery, specificity, precision, accuracy, limits of quantitative and qualitative determination.Results and discussion. The method of quantitative analysis of FBZ and its metabolites sulfone and sulfoxide in the body of sheep after the administration of the supramolecular complex has been adapted. The proposed method has a linear relationship (R > 0.99) in the range of 5–1000 ng / g and has shown a good reproducibility and accuracy.


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