Изучение фармакокинетики нового радиофармацевтического препарата на основе меченной технецием-99m производной глюкозы

Abstract

Purpose: To study the features of the distribution and removal of a new radiopharmaceutical (RPH) on the basis of a labeled 99mTc glucose derivative for radionuclide diagnostics of oncological diseases in the body of experimental animals.
 Material and methods: The main stage of the study was performed on 65 mature conventional outbred white rats and 9 rabbits of the Soviet Chinchilla breed. To study the dynamics of changes in the concentration of the studied RPH in the blood plasma and its distribution in the main organs and tissues, as well as to study the metabolic features of the drug and its excretion, the RPH studied was administered intravenously, once in activity of 20 MBq. Multiple introduction of the RPH was performed in order to study the cumulative properties of the study drug, and to elucidate the possibilities of predicting the cumulation processes from the data obtained with a single administration of RPH. For this purpose, intravenous RPH was administered at the same time 1 time / day for 5 days, at a dose of 20 MBq. To confirm the theory of linearity of the pharmacokinetics of the RFP studied, three groups of laboratory animals received the drug in three activity levels – 10, 20 and 40 MBq were used. After euthanasia, the animals were autopsied and removed the necessary organs and tissues. The prepared and washed organs were placed in tubes for further radiometry in order to study the concentrations of the RPH in the bioassay.
 Results: It has been established that the RPH being studied practically does not accumulate in the main organs and tissues, accumulating mainly in the kidneys and bladder. The main organs of elimination of the test drug are the kidneys, and the main excreta are urine. The half-life of the drug from the blood was 10 minutes. Pharmacokinetics of the drug is linear and does not depend on the administered activity, and the drug itself does not possess cumulative properties.
 Conclusion: A study of the pharmacokinetics of the RPH 99mTc-1-Thio-D-glucose showed that the preparation possesses optimal properties for the diagnostic agent. The drug stably does not accumulate in the main organs and tissues, which allows it to be reused, for example at the stages of dynamic observation of cancer patients.