Biomedical Chemistry: Research and Methods, 2018, 1(3), e00046
The 40th Anniversary of the Institute of Physiologically Active Compounds of the Russian Academy of Sciences

Pharmacokinetic Studies of New Stimulator of Brain Cognitive Functions OSPL-502

S.A. Pukhov1*, V.V. Grigoriev1, V.I. Kozlovskiy2, A.A. Romanova1, G.D. Shishko1, M.E. Neganova1, S.G. Klochkov1

1Institute of Physiologically Active Compounds of the Russian Academy of Sciences, 1 Severny proezd, Moscow region, Chernogolovka, 142432 Russia;*e-mail: pukhov.sergey@gmail.com
2Branch of Talrose Institute for Energy Problems of Chemical Physics of the Russian Academy of Sciences, 1-10 Acad. Semenov prosp., Chernogolovka, 142432 Russia

Key words: pharmacokinetics; nootropic; HPLC/MS; metabolites

DOI: 10.18097/BMCRM00046

The whole version of this paper is available in Russian.

The main pharmacokinetic parameters of a new stimulator of cognitive brain functions, OSPL – 502 have been determined: area under the concentration-time curve, elimination rate constant, half-elimination period, time to reach the maximum concentration, maximum concentration, volume distribution, total clearance and bioavailability of the dosage form. The main metabolites of the active substance of the dosage form of the new stimulator of cognitive functions OSPL – 502 have been analyzed. The data obtained predict the effects of the drug in humans relevant for further clinical investigation.

CLOSE
Table 1. The results of the OSPL-502 concentration determination in plasma samples taken at appropriate time intervals, with oral (p/o) and intravenous administration (i/v) of the dosage form (mg/kg) in terms of the substance.

CLOSE
Table 2. The dosage form of OSPL-502 pharmacokinetic parameters after oral administration of the dosage form (p/o), calculated as a substance, a dose of 10 mg/kg and after intravenous administration (i/v) of 2 mg/kg of OSPL-502 compound to CD rats.

CLOSE
Table 3. HPLC/ESI-MS data obtained for the compound OSPL-502 and its metabolites after 60-minute incubation with liver homogenate.

ACKNOWLEDGEMENTS

The work was carried out within the framework of the State Proposal 0090-2017-0018.

REFERENCES

  1. Kukes, V.G. (2009). Clinical pharmacokinetics: theoretical, applied and political aspects: Guide. Moscow, GEOTAR-Media Publishing.
  2. Concheiro, M., Gray, T.R., Shakleya, D.M., Huestis, M.A. (2010). High-throughput simultaneous analysis of buprenorphine, methadone, cocaine, opiates, nicotine, and metabolites in oral fluid by liquid chromatography tandem mass spectrometry. Analytical and Bioanalytical Chemistry, 398(2), 915-24. DOI
  3. Borgia – pharmacokinetic parameters calculator. Retrieved August 22, 2018 from http://ilch.vsmu.edu.ua/soft/borgia/borgia.htm
  4. Prasolov, I., Dikunets, M., Sukhanova, I., Sobolevsky, T., Rodchenkov, G. (2012). Study on an in vitro metabolism of novel doping substances to facilitate their detection in human urine. Analitika, 6, 6-14.