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ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2017; 63(3): 40-48


N.Ya. Golovenko, V.B. Larionov, I.P. Valivodz

    A.V. Bogatskiy Physical-Chemical Institute of NAS of Ukraine, Odessa


The aim of this work was determination of the absorption pharmacokinetic parameters (gastrointestinal tract - blood - organs/tissue) for 14C-propoxazepam after its intragastric administration to mice during transit along the gastrointestinal tract and entering to systemic circulation. Calculated lipophilicity (Log P 4,31 ± 0.64) and ionization constants (pKa1 and pKa2 10.65 ± 0.7 and 1.2 ± 0.5, respectively) suggest that this molecule exists as non-ionized under physiological conditions. 14C-propoxazepam evacuation from stomach (intragastral administration, 10 mg/kg) described as two-phase process (first phase with kel = 0,68 h-1, the second of kel = 0,0094 h-1). Total dose quantity, absorbed during experiment, was ~ 80%, with absorption constant of 0,371 ± 0,098 h-1. Similar values of distribution volume (743 ± 195 sm3/kg and 1090 ± 421 g/kg for blood and brain respectively) let suggest intensive mass transfer.

Keywords: 14C-propoxazepam; intragastral administration; absorption; distribution; mass transfer.


  1. Golovenko N Ya. Physical-chemical pharmacology. Odessa 2015; Astroprint 2004; Zaporozhye State Medical University. [Russian].
  3. Gabrielsson J, Weiner D. Pharmacokinetic and Pharmacodynamic Data Analysis, Concepts and Applications. 4th ed. Sweden: Swed Pharmaceut Press; 2007. PubMedCentral
  5. Balant L, Gex-Fabry M. Review physiological pharmacokinetic modelling. Xenobiotica. 1990; 20(11):1241–57. CrossRef PubMed
  7. Beregova T V, Falalyeyeva T M. The role of short chain fatty acids and lactic acid in regulation of gastric secretion. Physiol Zh. 2013; 52(3): 41–50. [Ukrainian].
  9. Spivak M Ya, Lazarenko L M, Falalyeyeva T M, Virchenko OV, Neporada KS. Prophylactic influence of probiotoc strains bifidobacterium animals VKL and VKB on stressinduced lesions in the gastric mucosa of rats. Physiol Zh. 2013; 59 (2): 23–30. [Ukrainian].
  11. Pavlovsky V, Kabanova T, Khalimova E, Andronati S. Analgesic and anti-inflammatory properties of the novel 3–alkoxy-1,2-dihydro-3h-1,4-benzodiazepin-2- ones. Odesa National University Herald Chemistry. 2014; 18(3(47)):28. CrossRef  
  12. Golovenko N, Zin'kovskii V. Determination of tranquilizers of the 1,4-benzodiazepine series and their metabolites in biological media. Pharm Chem J, 1978; 12(1):1–11. CrossRef  
  13. V.I. Pavlovsky, V.B. Larionov, I.P. Valivodz' Synthesis of 2[14S]-3-propoxy-1.4-benzdiazepine-2-one for pharmacokinetic research. Ukrainica Bioorganica Acta, 2015; 2:26–35.
  15. Johnson L. Physiology of the gastrointestinal tract. 1st ed., Academic Press, 2012, 2308 p.
  16.   Bogatskiy A, Andronati S, Golovenko N. 1st ed. Kiev: Naykova Dumka; 1980. 281 p. [Ukrainian]  
  17. Ahmed S, Siddiqi Z. Antiepileptic drugs and liver disease. Seizure. 2006;15(3):156–64. CrossRef PubMed
  19. Berezhkovskiy L. A Valid Equation for the Well-Stirred Perfusion Limited Physiologically Based Pharmacokinetic Model that Consistently Accounts for the Blood–Tissue Drug Distribution in the Organ and the Corresponding Valid Equation for the Steady State Volume of Distribution. J Pharm Sci. 2010;99(1):475–85. CrossRef PubMed
  21. Golovenko N, Larionov V. Pharmacodynamical and Neuroreceptor Analysis of the Permeability of the Blood- Brain Barrier for Derivatives of 1,4-Benzodiazepine. Neurophysiology. 2014;46(3):199-205. CrossRef  

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