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ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

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


ABSORPTION AND DISTRIBUTION OF 14C-PROPOXASEPAM AFTER ITS INTRAGASTRAL ADMINISTRATION

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

    A.V. Bogatskiy Physical-Chemical Institute of NAS of Ukraine, Odessa
DOI: https://doi.org/10.15407/fz63.03.040

Abstract

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.

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