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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
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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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© National Academy of Sciences of Ukraine, Bogomoletz Institute of Physiology, 2014-2024.
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