Цель работы состояла в изучении путей экскреции и их эффективности после однократного интрагастрального введения пропоксазепама и на фоне курсового применения его нерадиоактивного аналога. Параметры экскреции 214С-7-бром-5-(о-хлорфенил)-3-пропокси-1,2-дигидро-3Н-1,4-бенздиазепин-2-она (пропоксазепам) оценивали после его однократного введения и на фоне предварительного курсового (7 сут., 35,2 мг/кг) применения его нерадиоактивного аналога методом жидкостной сцинтилляционной фотометрии. Идентификацию метаболитов осуществляли на ВЭЖХ-масс-хроматографе 1260 Infinity с детектором 6530 Accurate Mass Q-TOF (Agilent
Technologies, США).
The aim of the work was studying of excretion ways and their effectiveness after oral propoxazepam
administration single and after its non-radioactive analog administration course. Excretion parameters
of 214C-7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-dihydro-3H-1,4-benzodiazepine-2-one (propoxazepam)
were determined after single administration and after previous course (7 days, 35.2 mg/kg)
administration of non-radioactive analog by liquid scintillation photometry. Metabolites identification
was performed on a HPLC-mass chromatograph with 1260 Infinity 6530 Accurate Mass Q-TOF detector
(Agilent Technologies, USA). It was found that after a single administration propoxazepam is slowly
excreted from the body (kel=(0.019±0.050) h-1), mainly with the urine ((67.5±18.5)% of the administered
dose). Long term (7 days) propoxazepam administration did not change its excretion parameters
(kel after previous course administration was (0.016±0.007) h-1), and has little effect on the redistribution
of radioactive material quantity excreted. During propoxazepam metabolism in mice hydroxylation
at aromatic ring with further methylation as well as 3-hydroxyderivative formation occurs, which
proves the partial alcoxypart elimination from the parent molecule
