Studies on Absorption, Biotransformation and Excretion of Drug. V. Metabolism of Pentazocine in the Rat

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The metabolism of pentazocine was studied in the rat following oral administration. After the enzymatic hydrolysis of the urine, eight metabolites including unchanged pentazocine were extracted with organic solvents and XAD-2 column, and isolated by preparative thin-layer chromatography. These metabolites were characterized by gas-liquid chromatography, and infrared, nuclear magnetic resonance and mass spectrometries. Unchanged pentazocine and three metabolites, 1,2,3,4,5,6-hexahydro-8-hydroxy-α, 6 (eq), 11 (ax)-trimethyl-2,6-methano-3-benzazocine-3-trans-2-buten-1-ol (trans-OH), 1,2,3,4,5,6-hexahydro-8-hydroxy-α, 6 (eq), 11 (ax)-trimethyl-2,6-methano-3-benzazocine-3-crotonic acid (trans-COOH) and norpentazocine were identified by comparison with corresponding authentic samples, and four other metabolites were characterized to be 1,2,3,4,5,6-hexahydro-8-hydroxy-α, 6 (eq), 11 (ax)-trimethyl-2,6-methano-3-benzazocine-3-cis-2-buten-1-ol (cis-OH), 9-methoxy pentazocine (or its 8-methoxyl-9-hydroxy isomer) and 8,9 (or 9,8)-methoxy hydroxy metabolites of cis-OH and trans-OH by spectral and chromatographic data. During 24 hr after oral administration, unchanged pentazocine was mainly excreted in the urine as the nonconjugated and conjugated forms. The amount of the other metabolites was found to be small.
社団法人日本薬学会の論文
1979-03-25