The Pharmacokinetic Study on the Fate of 8-Hydroxyquinoline in Rat

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The fate of 8-hydroxyquinoline (Oxine) (OX) in rats, which is the parent compound of iodochlorhydroxyquin (chinoform, 5-chloro-8-hydroxy-7-iodoquinoline) (I) suspected to cause SMON, was investigated. Although both OX and I are metabolized to glucuronide and sulfate, the differences obtained from the excretion data are as follows : 1) After the intravenous administration of OX, glucuronide was more excreted (about 65% of dose) than sulfate (about 25% of dose) in urine in contrast to the case of I. 2) In bile, only 10% as glucuronide was excreted. The difference from I was considered due to the difference of molecular weight caused by the halogen substitution. 3) Both OX glucuro nide and sulfate were stable in the body, and it was excreted as the administered form without exchanging to the another form after the intravenous administration of each conjugate. Accordingly the fate of these compounds in the body was shown to be well influenced by the halogenation. Furthermore, the blood concentration of free and conjugated OX, which was determined with synthesized ^<14>C-OX, was analyzed by the application of numerical deconvolution technique to the precursor-successor relationship between OX and each conjugate. Consequently, the usefulness of the technique was demonstrated and some pharmacokinetic features for OX were obtained.
公益社団法人日本薬学会の論文
1977-07-25