Differences in species of iodochlorhydroxyquin absorption, metabolism, and excretion.

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Abstract
The differences in species for absorption, metabolism and excretion of iodochlorhydroxyquin (I) were investigated by the separate determination method of unmetabolized I (free form) and its conjugated metabolites, i.e., glucuronide (I-G) and sulfate (I-S) in urine and bile. As for urinary excretion ratio in rat, the order of the conjugates was I-S>I-G, while in guinea-pig and rabbit, I-G>I-S, and in man, I-G»I-S. Moreover, the order of biliary excretion ratio in guinea-pig was characteristically I-S»I-G differently from rat, in which it was I-G»I-S. In all cases, unmetabolized I was of trace and neglected. In addition to urinary and biliary excretion, as to blood concentration after oral administration, the complexed absorbability of I was shown. In small animals (rat and guinea-pig), the order of the concentration of unmetabolized I and the conjugates was I-G and I-S> unmetabolized I, but in beagle which was sensitive to the toxicity of I, unmetabolized I>I-G and I-S. Furthermore, the biological stability of the conjugates of I was studied and the conversion of I-G⇋I-S was found to occur in rat. This result shows that the conjugates are hydrolyzed and reconjugation to glucuronide or sulfate occurs in rat.