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

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.