Metabolism of (-)-6(S)-hydroxy-4(R)-(1-hydroxy-1-methylethyl)-1-cyclohexene-1-ethanol in rat and dog

Abstract

1. The metabolism of a new mucoactive drug, chemically (−)-6(S)-hydroxy-4(R)-(1-hydroxy-1-methylethyl)-1-cyclohexene-1-ethanol (CO/1408), has been studied in rat and dog after a single oral dose; eight metabolites were identified.

2. Oxidation of the primary and secondary alcohol groups, hydroxylation in allylic positions and conjugation with glucuronic acid occurred in both species. Products of oxidation on the double bond have not been identified.

3. Using reversed-phase h.p.l.c. and β-cyclodextrin in the eluent it was found that the glucuronide metabolites varied with species and with the biological fluid examined.