Some studies on the pharmacological biochemistry of carbenoxolone.

Carbenoxolone has been labelled with [14]C and [3]H. [[14]C]Carbenoxolone administered as a positioned-release capsule to duodenal ulcer patients was shown to be readily absorbed. The fate of [[14]C]- and [[3]H]carbenoxolone administered orally to human volunteers has been investigated. Most of the dose was recovered as carbenoxolone in the faeces, although a portion ( 10[7]) for carbenoxolone and was found to be the principal binding protein in human plasma, although binding to globulins also occurred; carbenoxolone also induced a conformational change in the albumin. The distribution of [[14]C]carbenoxolone in the rat showed that it was confined largely to the gastrointestinal tract, liver and plasma. Pretreatment of rats with carbenoxolone had no significant effect on various hepatic microsomal enzymes concerned with the metabolism of drugs and steroids. Neither did such pretreatment influence the biliary and urinary excretion of [[3]H] cortisol and its metabolites