FATE OF OESTRIOL-16,17 DIHEMISUCCINATE AFTER ORAL ADMINISTRATION TO RATS

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Abstract
After oral administration to rats estriol-16, 17 dihemisuccinate is almost exclusively resorbed in the unchanged form and at a slower rate than estriol itself. Via the portal vein it is transported to the liver and the peripheral circulation. In the liver, hydrolysis of the ester takes place rapidly and the free estriol formed also enters the blood. In the blood the half life time of estriol-16,17 dihemisuccinate is 7.6 minutes and that of estriol 10.3 minutes. Elimination from the body occurs via the bile in which conjugates were found similar to those occurring after administration of estriol. The ways in which estriol dihemisuccinate is resorbed, distributed and eliminated differ from those of estriol itself. This might well be a significant factor in its pharmacological and clinical effectiveness.

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