OLIGOMERIC OESTRADIOL ESTERS: A NEW CLASS OF LONG-ACTING OESTROGENS

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Abstract
Dimeric and trimeric estradiol derivatives were administered as single s.c. injections into ovariectomized rats and the duration of estrogenic effect was determined by daily vaginal smears. These preparations have a very protracted estrogenic effect, and their threshold dose is considerably higher as compared to monomeric estradiol diacetate. A dimeric compound containing 1 free hydroxy group caused a relatively even response in all animals with a linear relationship between the logarithm of dose and the duration of action. The effect was even more protracted when fully esterified dimeric or trimeric estradiol succinates were used, but occurred in a more scattering manner. The duration of effect of 40 .mu.g of the trimeric compound exceeded that of the equivalent dose of estradiol undecylate. The depot-effect of these estradiol derivatives may be due to delayed elimination.

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