This invention relates to glycoesters of estradiol and estriol, processes for their preparation, and aqueous crystalline suspensions of these esters.
The natural estrogenic hormones estradiol and estriol have the disadvantage when used for medical purposes of poor solubility and rapid metabolization.
Esterification of the natural estrogens with longerchain carboxylic acids yields estrogenically active agents that can be administered as oily solutions and exhibit long-term activity.
For example, estradiol 17-valerate, 17-enanthate, 17-undecylate, 17-cipionate, and 3-benzoate are utilized in the form of oily solutions; furthermore, use is made in medicine of a water-soluble succinic ester of estriol, namely, sodium estriol 16,17-dihemisuccinate.
Thus far, aqueous crystalline suspensions of estradiol esters and estriol esters have not been known.
USPTO Backgrounds
USPTO Backgrounds