Transdermal delivery of estradiol and process for manufacturing said device
AssigneeBeta Pharmaceuticals Co.
InventorsFrancisco Jose Evaristo Stefano, Jose Adrian Nowogrodski, Dario Norberto Ramon Carrara
Life of this patent
Estimating the term…
Abstract
The present invention relates to a transdermal delivery device for estradiol where the metabolic degradation of estradiol to estrone during permeation is inhibited by another substance in the transdermal delivery device. The transdermal device also includes a compound for enhancing the rate of estradiol permeation. The transdermal delivery device containing the inhibitor and enhancer can also be used to simultaneously deliver both estradiol and a progestin at therapeutic rates.
Claims29
A transdermal delivery device for estradiol including a flexible substrate and a releasable protective film, the protected surface of said flexible substrate being at least partly covered with a coating layer containing:
- (a) a dermatologically or pharmacologically acceptable pressure sensitive adhesive material;
- (b) estradiol homogeneously distributed in said coating layer as a pharmacologically active ingredient;
- (c) one compound as an inhibitor of metabolic oxidation of estradiol to estrone, said compound selected from the group consisting of glycerin and (C.sub.3 -C.sub.6) alkylene 1,2-diols;
- (d) a second compound which enhances the rate of estradiol permeation, said second compound selected from the group consisting of unsaturated (C.sub.12 -C.sub.18) fatty acids;
- and
- (e) a pharmacologically active progestin.
A transdermal delivery device for estradiol comprising a flexible substrate and a releasable protective film, the protective surface of said flexible substrate being at least partly covered with a coating layer containing:
- a) a dermatologically or pharmacologically acceptable pressure sensitive adhesive material for securing the device to the skin;
- b) estradiol homogeneously distributed in said coating layer as a pharmacologically active ingredient, said estradiol comprising from 1 to 5 wt. %;
- c) one compound as an inhibitor of metabolic oxidation of estradiol to estrone, said compound selected from the group consisting of glycerin and (C.sub.3 -C.sub.6) alkylene 1,2 diols in a concentration from 0.25 to 30 wt %;
- d) a second compound which enhances the rate of estradiol permeation, said second compound selected from unsaturated (C.sub.12 -C.sub.18) fatty acids in a concentration from 1 to 20 wt %;
- and
- (e) a pharmacologically active progestin in a concentration from 2 to 10 wt %, said weight percentages being based on total weight of said coating layer.
A process for manufacturing a transdermal delivery device for estradiol, comprising the steps of providing a coating layer on at least part of one surface of a flexible substrate, said coating layer including:
- (a) a dermatologically or pharmacologically acceptable pressure sensitive adhesive material for securing the device to the epidermis;
- (b) estradiol homogeneously distributed in said coating layer as a pharmacologically active ingredient;
- (c) one compound as an inhibitor of inhibitor of enzymatic oxidation of estradiol to estrone, said compound being selected from the group consisting of glycerin and (C.sub.3 -C.sub.6) alkylene 1,2 diols in a concentration from 0.25 to 30 wt %;
- (d) a second compound which enhances the rate of estradiol permeation, said second compound selected from unsaturated (C.sub.12 -C.sub.18) fatty acids in a concentration from 1 to 20 wt %;
- and
- (e) a pharmacologically active progestin in a concentration from 2-10 wt %, said weight percentages being based on total weight of said coating layer;
- and providing a releasable protective layer which, in the finished device, lies on the opposite side of the coating layer to the flexible substrate.
Dependencies are inferred from the claim text.