Transdermal formulations, methods and devices
AssigneeAlza Corporation
InventorsRobert M. Gale, Diane E. Nedberge, Linda E. Atkinson
Life of this patent
Estimating the term…
Abstract
The present invention provides compositions and methods for the transdermal administration of a therapeutically effective amount of a synthetic 19-nor-progesterone (ST-1435) and an estrogen, in combination, together with, optionally, a suitable permeation enhancer.
Claims20
A composition of matter for the transdermal administration of a drug formulation comprised of an estrogen and ST-1435, the composition comprising, in combination, an amount of the drug formulation to deliver at least 10 .mu.g/day of estrogen and at least 20 .mu.g/day of ST-1435 and a skin permeation-enhancing amount of a suitable permeation enhancer, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof.
A method for the transdermal administration of a drug formulation comprised of an estrogen and ST-1435, which method comprises:
- (a) administering the drug formulation at a rate of at least 10 .mu.g/day of estrogen and at least 20 .mu.g/day of ST-1435 to an area of skin, the area being of from about 1 cm.sup.2 to about 50 cm.sup.2 ;
- and
- (b) simultaneously administering a suitable permeation enhancer to the area of skin at rates which are sufficient to substantially increase the permeability of the area to the drug formulation, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof.
A method for providing hormone replacement therapy to a woman, which method comprises:
- (a) administering a drug formulation comprised of 17-.beta.-estradiol and ST-1435 at a rate of at least 10 .mu.g/day of 17-.beta.-estradiol and at least 20 .mu.g/day of ST-1435 to an area of the woman's skin, the area being of from about 1 cm.sup.2 to about 50 cm.sup.2 ;
- (b) simultaneously administering a suitable permeation enhancer to the area of skin at rates which are sufficient to substantially increase the permeability of the area to the drug formulation, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof.
A method for providing hormone replacement therapy to a woman, which method comprises the steps of:
- (1) administering for a period of two weeks to an area of the woman's skin, the area being of from about 1 cm.sup.2 to about 50 cm.sup.2 :
- (a) a drug formulation comprised of 17-.beta.-estradiol and ST-1435 at a rate of at least 10 .mu.g/day of 17-.beta.-estradiol and at least 20 .mu.g/day of ST-1435;
- and
- (b) simultaneously, a suitable permeation enhancer to the area of skin at rates which are sufficient to substantially increase the permeability of the area to the drug formulation, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof;
- followed by
- (2) administering for a period of two weeks to an area of the woman's skin, the area being of from about 1 cm.sup.2 to about 50 cm.sup.2 :
- (a) a drug formulation consisting essentially of 17-.beta.-estradiol at a rate of at least 10 .mu.g/day;
- and
- (b) simultaneously, a suitable permeation enhancer to the area of skin at rates which are sufficient to substantially increase the permeability of the area to the drug formulation, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof;
- steps (1) and (2) being repeated as necessary to provide hormone replacement therapy.
A device for the transdermal administration of a drug formulation comprised of an estrogen and ST-1435, which device is of a size of from about 1 cm.sup.2 to about 50 cm.sup.2 and comprises:
- (a) a reservoir comprising a matrix containing a therapeutically effective amount of the drug formulation to deliver at least 10 .mu.g/day of estrogen and at least 20 .mu.g/day of ST-1435 and a skin permeation-enhancing amount of a suitable permeation enhancer, the permeation enhancer being selected from C.sub.2-4 alcohols, polyethylene glycol monolaurate, polyethylene glycol-3-lauramide, dimethyl lauramide, lauric diethanolamide, lauryl lactate, esters of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, triglycerides of fatty acids, acetylated monoglycerides, and lactylated monoglycerides, and mixtures thereof;
- (b) a backing on the skin-distal surface of the reservoir;
- and
- (c) means for maintaining the reservoir in estrogen, ST-1435 and permeation enhancer-transmitting relation with the skin.
Dependencies are inferred from the claim text.