US4816258A — Transdermal contraceptive formulations

Claim 1

Independent Claim 34 words

A composition of matter for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel, comprising a matrix containing said drug formulation and a skin permeation enhancing amount of glycerol monooleate.

Claim 2

Dependent Claim 34 words

A composition of matter for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel, comprising a matrix containing said drug formulation and a skin permeation enhancing amount of glycerol monooleate.

Claim 3

Dependent Claim 23 words

The composition of claim 1 wherein said ethinyl estradiol is present in an amount in excess of its saturation concentration in the matrix.

Claim 4

Dependent Claim 22 words

The composition of claim 1 wherein said levonorgestrel is present in an amount in excess of its saturation concentration in the matrix.

Claim 5

Dependent Claim 13 words

The composition of claim 1 wherein said matrix comprises an ethylene vinylacetate co-polymer.

Claim 6

Dependent Claim 16 words

The composition of claim 4 wherein said ethylene vinylacetate co-polymer comprises about 28 to 60% vinylacetate.

Claim 7

Dependent Claim 14 words

The composition of claim 5 wherein said ethylene vinylacetate co-polymer comprises about 40% vinylacetate.

Claim 8

Dependent Claim 59 words

A transdermal therapeutic system comprising a reservoir containing a drug formulation comprised of ethinyl estradiol and levonorgestrel, and a skin permeation enhancing amount of glycerol monooleate, in combination with: an occlusive backing behind the skin distal surface of said reservoir composition; and means for maintaining said reservoir composition in drug formulation and glycerol monooleate transferring relationship to human skin.

Claim 9

Dependent Claim 59 words

A transdermal therapeutic system comprising a reservoir containing a drug formulation comprised of ethinyl estradiol and levonorgestrel, and a skin permeation enhancing amount of glycerol monooleate, in combination with: an occlusive backing behind the skin distal surface of said reservoir composition; and means for maintaining said reservoir composition in drug formulation and glycerol monooleate transferring relationship to human skin.

Claim 10

Independent Claim 41 words

A method for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel, which comprises placing said drug formulation in drug transmitting relationship to the skin in the presence of a drug permeation enhancing amount of glycerol monooleate.

Claim 11

Independent Claim 41 words

A method for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel, which comprises placing said drug formulation in drug transmitting relationship to the skin in the presence of a drug permeation enhancing amount of glycerol monooleate.

Claim 12

Dependent Claim 13 words

The method of claim 8 wherein said ethinyl estradiol is at unit activity.

Claim 13

Dependent Claim 12 words

The method of claim 8 wherein said levonorgestrel is at unit activity.

Claim 14

Dependent Claim 28 words

The method of claim 8 wherein said ethinyl estradiol is delivered through the skin at a rate of at least 15 μg/day for an extended period of time.

Claim 15

Dependent Claim 27 words

The method of claim 8 wherein said levonorgestrel is delivered through the skin at a rate of at least 50 μg/day for an extended period of time.

Claim 16

Dependent Claim 73 words

A medical device for the transdermal delivery of a drug formulation comprised of ethinyl estradiol and levonorgestrel, comprising in combination: a reservoir means containing a skin permeable formulation containing said drug formulation; an occlusive backing behind the skin distal surface of said reservoir means and extending beyond the periphery of said reservoir means; and an adhesive overlay disposed on the skin distal surface of said occlusive backing and extending beyond the periphery thereof.

Claim 17

Dependent Claim 73 words

A medical device for the transdermal delivery of a drug formulation comprised of ethinyl estradiol and levonorgestrel, comprising in combination: a reservoir means containing a skin permeable formulation containing said drug formulation; an occlusive backing behind the skin distal surface of said reservoir means and extending beyond the periphery of said reservoir means; and an adhesive overlay disposed on the skin distal surface of said occlusive backing and extending beyond the periphery thereof.

Claim 18

Dependent Claim 113 words

A medical device for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel through intact skin for an extended period of time at a therapeutic rate of at least 15 μg/day of ethinyl estradiol and at least 50 μg/day of levonorgestrel, which comprises: a unit activity reservoir of a skin permeable form of said formulation, said reservoir comprising a carrier having said formulation substantially uniformly distributed there through at a concentration above saturation; a reservoir of a skin permeation enhancer for said material; and means for maintaining said formulation reservoir and said permeation enhancer reservoir in formulation and permeation enhancer transferring relationship to the same area of intact skin.

Claim 19

Dependent Claim 113 words

A medical device for the transdermal administration of a drug formulation comprised of ethinyl estradiol and levonorgestrel through intact skin for an extended period of time at a therapeutic rate of at least 15 μg/day of ethinyl estradiol and at least 50 μg/day of levonorgestrel, which comprises: a unit activity reservoir of a skin permeable form of said formulation, said reservoir comprising a carrier having said formulation substantially uniformly distributed there through at a concentration above saturation; a reservoir of a skin permeation enhancer for said material; and means for maintaining said formulation reservoir and said permeation enhancer reservoir in formulation and permeation enhancer transferring relationship to the same area of intact skin.

Claim 20

Dependent Claim 17 words

The medical device of claim 14 wherein said permeation enhancer reservoir is combined with said formulation reservoir.

Claim 21

Dependent Claim 13 words

The medical device of claim 14 wherein said permeation enhancer is glycerol monooleate.

Claim 22

Dependent Claim 38 words

The medical device of claim 14, further comprising a means for controlling the release of permeation enhancer from said enhancer reservoir to said formulation reservoir, said formulation reservoir being disposed between said rate controlling means and the skin.

Claim 23

Dependent Claim 45 words

The medical device of claim 14, wherein said permeation enhancer is glycerol monooleate and said formulation reservoir contains said formulation at a concentration above saturation in an amount sufficient to maintain the concentration of said formulation at least at the saturation level throughout said period.

Claim 24

Dependent Claim 19 words

The medical device of claim 14, further comprising an impermeable backing on the skin distal side of said reservoir.

Claim 25

Independent Claim 120 words

A method for the transdermal delivery of a drug formulation comprised of ethinyl estradiol and levonorgestrel at a therapeutic rate of at least 15 μg/day of ethinyl estradiol and at least 50 μg/day of levonorgestrel, for an extended period of time, which comprises: contacting an area of intact skin with a source of a skin permeable form of said formulation at unit activity and a skin permeation enhancer for said formulation at a permeation enhancing concentration; maintaining said source in formulation and permeation enhancer transmitting contact with the skin for said extended period of time; and maintaining the source of said formulation at unit activity and said permeation enhancer at a permeation enhancing concentration for said extended period of time.

Claim 26

Independent Claim 120 words

A method for the transdermal delivery of a drug formulation comprised of ethinyl estradiol and levonorgestrel at a therapeutic rate of at least 15 μg/day of ethinyl estradiol and at least 50 μg/day of levonorgestrel, for an extended period of time, which comprises: contacting an area of intact skin with a source of a skin permeable form of said formulation at unit activity and a skin permeation enhancer for said formulation at a permeation enhancing concentration; maintaining said source in formulation and permeation enhancer transmitting contact with the skin for said extended period of time; and maintaining the source of said formulation at unit activity and said permeation enhancer at a permeation enhancing concentration for said extended period of time.

Claim 27

Independent Claim 36 words

A method for producing a contraceptive effect in the human female which comprises transdermally co-administering ethinyl estradiol and levonorgestrel at contraceptively effective rates and maintaining said co-administration continuously throughout the period for which contraception is required.

Claim 28

Independent Claim 36 words

A method for producing a contraceptive effect in the human female which comprises transdermally co-administering ethinyl estradiol and levonorgestrel at contraceptively effective rates and maintaining said co-administration continuously throughout the period for which contraception is required.

Claim 29

Dependent Claim 30 words

The method of claim 21 wherein said maintenance comprises placing a transdermally therapeutic system in ethinyl estradiol and levonorgestrel transmitting relationship to human skin for an extended period of time.

Claim 30

Dependent Claim 18 words

The method of claim 22 wherein said extended period of time is the effective life of said system.

Claim 31

Dependent Claim 14 words

The method of claim 23 wherein said effective life is up to 7 days.

Claim 32

Dependent Claim 23 words

The method of claim 22 wherein said maintenance further comprises replacing said system with a second system after said extended period of time.

Claim 33

Dependent Claim 20 words

The method of claim 25 wherein said replacement is carried on repeatedly throughout the period for which contraception is desired.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1992-03-27	1992-09-26	1993-03-28	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1996-03-27	1996-09-26	1997-03-28	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	2000-03-27	2000-09-26	2001-03-28	$7700.00	Window Closed / Lapsed

Transdermal contraceptive formulations

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