US4788062A
Expired / Lapsed
US
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Transdermal administration of progesterone, estradiol esters, and mixtures thereof
Assignee: Alza Corp
•
Filing: 1987-02-26
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Granted: 1988-11-29
•
Expires: 2007-02-26
Abstract
Abstract A transdermal delivery system for the administering of progesterone and an estradiol ester alone or in combination utilizing a polymer matrix having the drug(s) along with a permeation enhancer dispersed throughout.
Inventors
- 👤 Robert M. Gale
- 👤 David J. Enscore
- 👤 Diane E. Nedberge
- 👤 Melinda Nelson
- 👤 Yu-Ling Cheng
- 👤 Shari B. Libicki
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:03
CPC Classifications
A; A61; A61M; A61M37/00; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7038; A61K9/7046; A61K9/7053; A61K31/00; A61K31/56; A61K31/565; A61K31/57; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K47/26; A61K9/0012; A61K9/0014; A61K9/7076; A61K9/7084
Claims Analysis
Total Claims: 47
Claim 1
Independent Claim
51 words
A composition of matter for the transdermal administration of a drug selected from the group consisting of progesterone, an estradiol ester and mixtures thereof, comprising said drug and a skin permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, and neopentyl glycol dicaprate.
Claim 2
Dependent Claim
51 words
A composition of matter for the transdermal administration of a drug selected from the group consisting of progesterone, an estradiol ester and mixtures thereof, comprising said drug and a skin permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, and neopentyl glycol dicaprate.
Claim 3
Dependent Claim
22 words
The composition of claim 1 wherein said drug is present in an amount in excess of its saturation concentration in said carrier.
Claim 4
Dependent Claim
30 words
The composition of claim 1 wherein said permeation enhancer is present at a predetermined concentration such that it has an activity within the range of about 0.1 to unit activity.
Claim 5
Dependent Claim
10 words
The composition of claim 1 wherein said drug is progesterone.
Claim 6
Dependent Claim
12 words
The composition of claim 1 wherein said drug is an estradiol ester.
Claim 7
Dependent Claim
17 words
The composition of claim 1 wherein said drug is a combination of progesterone and an estradiol ester.
Claim 8
Dependent Claim
10 words
The composition of claim 1 which further comprises an adhesive.
Claim 9
Dependent Claim
39 words
The composition of claim 7 wherein said adhesive is an adhesive mixture forming said matrix, selected from the group consisting of an elastomer and tackifier mix, and a high molecular weight polymer, low molecular weight polymer and oil mix.
Claim 10
Dependent Claim
13 words
The composition of claim 7 wherein said adhesive is an in-line contact adhesive.
Claim 11
Dependent Claim
15 words
The composition of claim 9 wherein said adhesive is further comprised of a permeation enhancer.
Claim 12
Dependent Claim
18 words
The composition of claim 9 wherein said adhesive controls the rate of release of drug from said composition.
Claim 13
Dependent Claim
19 words
The composition of claim 9 wherein said adhesive controls the rate of release of permeation enhancer from said composition.
Claim 14
Independent Claim
63 words
A method for the transdermal administration of a drug selected from the group consisting of progesterone, an estradiol ester and mixtures thereof which comprises placing a matrix containing said drug in drug transmitting relationship to the skin in the presence of a permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, and neopentyl glycol dicaprate.
Claim 15
Independent Claim
63 words
A method for the transdermal administration of a drug selected from the group consisting of progesterone, an estradiol ester and mixtures thereof which comprises placing a matrix containing said drug in drug transmitting relationship to the skin in the presence of a permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, and neopentyl glycol dicaprate.
Claim 16
Dependent Claim
12 words
The method of claim 13 wherein said drug is at unit activity.
Claim 17
Dependent Claim
21 words
The method of claim 13 wherein said permeation enhancer has an activity within the range of about 0.1 to unit activity.
Claim 18
Dependent Claim
10 words
The method of claim 13 wherein said drug is progesterone.
Claim 19
Dependent Claim
22 words
The method of claim 16 wherein said progesterone is delivered through the skin at a rate of up to about 24 mg/day.
Claim 20
Dependent Claim
12 words
The method of claim 13 wherein said drug is an estradiol ester.
Claim 21
Dependent Claim
21 words
The method of claim 18 wherein said estradiol ester is delivered through the skin at a rate of about 25-250 μg/day.
Claim 22
Dependent Claim
21 words
The method of claim 18 wherein said estradiol ester is delivered through the skin at a rate of about 50-150 μg/day.
Claim 23
Dependent Claim
17 words
The method of claim 13 wherein said drug is a combination of progesterone and an estradiol ester.
Claim 24
Dependent Claim
36 words
The method of claim 21 wherein said progesterone is delivered through the skin at a rate of about 24 mg/day and said estradiol ester is delivered through the skin at a rate of about 25-250 μg/day.
Claim 25
Dependent Claim
36 words
The method of claim 21 wherein said progesterone is delivered through the skin at a rate of about 24 mg/day and said estradiol ester is delivered through the skin at a rate of about 50-150 μg/day.
Claim 26
Dependent Claim
141 words
A medical device for the transdermal delivery of a drug for a predetermined time period selected from the group consisting of progesterone, an estradiol ester and mixtures thereof comprising in combination: (a) a reservoir means containing said drug and a permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, propylene glycol dipelarginate and neopentyl glycol dicaprate; (b) a means for maintaining said reservoir means in drug and permeation enhancer transmitting relationship to the skin at therapeutically effective rates; (c) said drug being present in said reservoir means in amounts sufficient to deliver said drug at said therapeutically effective rates for said predetermined time period; and (d) said permeation enhancer being present in said reservoir means in amounts sufficient to deliver said permeation enhancer at said therapeutically effective rates for said predetermined time period.
Claim 27
Dependent Claim
141 words
A medical device for the transdermal delivery of a drug for a predetermined time period selected from the group consisting of progesterone, an estradiol ester and mixtures thereof comprising in combination: (a) a reservoir means containing said drug and a permeation enhancer selected from the group consisting of sucrose monolaurate, glycerol monooleate, glycerol monolaurate, propylene glycol laurate, propylene glycol dipelarginate and neopentyl glycol dicaprate; (b) a means for maintaining said reservoir means in drug and permeation enhancer transmitting relationship to the skin at therapeutically effective rates; (c) said drug being present in said reservoir means in amounts sufficient to deliver said drug at said therapeutically effective rates for said predetermined time period; and (d) said permeation enhancer being present in said reservoir means in amounts sufficient to deliver said permeation enhancer at said therapeutically effective rates for said predetermined time period.
Claim 28
Dependent Claim
27 words
The medical device of claim 24 wherein said means for maintaining said reservoir in drug and permeation enhancer transmitting relationship to the skin is an adhesive overlay.
Claim 29
Dependent Claim
28 words
The medical device of claim 24 wherein said means for maintaining said reservoir in drug and permeation enhancer transmitting relationship to the skin is an in-line contact adhesive.
Claim 30
Dependent Claim
11 words
The medical device of claim 24 wherein said drug is progesterone.
Claim 31
Dependent Claim
13 words
The medical device of claim 24 wherein said drug is an estradiol ester.
Claim 32
Dependent Claim
18 words
The medical device of claim 24 wherein said drug is a combination of progesterone and an estradiol ester.
Claim 33
Independent Claim
57 words
A method for the treatment of post-menopausal symptoms in the human female which comprises transdermally administering progesterone and an estradiol ester at therapeutically effective rates nd durations, said rates and durations defining a 28 day therapeutic regimen, and repeating said regimen at the expiration of the preceding 28 day regimen for so long as therapy is desired.
Claim 34
Independent Claim
57 words
A method for the treatment of post-menopausal symptoms in the human female which comprises transdermally administering progesterone and an estradiol ester at therapeutically effective rates nd durations, said rates and durations defining a 28 day therapeutic regimen, and repeating said regimen at the expiration of the preceding 28 day regimen for so long as therapy is desired.
Claim 35
Dependent Claim
32 words
The method of claim 30 wherein said 28 day regimen comprises delivering an estradiol ester for 14 days, followed by delivering a mixture of an estradiol ester and progesterone for 14 days.
Claim 36
Dependent Claim
25 words
The method of claim 30 wherein said 28 day regimen comprises delivering an estradiol ester for 14 days, followed by delivering progesterone for 14 days.
Claim 37
Dependent Claim
39 words
The method of claim 30 wherein said 28 day regimen comprises delivering an estradiol ester for 7 days, followed by delivering a mixture of an estradiol ester and progesterone for 14 days, followed by delivering progesterone for 7 days.
Claim 38
Dependent Claim
23 words
The method of claim 30 wherein said 28 day regimen comprises delivering a mixture of an estradiol ester and progesterone for 28 days.
Claim 39
Dependent Claim
23 words
The method of claim 34 wherein the delivery ratio of said estradiol ester to said progesterone varies within the 28 day delivery period.
Claim 40
Dependent Claim
17 words
The composition of claim 1 wherein said drug and skin permeation enhancer are dispersed within a carrier.
Claim 41
Dependent Claim
46 words
A 28 day transdermal dosage package for the treatment of post-menopausal symptoms comprising in combination, a container containing a plurality of transdermal systems for delivering progesterone and an estradiol ester at therapeutically effective rates and durations, said rates and durations defining a 28 day therapeutic regimen.
Claim 42
Dependent Claim
46 words
A 28 day transdermal dosage package for the treatment of post-menopausal symptoms comprising in combination, a container containing a plurality of transdermal systems for delivering progesterone and an estradiol ester at therapeutically effective rates and durations, said rates and durations defining a 28 day therapeutic regimen.
Claim 43
Dependent Claim
63 words
The package of claim 37 wherein a portion of said systems deliver said estradiol ester and the remainder of said systems deliver a mixture of said estradiol ester and progesterone, wherein said systems delivering the estradiol ester deliver said estradiol ester for the initial 14 day and systems delivering the estradiol ester and progesterone mixture deliver said mixture for the remaining 14 days.
Claim 44
Dependent Claim
51 words
The package of claim 37 wherein a portion of said systems deliver said estradiol ester and the remainder of said systems deliver progesterone, wherein said systems delivering the estradiol ester deliver said estradiol ester for the initial 14 days and systems delivering progesterone deliver said progesterone for the remaining 14 days.
Claim 45
Dependent Claim
85 words
The package of claim 37 wherein a first portion of said systems deliver said estradiol ester, a second portion of said systems deliver a mixture of said estradiol ester and progesterone and the remainder of said systems deliver progesterone, wherein said systems delivering the estradiol ester deliver said estradiol ester for the initial 7 days, systems delivering a mixture of the estradiol ester and progesterone deliver said mixture for the subsequent 14 days and systems delivering progesterone deliver said progesterone for the remaining 7 days.
Claim 46
Dependent Claim
17 words
The package of claim 37 wherein said systems deliver a mixture of said estradiol ester and progesterone.
Claim 47
Dependent Claim
17 words
The package of claim 41 wherein said systems have varying amounts of said estradiol ester and progesterone.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-11-29 | 1992-05-30 | 1992-11-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-11-29 | 1996-05-30 | 1996-11-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-11-29 | 2000-05-30 | 2000-11-29 | $7700.00 | Window Closed / Lapsed |