US4818540A
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US
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Transdermal fertility control system and process
Assignee: Rutgers, The State University of New Jersey
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Filing: 1986-08-29
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Granted: 1989-04-04
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Expires: 2006-08-29
Abstract
Abstract Transdermal fertility-controlling absorption polymer matrix dosage units have been developed which comprise a backing layer, an adjoining layer of a solid polymer matrix in which minimum effective daily doses of an estrogen and a progestin are microdispersed and released for transdermal absorption. Presently preferred is use of the natural estrogen, 17-beta-estradiol, and of the progestin, levonorgestrel. The units have a biologically acceptable adhesive polymer layer. The polymer matrix as well as the adhesive layer can have dispersed one or more skin permeation enhancers. Dosage units are provided which transdermally deliver at least minimum daily doses of the estrogen and progestin for multiple days, such as for one week. The invention also provides a process of fertility control using the novel polymer matrix dosage units for the first three weeks of consecutive menstrual cycles of the subject desiring fertility control.
Inventors
- 👤 Yie W. Chien
- 👤 Te-Yen Chien
- 👤 Yih-Chain Huang
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 00:30
CPC Classifications
A; A61; A61F; A61F13/00; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7038; A61K9/7046; A61K9/7069; A61K9/7084
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
145 words
A transdermal fertility-controlling polymer matrix dosage unit comprising: (a) a backing layer which is substantially impervious to the fertility-controlling estrogen and progestin hormones to be delivered transdermally; (b) a polymer matrix disc layer which is adhered to said backing layer and which has microdispersed therein effective dosage amounts of fertility-controlling estrogen and progestin hormones said estrogen being selected from the group consisting of 17-beta estradiol, ethinyl estradiol and biocompatible derivatives thereof convertible to said estradiols, progestin being selected from the group consisting of levonorgestrel and norethindrone, said polymer being bioacceptable and permitting said hormones to be transmitted for transdermal absorption, said hormones being stable in said polymer matrix and being transdermally absorbed simultaneously to provide at least minimum effective daily doses of said hormones to effect fertility control; and (c) an adhesive means for securing the dosage unit for transdermal absorption to the subject treated.
Claim 2
Dependent Claim
145 words
A transdermal fertility-controlling polymer matrix dosage unit comprising: (a) a backing layer which is substantially impervious to the fertility-controlling estrogen and progestin hormones to be delivered transdermally; (b) a polymer matrix disc layer which is adhered to said backing layer and which has microdispersed therein effective dosage amounts of fertility-controlling estrogen and progestin hormones said estrogen being selected from the group consisting of 17-beta estradiol, ethinyl estradiol and biocompatible derivatives thereof convertible to said estradiols, progestin being selected from the group consisting of levonorgestrel and norethindrone, said polymer being bioacceptable and permitting said hormones to be transmitted for transdermal absorption, said hormones being stable in said polymer matrix and being transdermally absorbed simultaneously to provide at least minimum effective daily doses of said hormones to effect fertility control; and (c) an adhesive means for securing the dosage unit for transdermal absorption to the subject treated.
Claim 3
Dependent Claim
29 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein said polymer matrix layer has dispersed therein an effective amount of one or more skin permeation enhancing agents.
Claim 4
Dependent Claim
18 words
A transdermal fertility-controlling dosage unit of claim 1 wherein the polymer matrix is a silicone polymer or copolymer.
Claim 5
Dependent Claim
30 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 3 wherein the silicone polymer or copolymer is a methyl silicone polymer or copolymer or a methylvinyl silicone polymer or copolymer.
Claim 6
Dependent Claim
57 words
A. transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein the polymer matrix disc layer is a crosslinked polysiloxane polymer of the following formula: ##STR5## wherein R is selected from the group consisting of alkyl or alkoxy having 1-7 carbon atoms, vinyl, phenyl or a combination thereof; and wherein n is about 100 to about 5,000.
Claim 7
Dependent Claim
31 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 3 wherein the matrix is made up of microdispersed compartments having a cross-sectional dimension of from about 10 to about 200 microns.
Claim 8
Dependent Claim
16 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein the estrogen hormone is 17-beta-estradiol.
Claim 9
Dependent Claim
15 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein the progestin is levonorgestrel.
Claim 10
Dependent Claim
20 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein the estrogen is 17-beta-estradiol and the progestin is levonorgestrel.
Claim 11
Dependent Claim
69 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein an effective progestin dosage of at least about 20 mcg per day is transdermally delivered for at least for a term of more than one day to about one week and an effective dose of estrogen of at least 20 is transdermally delivered for at least for a term of more than one day to about one week.
Claim 12
Dependent Claim
20 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 10 wherein the progestin is levonorgestrel and the estrogen is 17beta-estradiol.
Claim 13
Dependent Claim
20 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 6 wherein the progestin is levonorgestrel and the estrogen is 17-beta-estradiol.
Claim 14
Dependent Claim
21 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 1 wherein the progestin is norethindrone and the estrogen is ethinyl estradiol.
Claim 15
Dependent Claim
105 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 12 wherein the silicone polymer is a cross-linked siloxane polymer levonorgestrel is transdermally delivered at a dosage of at least about 20 mcg per day for at least for a term of more than one day to about one week and 17-beta-estradiol is transdermally delivered at a dosage of at least about 20 mcg per day for at least for a term of more than one day to about one week, the microdispersed compartment having present aqueous polyethylene glycol dispersing agent and the matrix layer having present an enhancing amount of a skin permeation enhancing agent.
Claim 16
Dependent Claim
93 words
A transdermal fertility-controlling polymer matrix dosoage unit of claim 12 wherein the silicone polymer is a cross-linked siloxane polymer norethindrone, is transdermally delivered at an effective dose for at least for a term of more than one day to about one week and ethinyl estradiol is transdermally delivered at an effective dialy dose for at least for a term of more than one day to about one week, the microdispersed compartment having present aqueous polyethylene glycol dispersing agent and the matrix layer having present an enhancing amount of a skin permeation enhancing agent.
Claim 17
Dependent Claim
23 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 13 wherein the daily dose amounts are transdermally delivered for at least one week.
Claim 18
Dependent Claim
17 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 14 wherein the cross-linked silicone polymer is polydimethylsiloxane.
Claim 19
Dependent Claim
21 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 4 wherein the cross-linked silicone polymer is a cross-linked methylvinyl silicone polymer.
Claim 20
Dependent Claim
52 words
A transdermal fertility-controlling polymer matrix dosage unit of claim 5 wherein the skin permeation enhancing agent is present in the matrix layer, the adhesive layer or both layers and is selected from isopropyl myristate, straight chain fatty acids having an alkyl groups having 4 to 18 carbon atoms or decyl methyl sulfoxide.
Claim 21
Dependent Claim
50 words
A transdermal fertility dosage unit of claim 16 wherein the skin permeation enhancing agent is present in the matrix layer, the adhesive layer or both layers and is selected from isopropyl myristate, straight chain fatty acids having an alkyl groups having 4 to 18 carbon atoms or decyl methyl sulfoxide.
Claim 22
Dependent Claim
62 words
A process of controlling fertility by applying to the skin of a subject desiring said treatment a dosage unit as described in claim 1 to provide at least the minimum effective dose amounts of progestin and estrogen for about the first three weeks of a menstrual cycle for successive menstrual cycles for a peroid extending as long as fertility control is desired.
Claim 23
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 3.
Claim 24
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 4.
Claim 25
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 6.
Claim 26
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 7.
Claim 27
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 10.
Claim 28
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 11.
Claim 29
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 12.
Claim 30
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 17.
Claim 31
Dependent Claim
16 words
A process of claim 19 wherein the dosage unit used is as described in claim 18.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-04-03 | 1992-10-03 | 1993-04-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-04-03 | 1996-10-03 | 1997-04-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-04-03 | 2000-10-03 | 2001-04-04 | $7700.00 | Window Closed / Lapsed |