US4291014A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Polymeric diffusion matrix containing estradiol diacetate
Assignee: Key Pharmaceuticals Inc
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Filing: 1980-07-11
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Granted: 1981-09-22
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Expires: 2000-07-11
Abstract
Abstract There is disclosed a polymeric diffusion matrix for the sustained release of estradiol diacetate by delivery to a patient requiring uterine wall maintenance or other types of estrogen therapy wherein the matrix comprises a polar plasticizer, polyvinylalcohol, polyvinylpyrrolidone, and a pharmaceutically effective amount of estradiol diacetate.
Inventors
- 👤 Alec D. Keith
- 👤 Wallace Snipes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 20:05
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K31/00; A61K31/56; A61K31/565; A61K9/0012; A61K9/0034; A61K9/0036; A61L; A61L15/00; A61L15/16; A61L15/22; A61L15/225
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
84 words
A self-supporting polymeric diffusion matrix for the sustained release of estradiol diacetate in order to deliver said estradiol diacetate to a patient and provide said patient with a uterine wall maintenance effect, said matrix comprising from about 2 to about 60% of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone, and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 2
Dependent Claim
84 words
A self-supporting polymeric diffusion matrix for the sustained release of estradiol diacetate in order to deliver said estradiol diacetate to a patient and provide said patient with a uterine wall maintenance effect, said matrix comprising from about 2 to about 60% of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone, and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 3
Dependent Claim
13 words
The polymeric diffusion matrix of claim 1 wherein said polar plasticizer is glycerol.
Claim 4
Dependent Claim
20 words
The polymeric diffusion matrix of claim 1 wherein said polyvinylalcohol has a molecular weight of about 50,000 to about 150,000.
Claim 5
Dependent Claim
20 words
The polymeric diffusion matrix of claim 1 wherein said polyvinylalcohol has a molecular weight of about 100,000 to about 150,000.
Claim 6
Dependent Claim
21 words
The polymeric diffusion matrix of claim 1 wherein said polyvinylpyrrolidone has a molecular weight of from about 15,000 to about 85,000.
Claim 7
Dependent Claim
20 words
The polymeric diffusion matrix of claim 1 wherein said polyvinylpyrrolidone has a molecular weight of about 20,000 to about 60,000.
Claim 8
Dependent Claim
25 words
The polymeric diffusion matrix of claim 1 wherein said polar plasticizer is polyethylene glycol present in an amount of about 1 to about 15% weight.
Claim 9
Dependent Claim
41 words
The polymeric diffusion matrix of claim 1 wherein said polar plasticizer is a mixture of glycerol and polyethylene glycol wherein said polyethylene glycol is present in an amount by weight of from about 1 to about 5 parts per weight glycerol.
Claim 10
Independent Claim
88 words
A method for the delivery of estradiol diacetate to a patient to provide said patient with a uterine wall maintenance effect, comprising applying in the vicinity of the cervix of said patient a self-supporting diffusion matrix comprising from about 1 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 11
Independent Claim
88 words
A method for the delivery of estradiol diacetate to a patient to provide said patient with a uterine wall maintenance effect, comprising applying in the vicinity of the cervix of said patient a self-supporting diffusion matrix comprising from about 1 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 12
Dependent Claim
30 words
The method of claim 9 wherein said estradiol diacetate is present in an amount to provide sustained release of about 0.1 to about 1 mg of estradiol diacetate per day.
Claim 13
Independent Claim
85 words
A method for the transdermal delivery of estradiol diacetate to a patient to provide said patient with an increased blood level of estradiol comprising applying to said patient a self supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 14
Independent Claim
85 words
A method for the transdermal delivery of estradiol diacetate to a patient to provide said patient with an increased blood level of estradiol comprising applying to said patient a self supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 15
Dependent Claim
30 words
The method of claim 11 wherein said estradiol diacetate is present in an amount to provide sustained release of about 0.05 to about 1 mg of estradiol diacetate per day.
Claim 16
Independent Claim
95 words
A method for the transdermal delivery of estradiol diacetate to a patient for the treatment or prevention of diseases associated with estradiol deficiency to provide said patient with an increased blood level of estradiol comprising applying to said patient a self-supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 17
Independent Claim
95 words
A method for the transdermal delivery of estradiol diacetate to a patient for the treatment or prevention of diseases associated with estradiol deficiency to provide said patient with an increased blood level of estradiol comprising applying to said patient a self-supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol diacetate over a prolonged period.
Claim 18
Dependent Claim
16 words
The method of claim 13 where the disease condition to be treated or prevented is osteoporosis.
Claim 19
Independent Claim
94 words
A method for the intravaginal delivery of estradiol diacetate to a patient for the treatment or prevention of diseases associated with estradiol deficiency to provide said patient with an increased blood level of estradiol comprising applying to said patient a self-supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol over a prolonged period.
Claim 20
Independent Claim
94 words
A method for the intravaginal delivery of estradiol diacetate to a patient for the treatment or prevention of diseases associated with estradiol deficiency to provide said patient with an increased blood level of estradiol comprising applying to said patient a self-supporting diffusion matrix comprising from about 2 to about 60% by weight of a polar plasticizer, from about 6 to about 20% by weight polyvinylalcohol, from about 2 to about 10% by weight polyvinylpyrrolidone and a pharmaceutically effective amount of estradiol diacetate to provide a sustained release of said estradiol over a prolonged period.
Claim 21
Dependent Claim
16 words
The method of claim 14 where the disease condition to be treated or prevented is osteoporosis.
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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) | 1984-09-21 | 1985-03-23 | 1985-09-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-09-21 | 1989-03-23 | 1989-09-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-09-21 | 1993-03-23 | 1993-09-22 | $7700.00 | Window Closed / Lapsed |