US4291015A
Expired / Lapsed
US
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Polymeric diffusion matrix containing a vasodilator
Assignee: Key Pharmaceuticals Inc
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Filing: 1980-06-26
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Granted: 1981-09-22
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Expires: 2000-06-26
Abstract
Abstract A polymeric diffusion matrix containing a vasodilator is provided comprising from about 2 to about 60% of a polar plasticizer, e.g., glycerol, from about 2 to about 15% of a matrix component, e.g., polyvinylalcohol, from about 2 to about 10% of a water-soluble polymer with hydration sites, e.g., polyvinylpyrrolidone, which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator drug dispersed therein, and the balance water, the percentages being by weight.
Inventors
- 👤 Alec D. Keith
- 👤 Wallace Snipes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 23:44
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K31/00; A61K31/13; A61K31/135; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/56; A61K31/565
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
123 words
A self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a vasodilator comprising from about 2 to about 60% of the polar plasticizer selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol, from about 2 to about 15% of a matrix component selected from the group consisting of polyvinylalcohol, a polymer of hydroxyethylacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate, from about 2 to about 10% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator dispersed therein, at least one vasodilator suitable for transdermal delivery to a patient, and the balance water, the percentages being by weight.
Claim 2
Dependent Claim
123 words
A self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a vasodilator comprising from about 2 to about 60% of the polar plasticizer selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol, from about 2 to about 15% of a matrix component selected from the group consisting of polyvinylalcohol, a polymer of hydroxyethylacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate, from about 2 to about 10% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator dispersed therein, at least one vasodilator suitable for transdermal delivery to a patient, and the balance water, the percentages being by weight.
Claim 3
Dependent Claim
33 words
The polymeric diffusion matrix of claim 1 wherein said water-soluble polymer is selected from the group consisting of polyvinylpyrrolidone, agar, agarose, gum arabic, gum tragacanth, polyacrylic acid, polymethacrylic acid, polyvinyloxazolidone, polyvinylmorpholinone, and polyvinylpiperidone.
Claim 4
Dependent Claim
13 words
The polymeric diffusion matrix of claim 2 wherein said water-soluble polymer is polyvinylpyrrolidone.
Claim 5
Dependent Claim
24 words
The polymeric diffusion matrix of claim 3 wherein said matrix component is polyvinylalcohol having a molecular weight of from about 50,000 to about 150,000.
Claim 6
Dependent Claim
21 words
The polymeric diffusion matrix of claim 4 wherein said polyvinylalcohol has a molecular weight of from about 100,000 to about 150,000.
Claim 7
Dependent Claim
21 words
The polymeric diffusion matrix of claim 3 wherein said polyvinylpyrrolidone has a molecular weight of from about 20,000 to about 60,000.
Claim 8
Dependent Claim
38 words
The polymeric diffusion matrix of claim 3 wherein said matrix component is polyvinylalcohol having a molecular weight of from about 100,000 to about 150,000 and said polyvinylpyrrolidone has a molecular weight of from about 20,000 to about 60,000.
Claim 9
Dependent Claim
12 words
The polymeric diffusion matrix of claim 1 wherein said vasodilator is trinitroglycerol.
Claim 10
Dependent Claim
13 words
The polymeric diffusion matrix of claim 1 wherein said vasodilator is lactose triturate.
Claim 11
Dependent Claim
22 words
The polymeric diffusion matrix of claim 1 wherein said vasodilator is nitroglycerin and said nitroglycerin is attached to an active absorbent surface.
Claim 12
Dependent Claim
48 words
The polymeric diffusion matrix of claim 10 wherein said absorbent surface is provided by a member selected from the group consisting of lactose, insolubilized starch, micronized cellulose, silica gel, di- and oligosaccharides having a degree of solubility from lower than up to twice that of lactose, and cyclitols.
Claim 13
Dependent Claim
79 words
A self-supporting polymeric diffusion matrix suitable for the delivery of a drug having a vasodilator effect comprising from about 35 to about 60% glycerol, from about 4 to about 9% polyvinylalcohol, from about 2 to about 5% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator drug dispersed therein, a therapeutically effective amount of trinitroglycerol and the balance water, the percentages being by weight.
Claim 14
Dependent Claim
79 words
A self-supporting polymeric diffusion matrix suitable for the delivery of a drug having a vasodilator effect comprising from about 35 to about 60% glycerol, from about 4 to about 9% polyvinylalcohol, from about 2 to about 5% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator drug dispersed therein, a therapeutically effective amount of trinitroglycerol and the balance water, the percentages being by weight.
Claim 15
Dependent Claim
24 words
The polymeric diffusion matrix of claim 12 wherein said water-soluble polymer is polyvinylpyrrolidone having a moleculr weight of from about 20,000 to about 60,000.
Claim 16
Dependent Claim
22 words
The polymeric diffusion matrix of claim 12 wherein said glycerol is present in an amount of from about 45 to about 55%.
Claim 17
Dependent Claim
21 words
The polymeric diffusion matrix of claim 8 wherein said polyvinylalcohol has a molecular weight of from about 100,000 to about 150,000.
Claim 18
Independent Claim
154 words
A method of delivering a vasodilator drug to a patient over a prolonged period at a steady rate which comprises applying to said patient a self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a vasodilator drug, said mixture comprising from about 2 to about 60% of a polar plasticizer compound selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol, from about 2 to about 15% of a matrix component selected from the group consisting of polyvinyl alcohol, a polymer of hydroxyethylacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate, from about 2 to about 10% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator drug dispersed therein, at least one vasodilator drug suitable for transdermal delivery to said patient, and the balance water, the percentages being by weight.
Claim 19
Independent Claim
154 words
A method of delivering a vasodilator drug to a patient over a prolonged period at a steady rate which comprises applying to said patient a self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a vasodilator drug, said mixture comprising from about 2 to about 60% of a polar plasticizer compound selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol, from about 2 to about 15% of a matrix component selected from the group consisting of polyvinyl alcohol, a polymer of hydroxyethylacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate, from about 2 to about 10% of a water-soluble polymer with hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a vasodilator drug dispersed therein, at least one vasodilator drug suitable for transdermal delivery to said patient, and the balance water, the percentages being by weight.
Claim 20
Dependent Claim
11 words
The method of claim 16 wherein said vasodilator drug is trinitroglycerol.
Claim 21
Dependent Claim
28 words
The method of claim 17 wherein said water soluble polymer in said matrix is polyvinylpyrrolidone, said polyvinylpyrrolidone having a molecular weight of from about 20,000 to about 60,000.
Claim 22
Dependent Claim
21 words
The method of claim 17 wherein said matrix component is polyvinylalcohol having a molecular weight of from about 100,000 to 150,000.
Claim 23
Dependent Claim
58 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient by transdermal application, said matrix comprising (a) from about 2 to about 60% by weight glycerol; (b) from about 2 to about 15% by weight polyvinylalcohol; (c) from about 2 to about 10% by weight polyvinylpyrrolidone; and (d) a pharmaceutically effective amount of trinitroglycerol.
Claim 24
Dependent Claim
58 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient by transdermal application, said matrix comprising (a) from about 2 to about 60% by weight glycerol; (b) from about 2 to about 15% by weight polyvinylalcohol; (c) from about 2 to about 10% by weight polyvinylpyrrolidone; and (d) a pharmaceutically effective amount of trinitroglycerol.
Claim 25
Dependent Claim
80 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient for transdermal application, said matrix comprising (a) from about 35 to about 55% by weight glycerol; (b) from about 4 to about 15% by weight polyvinylalcohol having a molecular weight of from about 100,000 to about 150,000; (c) from about 2 to about 10% by weight polyvinylpyrrolidone having a molecular weight of from about 20,000 to about 60,000; and (d) a pharmaceutically effective amount of trinitroglycerol.
Claim 26
Dependent Claim
80 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient for transdermal application, said matrix comprising (a) from about 35 to about 55% by weight glycerol; (b) from about 4 to about 15% by weight polyvinylalcohol having a molecular weight of from about 100,000 to about 150,000; (c) from about 2 to about 10% by weight polyvinylpyrrolidone having a molecular weight of from about 20,000 to about 60,000; and (d) a pharmaceutically effective amount of trinitroglycerol.
Claim 27
Dependent Claim
12 words
The polymeric diffusion matrix of claim 21 formed from an aqueous mixture.
Claim 28
Dependent Claim
57 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient by transdermal application, said matrix containing about equal parts water and glycerol, about 7% by weight polyvinylalcohol having a molecular weight of abiout 115,000, about 5% by weight polyvinylpyrrolidone having a molecular weight of about 40,000, and a pharmaceutically effective amount of trinitroglycerol.
Claim 29
Dependent Claim
57 words
A self-supporting polymeric diffusion matrix for the sustained release of trinitroglycerol to a patient by transdermal application, said matrix containing about equal parts water and glycerol, about 7% by weight polyvinylalcohol having a molecular weight of abiout 115,000, about 5% by weight polyvinylpyrrolidone having a molecular weight of about 40,000, and a pharmaceutically effective amount of trinitroglycerol.
Claim 30
Dependent Claim
18 words
The polymeric diffusion matrix of claim 23 wherein said trinitroglycerol is present in the form of lactose triturate.
Claim 31
Dependent Claim
117 words
A self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a drug, said matrix comprising (a) from about 2 to about 60% of a polar plasticizer selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol; (b) from about 2 to 15% of a matrix component selected from the group consisting of polyvinylalcohol, a polymer of hydroxyethyacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate; (c) from about 2 to about 10% of a water-soluble polymer with hydration sites, which in combination with the remaining ingredients yields a matrix capable of sustained release of a drug dispersed therein; and (d) the balance water, the percentages being by weight.
Claim 32
Dependent Claim
117 words
A self-supporting polymeric diffusion matrix suitable for the transdermal delivery of a drug, said matrix comprising (a) from about 2 to about 60% of a polar plasticizer selected from the group consisting of glycerol, propylene glycol, and a polyalkylene glycol; (b) from about 2 to 15% of a matrix component selected from the group consisting of polyvinylalcohol, a polymer of hydroxyethyacrylate, a polymer of hydroxyethylmethacrylate, a polymer of hydroxypropylacrylate, and a polymer of hydroxypropylmethacrylate; (c) from about 2 to about 10% of a water-soluble polymer with hydration sites, which in combination with the remaining ingredients yields a matrix capable of sustained release of a drug dispersed therein; and (d) the balance water, the percentages being by weight.
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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 |