US4057619A
Expired / Lapsed
US
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Ocular therapeutic system with selected membranes for administering ophthalmic drug
Assignee: Alza Corp
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Filing: 1976-07-15
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Granted: 1977-11-08
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Expires: 1996-07-15
Abstract
Abstract An ocular therapeutic system for releasing a drug to the eye at a controlled and continuous rate for a prolonged period of time is disclosed. The system is shaped, sized and adapted for insertion and retention in the eye. The system contains an ophthalmically acceptable drug and it is formed of a polymeric material permeable to the passage of drug by diffusion. The material is an ethylene-vinyl ester copolymer of the general formula: ##STR1## WHEREIN R is hydrogen, alkyl of 2 to 7 carbons, or aryl, m is (4 to 80)% by weight and n is (100 - m)% by weight.
Inventors
- 👤 Takeru Higuchi
- 👤 Anwar Hussain
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:11
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0048; A61K9/0051
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
142 words
An ocular therapeutic system for the controlled administration of drug to the eye comprising a flexible body formed of a polymeric material containing a drug capable of diffusing through the material at a therapeutically effective rate, the body shaped, sized and adapted for comfortable insertion and retention in the cul-de-sac of the conjunctiva between the sclera of the eyeball and the lid to be held in place against the eyeball by the pressure of the lid, and wherein said material comprises an ethylene-vinyl alkyl substituted acetate copolymer having the following formula: ##STR16## which copolymer has a vinyl alkyl acetate content m of about 4 to 80% by weight, an ethylene content n of (100 - m)% by weight, a melt index of about 0.1 to 1000 grams per 10 minutes, and R is an alkyl group having 2 to 7 carbon atoms.
Claim 2
Dependent Claim
142 words
An ocular therapeutic system for the controlled administration of drug to the eye comprising a flexible body formed of a polymeric material containing a drug capable of diffusing through the material at a therapeutically effective rate, the body shaped, sized and adapted for comfortable insertion and retention in the cul-de-sac of the conjunctiva between the sclera of the eyeball and the lid to be held in place against the eyeball by the pressure of the lid, and wherein said material comprises an ethylene-vinyl alkyl substituted acetate copolymer having the following formula: ##STR16## which copolymer has a vinyl alkyl acetate content m of about 4 to 80% by weight, an ethylene content n of (100 - m)% by weight, a melt index of about 0.1 to 1000 grams per 10 minutes, and R is an alkyl group having 2 to 7 carbon atoms.
Claim 3
Dependent Claim
30 words
The system according to claim 1 wherein the copolymer has a frequency of acyloxy groups on the polyethylene backbone of 1/200 to 1/35, and a density of 0.920 to 1.25.
Claim 4
Dependent Claim
53 words
The system according to claim 1 wherein the copolymer has a vinyl alkyl substituted acetate content of 4 to 50% by weight, a melt index of 0.5 to 500 grams per 10 minutes, a frequency of acyloxy groups on the polyethylene backbone of 1/150 to 1/8 and a density of 0.920 to 1.190.
Claim 5
Dependent Claim
11 words
The system according to claim 1 wherein the drug is pilocarpine.
Claim 6
Dependent Claim
21 words
The system according to claim 1 wherein the body is a container and said drug is contained in the reservoir thereof.
Claim 7
Dependent Claim
127 words
An ocular therapeutic system for the controlled administration of drug to the eye comprising a flexible body formed of a polymeric material surrounding a drug capable of diffusion through the material at a therapeutically effective rate, the body shaped, sized and adapted for comfortable insertion and retention in the cul-de-sac of the conjunctiva between the sclera of the eyeball and the eyelid to be held in place by the pressure of the eyelid, and wherein said material comprises a copolymer of the formula: ##STR17## wherein R is an alkyl group of 2 to 7 carbon atoms inclusive, m is (4 to 80)% by weight, n is (100 - m)% by weight, and the copolymer has a melt index of about 0.1 to 1000 grams per 10 minutes.
Claim 8
Dependent Claim
127 words
An ocular therapeutic system for the controlled administration of drug to the eye comprising a flexible body formed of a polymeric material surrounding a drug capable of diffusion through the material at a therapeutically effective rate, the body shaped, sized and adapted for comfortable insertion and retention in the cul-de-sac of the conjunctiva between the sclera of the eyeball and the eyelid to be held in place by the pressure of the eyelid, and wherein said material comprises a copolymer of the formula: ##STR17## wherein R is an alkyl group of 2 to 7 carbon atoms inclusive, m is (4 to 80)% by weight, n is (100 - m)% by weight, and the copolymer has a melt index of about 0.1 to 1000 grams per 10 minutes.
Claim 9
Dependent Claim
30 words
The system according to claim 6 wherein the copolymer has a frequency of acyloxy groups on the polyethylene backbone of 1/200 to 1/3.5, and a density of 0.920 to 1.25.
Claim 10
Dependent Claim
53 words
The system according to claim 6 wherein the copolymer has a vinyl alkyl substituted acetate content of 4 to 50% by weight, a melt index of 0.5 to 500 grams per 10 minutes, a frequency of aceloxy groups on the polyethylene backbone of 1/150 to 1/8, and a density of 0.920 to 1.190.
Claim 11
Dependent Claim
11 words
The system according to claim 6 wherein the drug is pilocarpine.
Claim 12
Dependent Claim
111 words
An ocular therapeutic system for the controlled administration of drug to an eye of a warm blooded mammal comprising a flexible body shaped, sized and adapted for insertion and placement in the eye and formed of a non-toxic, polymeric material permeable to the passage of drug contained in the body and capable of diffusing through the material in a therapeutically effective amount, and wherein the material comprises a copolymer of the formula: ##STR18## wherein R is a member selected from the group consisting of hydrogen, a lower alkyl group of 2 to 7 carbons and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight.
Claim 13
Dependent Claim
111 words
An ocular therapeutic system for the controlled administration of drug to an eye of a warm blooded mammal comprising a flexible body shaped, sized and adapted for insertion and placement in the eye and formed of a non-toxic, polymeric material permeable to the passage of drug contained in the body and capable of diffusing through the material in a therapeutically effective amount, and wherein the material comprises a copolymer of the formula: ##STR18## wherein R is a member selected from the group consisting of hydrogen, a lower alkyl group of 2 to 7 carbons and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight.
Claim 14
Dependent Claim
117 words
An ocular therapeutic system for the controlled administration of drug to an eye of a warm blooded animal comprising a flexible body shaped, sized and adapted for insertion and placement in the eye and formed of a non-toxic, polymeric material permeable to the passage of drug by diffusion, the material surrounding a reservoir containing a dosage amount of drug capable of diffusion through the material in a therapeutically effective amount, and wherein said material comprises a copolymer of the formula: ##STR19## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 2 to 7 carbons and phenyl, m is (4 to 80)% by weight, and n is (100 - m)% by weight.
Claim 15
Dependent Claim
117 words
An ocular therapeutic system for the controlled administration of drug to an eye of a warm blooded animal comprising a flexible body shaped, sized and adapted for insertion and placement in the eye and formed of a non-toxic, polymeric material permeable to the passage of drug by diffusion, the material surrounding a reservoir containing a dosage amount of drug capable of diffusion through the material in a therapeutically effective amount, and wherein said material comprises a copolymer of the formula: ##STR19## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 2 to 7 carbons and phenyl, m is (4 to 80)% by weight, and n is (100 - m)% by weight.
Claim 16
Dependent Claim
147 words
An ocular therapeutic system for the controlled and continuous administration of drug to the eye comprising a flexible body formed of a drug release rate controlling polymeric material permeable to the passage of drug by diffusion, the body adapted, shaped and sized with a length of 4 to 20 mm, a width of 0.1 to 12 mm, and a thickness of 0.1 to 4 mm for insertion and retention in the eye and containing drug therein, and wherein said material comprises a non-toxic copolymer of the formula: ##STR20## wherein R is a member selected from the group consisting of hydrogen, alkyl of 2 to 7 carbon atoms and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight, which copolymer when in the eye administers a therapeutically effective amount of drug at a controlled rate over a prolonged period of time.
Claim 17
Dependent Claim
147 words
An ocular therapeutic system for the controlled and continuous administration of drug to the eye comprising a flexible body formed of a drug release rate controlling polymeric material permeable to the passage of drug by diffusion, the body adapted, shaped and sized with a length of 4 to 20 mm, a width of 0.1 to 12 mm, and a thickness of 0.1 to 4 mm for insertion and retention in the eye and containing drug therein, and wherein said material comprises a non-toxic copolymer of the formula: ##STR20## wherein R is a member selected from the group consisting of hydrogen, alkyl of 2 to 7 carbon atoms and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight, which copolymer when in the eye administers a therapeutically effective amount of drug at a controlled rate over a prolonged period of time.
Claim 18
Dependent Claim
146 words
An ocular therapeutic system for the controlled and continuous administration of drug to the eye comprising a flexible body formed of a drug release rate controlling polymeric material permeable to the passage of drug by diffusion surrounding a reservoir containing drug, the body adapted, shaped and sized with a length of 4 to 20 mm, a width of 0.1 to 12 mm, and a thickness of 0.1 to 4 mm, for insertion and retention in the eye, the material comprising a non-toxic copolymer of the formula: ##STR21## wherein R is a member selected from the group consisting of hydrogen, alkyl of 2 to 7 carbon atoms and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight, which copolymer when in the eye administers a therapeutically effective amount of drug at a controlled rate over a prolonged period of time.
Claim 19
Dependent Claim
146 words
An ocular therapeutic system for the controlled and continuous administration of drug to the eye comprising a flexible body formed of a drug release rate controlling polymeric material permeable to the passage of drug by diffusion surrounding a reservoir containing drug, the body adapted, shaped and sized with a length of 4 to 20 mm, a width of 0.1 to 12 mm, and a thickness of 0.1 to 4 mm, for insertion and retention in the eye, the material comprising a non-toxic copolymer of the formula: ##STR21## wherein R is a member selected from the group consisting of hydrogen, alkyl of 2 to 7 carbon atoms and phenyl, m is (4 to 80)% by weight and n is (100 - m)% by weight, which copolymer when in the eye administers a therapeutically effective amount of drug at a controlled rate over a prolonged period of time.
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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) | 1980-11-07 | 1981-05-09 | 1981-11-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-11-07 | 1985-05-09 | 1985-11-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-11-07 | 1989-05-09 | 1989-11-08 | $7700.00 | Window Closed / Lapsed |