Sustained release ophthalmic drug dosage

Claim 2

An ophthalmic dosage of an aqueous gel for application to the conjunctival sac of the eye, said gel comprising an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer, said polymer having a molecular weight in excess of 1,000,000, said ophthalmic drug being present at a level of from about 0.03 to about 15 percent by weight, said polymer being present at a level of from about 2 to about 8 percent by weight, said gel having a viscosity of from about 40,000 to about 300,000 cps and a yield value of from about 5,000 to about 20,000 dyne/cm 2 .

Claim 3

An aqueous gel in accordance with claim 1 wherein said polymer has a molecular weight of from about 1,000,000 to about 6,000,000.

Claim 4

An aqueous gel in accordance with claim 1 wherein said gel has a viscosity of from about 75,000 to about 200,000 cps.

Claim 5

An aqueous gel in accordance with claim 1 wherein said gel has a viscosity of from about 90,000 to about 150,000 cps.

Claim 6

An aqueous gel in accordance with claim 1 wherein said ophthalmic drug is selected from the group consisting of idoxuridine, pilocarpine and its acceptable salts, and carbachol.

Claim 7

An aqueous gel in accordance with claim 1 wherein said ophthalmic drug is an ophthalmic steroid selected from the group consisting of hydrocortisone, hydrocortisone acetate, dexamethasone, dexamethasone 21-phosphate, fluorocinoline, medrysone, prednisolone, methylprednisolone, prednisolone 21-phosphate, prednisolone acetate, fluorometholone, betamethasone and triamcinolone.

Claim 8

An aqueous gel in accordance with claim 1 wherein said ophthalmic drug is an ophthalmic antibiotic selected from the group consisting of neomycin, polymyxin, chloramphenicol, erythromycin, tobramycin and gentamycin.

Claim 9

An aqueous gel in accordance with claim 1 wherein the pH of said gel is from about 4.5 to about 8.5.

Claim 10

An aqueous gel in accordance with claim 1 wherein said ophthalmic drug is pilocarpine, said gel having a viscosity of from about 75,000 to about 200,000 cps and a yield value of from about 5,000 to about 20,000 dyne/cm 2 .

Claim 11

An ophthalmic drug dosage comprising an anhydrous mixture of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, the concentration of said ophthalmic drug and said polymer in said mixture being selected such that when said mixture is introduced into the conjunctival sac of the eye and mixed with the aqueous tear fluid therein an aqueous gel is formed containing between about 0.03 and about 15 percent by weight of said ophthalmic drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between about 5,000 and about 20,000 dynes/cm 2 .

Claim 12

An ophthalmic drug dosage comprising an anhydrous mixture of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, the concentration of said ophthalmic drug and said polymer in said mixture being selected such that when said mixture is introduced into the conjunctival sac of the eye and mixed with the aqueous tear fluid therein an aqueous gel is formed containing between about 0.03 and about 15 percent by weight of said ophthalmic drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between about 5,000 and about 20,000 dynes/cm 2 .

Claim 13

An ophthalmic dosage in accordance with claim 10 wherein said polymer has a molecular weight of from about 1,000,000 to about 6,000,000.

Claim 14

An ophthalmic dosage in accordance with claim 10 wherein said ophthalmic drug is selected from the group consisting of idoxuridine, pilocarpine and carbachol.

Claim 15

An ophthalmic dosage in accordance with claim 10 wherein said ophthalmic drug is an ophthalmic antibiotic selected from the group consisting of neomycin, polymyxin, chloramphenicol, erythromycin, tobramycin and gentamycin.

Claim 16

An ophthalmic dosage in accordance with claim 10 wherein said ophthalmic drug is pilocarpine.

Claim 17

An ophthalmic dosage in accordance with claim 10 wherein said mixture is suspended in a nonaqueous vehicle.

Claim 18

An ophthalmic drug dosage in accordance with claim 10 wherein said vehicle is a stabilized oil selected from the group consisting of mineral oil, vegetable oil, and silicone fluid.

Claim 19

An improved method for delivering an ophthalmic drug to the surface of the eye over extended periods of time, comprising preparing an aqueous gel of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, and adjusting the pH of said gel to between about 4.5 and about 8.5, said gel containing between about 0.03 and about 15 percent by weight of said ophthalmic drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between about 5,000 and about 20,000 dynes/cm 2 , and introducing said gel into the conjunctival sac of the eye, whereby prolonged retention and slow release of said ophthalmic drug is provided.

Claim 20

An improved method for delivering an ophthalmic drug to the surface of the eye over extended periods of time, comprising preparing an aqueous gel of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, and adjusting the pH of said gel to between about 4.5 and about 8.5, said gel containing between about 0.03 and about 15 percent by weight of said ophthalmic drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between about 5,000 and about 20,000 dynes/cm 2 , and introducing said gel into the conjunctival sac of the eye, whereby prolonged retention and slow release of said ophthalmic drug is provided.

Claim 21

A method in accordance with claim 17 wherein said polymer has a molecular weight of from about 1,000,000 to about 6,000,000.

Claim 22

A method in accordance with claim 17 wherein said aqueous gel has a viscosity of from about 75,000 to about 200,000 cps.

Claim 23

A method in accordance with claim 17 wherein said gel has a viscosity of from about 90,000 to about 150,000 cps.

Claim 24

A method in accordance with claim 17 wherein said ophthalmic drug is selected from the group consisting of idoxuridine, pilocarpine and its acceptable salts, and carbachol.

Claim 25

A method in accordance with claim 17 wherein said ophthalmic drug is an ophthalmic steroid selected from the group consisting of hydrocortisone, hydrocortisone acetate, dexamethasone, dexamethasone 21-phosphate, fluorocinolone, medrysone, prednisolone, methylprednisolone, prednisolone 21-phosphate, prednisolone acetate, fluorometholone, betamethasone and triamcinolone.

Claim 26

A method in accordance with claim 17 wherein said ophthalmic drug is an ophthalmic antibiotic selected from the group consisting of neomycin, polymyxin, chloramphenicol, erythromycin, tobramycin and gentamycin.

Claim 27

A method in accordance with claim 17 wherein the pH of said gel is from about 4.5 to about 8.5.

Claim 28

A method in accordance with claim 17 wherein said ophthalmic drug is pilocarpine, said gel having a viscosity of from about 75,000 to about 200,000 cps and a yield value of from about 5,000 to about 20,000 dyne/cm 2 .

Claim 29

An improved method for delivering an ophthalmic drug to the surface of the eye over extended periods of time, comprising preparing an anhydrous mixture of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, introducing said mixture into the conjunctival sac of the eye and reacting said polymer with the aqueous tear fluid in said sac to form a gel containing between about 0.03 and about 15 percent by weight of said drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between 5,000 and 20,000 dynes/cm 2 .

Claim 30

An improved method for delivering an ophthalmic drug to the surface of the eye over extended periods of time, comprising preparing an anhydrous mixture of an ophthalmic drug and a gel-forming high molecular weight ethylene maleic anhydride polymer having a molecular weight in excess of 1,000,000, introducing said mixture into the conjunctival sac of the eye and reacting said polymer with the aqueous tear fluid in said sac to form a gel containing between about 0.03 and about 15 percent by weight of said drug and between about 2 and about 8 percent by weight of said polymer, said gel having a viscosity of between about 40,000 and about 300,000 cps and a yield point of between 5,000 and 20,000 dynes/cm 2 .

Claim 31

A method in accordance with claim 26 wherein said ophthalmic drug is selected from the group consisting of idoxuridine, pilocarpine and carbachol.

Claim 32

A method in accordance with claim 26 wherein said ophthalmic drug is an ophthalmic antibiotic selected from the group consisting of neomycin, polymyxin, chloramphenicol, erythromycin, tobramycin and gentamycin.

Claim 33

A method in accordance with claim 26 wherein said ophthalmic drug is pilocarpine.