# US 8,771,722 B2 · Methods of treating ocular disease using steroid-containing sustained release intraocular implants

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- Number: US 8,771,722 B2
- Document ID: US8771722B2
- Status: Granted
- Kind: B2
- Application number: 13/356,934
- Filed: 2012-01-24
- Published: 2012-05-17
- Granted: 2014-07-08
- Earliest claimed: 2004-04-30
- Assignees: Allergan, Inc.
- Applicants: Glenn T. Huang; Thierry Nivaggioli; Lon T. Spada; Hiroshi Sugimoto; Wendy M. Blanda; James N. Chang; Orest Olejnik
- Inventors: Glenn T. Huang; Thierry Nivaggioli; Lon T. Spada; Hiroshi Sugimoto; Wendy M. Blanda; James N. Chang; Orest Olejnik
- Web page: https://patentgrep.com/patent/US8771722B2

## CPC

- A61K 9/0051: {Ocular inserts or implants}
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 9/0092: {Hollow drug-filled fibres, tubes of the core-shell type, coated fibres, coated rods, microtubules or nanotubes}
- A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/593: {Polyesters, e.g. PLGA or polylactide-co-glycolide}
- A61L 27/18: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
- A61L 27/54: Biologically active materials, e.g. therapeutic substances {(A61L27/227 takes precedence)}
- A61L 27/58: Materials at least partially resorbable by the body
- A61L 31/06: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds {(A61L31/041 takes precedence)}
- A61L 31/148: {Materials at least partially resorbable by the body}
- A61L 31/16: Biologically active materials, e.g. therapeutic substances {(A61L31/047 takes precedence)}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61F 9/0017: {implantable in, or in contact with, the eye, e.g. ocular inserts}
- A61K 9/204: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61L 2300/222: Steroids, e.g. corticosteroids
- A61L 2300/436: of receptors
- A61L 2300/45: Mixtures of two or more drugs, e.g. synergistic mixtures
- A61L 2300/604: Biodegradation
- A61L 2430/16: for reconstruction of eye parts, e.g. intraocular lens, cornea
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61F: FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS (dental prosthetics A61C)

## Abstract

Biocompatible intraocular implants include a steroid and an auxiliary agent, where the auxiliary agent is present in an amount sufficient to lessen the severity of at least one side effect compared to the use of an otherwise identical implant lacking said auxiliary agent. The steroid and the auxiliary agent may be present on the same intraocular implant or on different implants. The steroid and auxiliary agent may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants containing the steroid and an auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the side effects otherwise accompanying steroid use.

## Claims

### Claim 1

A method of treating an ocular disease in an eye of a patient comprising contacting an implant comprising a steroid with an ocular fluid in the eye of the patient, thereby releasing steroid from the implant into the ocular fluid; and contacting an implant comprising an auxiliary agent with the ocular fluid in the eye of the patient, thereby releasing auxiliary agent from the implant into the ocular fluid, wherein the steroid is present in an amount effective to treat the ocular disease, and wherein the auxiliary agent is present in an amount effective to reduce the occurrence of at least one side effect of the steroid.

### Claim 2 (depends on 1)

The method of claim 1, wherein the auxiliary agent comprises an antiglaucoma drug selected from the group consisting of a parasympathomimetic, a sympathomimetic, an alpha 2 adrenergic receptor agonist, a beta blocker, a carbonic anhydrase inhibitor, a prostaglandin analog, a neuroprotectant, and mixtures thereof.

### Claim 3 (depends on 2)

The method of claim 2, wherein the antiglaucoma drug is selected from the group consisting of, carbachol, echothiophate, epinephrine, dipivefrin, brimonidine, clonidine, apraclonidine, oxymetazoline, epinephrine, norepinephrine, cirazoline, mivazerol, xylazine, memantine, timolol, levobunolol, metipranolol, carteolol, betaxolol, dorzolamide, brinzolamide, dichlorphenamide, latanoprost, bimatoprost, travoprost, unoprostone, and mixtures thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein the steroid and the auxiliary agent are released from the implant simultaneously.

### Claim 5 (depends on 1)

The method of claim 1, wherein the steroid and the auxiliary agent are released from the implant at different times.

### Claim 6 (depends on 1)

The method of claim 1, wherein the steroid and the auxiliary agent are released from the implant intermittently.

### Claim 7 (depends on 1)

The method of claim 1, wherein the ocular implant comprising the steroid and the ocular implant comprising the auxiliary agent are the same implant.

### Claim 8 (depends on 1)

The method of claim 1, wherein the ocular implant comprising the steroid and the ocular implant comprising the auxiliary agent are different implants.

### Claim 9 (depends on 1)

The method of claim 1, wherein the steroid is dexamethasone and the auxiliary agent is bimatoprost.

### Claim 10 (depends on 9)

The method of claim 9, wherein the ocular disease is macular degeneration, macular edema, or uveitis.