# US 11,298,360 B2 · Ophthalmic compositions of brinzolamide

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 11,298,360 B2
- Document ID: US11298360B2
- Status: Granted
- Kind: B2
- Application number: 16/470,987
- Filed: 2019-04-02
- Published: 2021-11-18
- Granted: 2022-04-12
- Earliest claimed: 2018-04-25
- Assignees: Shilpa Medicare Limited
- Applicants: Shilpa Medicare Limited
- Inventors: Saraganachari Andanayya; Narayanaswamy Abhilash; Sreenivasa Reddy; Shivakumar Pradeep
- Web page: https://patentgrep.com/patent/US11298360B2

## CPC

- A61K 31/542: ortho- or peri-condensed with heterocyclic ring systems
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61P 27/02: Ophthalmic agents
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to an aqueous ophthalmic solution for treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma, the solution comprising at least 0.5 w/v % brinzolamide dissolved in the solution; hydroxy-propyl-β-cyclodextrin; polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; and water and/or the process for preparation thereof.

## Claims

### Claim 1

An aqueous ophthalmic solution for treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma, the solution comprising
(a) at least 0.5 w/v % brinzolamide dissolved in the solution;
(b) at least 1.0 w/v % but no greater than 10.0 w/v % hydroxy-propyl-β-cyclodextrin;
(c) about 0.2 w/v % to about 5.0 w/v % polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; and
(d) water;
wherein the pH of the solution is about 6.0 to about 7.8 and wherein the ophthalmic solution is free of polysorbate 80.

### Claim 2 (depends on 1)

The aqueous ophthalmic solution as in claim 1, wherein the solution comprises of about 0.75 w/v % brinzolamide.

### Claim 3 (depends on 1)

The aqueous ophthalmic solution as in claim 1, further comprises isotonizing agent; and a chelating agent.

### Claim 4

An aqueous ophthalmic solution comprising
(a) at least 0.5 w/v % brinzolamide but no greater than 0.95 w/v % of brinzolamide dissolved in the solution;
(b) at least 1.0 w/v % but no greater than 10.0 w/v % hydroxy-propyl-β-cyclodextrin;
(c) about 0.2 w/v % to about 5.0 w/v % polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer;
(d) about 0.1 w/v % to about 1.0 w/v % sodium chloride; and
(e) water;
wherein the pH of the solution is about 6.0 to about 7.8 and wherein the ophthalmic solution is free of polysorbate 80.

### Claim 5 (depends on 4)

The aqueous ophthalmic solution as in claim 4, wherein the solution comprises of about 0.75 w/v % brinzolamide.

### Claim 6 (depends on 4)

The aqueous ophthalmic solution as in claim 4, wherein the solution comprises of about 1.0 w/v % polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

### Claim 7 (depends on 4)

The aqueous ophthalmic solution as in claim 4, wherein the solution comprises of about 5.0 w/v % hydroxy-propyl-β-cyclodextrin.

### Claim 8 (depends on 4)

The aqueous ophthalmic solution as in claim 4, wherein the solution comprises of about 0.7 w/v % sodium chloride.

### Claim 9 (depends on 4)

The aqueous ophthalmic solution as in claim 4, wherein osmolality of the solution is of about 200 to about 400 mOsm/kg.

### Claim 10 (depends on 4)

The method of treating elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma, the method comprising: topically applying to an eye of the patient at least one drop of the solution of claim 4 to the eye.