Ophthalmic compositions of brinzolamide

Patent metadata

Field	Value
Publication number	US-11298360-B2
Application number	US-201916470987-A
Country	US
Kind code	B2
Filing date	Apr 2, 2019
Priority date	Apr 25, 2018
Publication date	Apr 12, 2022
Grant date	Apr 12, 2022

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.

First claim

We 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.

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

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

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.

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

6. 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.

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

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

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

10. 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.

Assignees

• Shilpa Medicare Ltd

Inventors

• Andanayya Saraganachari
• Abhilash Narayanaswamy
• Reddy Sreenivasa
• Pradeep Shivakumar

Classifications

• A61K31/542 Primary

  ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title

• A61K47/40 Primary

  Cyclodextrins; Derivatives thereof · CPC title