Combination of brimonidine and timolol for topical ophthalmic use

• US 9,770,453 B2
• Filed: 02/22/2017
• Issued: 09/26/2017
• Est. Priority Date: 04/19/2002
• Status: Expired due to Term

• Current Assignee: Allergan Sales LLC (Abbvie Incorporated)
• Original Assignee: Allergan Sales LLC (Abbvie Incorporated)
• Inventors: Chang, Chin-Ming, Beck, Gary J., Pratt, Cynthia C., Batoosingh, Amy L.
• Primary Examiner(s): Baek, Bong-Sook
• Application Number:
  US15/439,112
• Publication Number:
  US 20170157138A1
• Time in Patent Office: 216 Days
• Field of Search: None
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/4168 having a nitrogen attached in position 2, e.g. clonidine
• CPC Class Codes: A61K 31/498 Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• CPC Class Codes: A61K 31/535 having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• CPC Class Codes: A61K 31/5377 not condensed and containing further heterocyclic rings, e.g. timolol
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/04 Artificial tears; Irrigation solutions
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: F21V 23/002 Arrangements of cables or conductors inside a lighting device, e.g. means for guiding along parts of the housing or in a pivoting arm
• CPC Class Codes: F21V 23/004 arranged on a substrate, e.g. a printed circuit board
• CPC Class Codes: F21V 23/023 Power supplies in a casing F21V23/003 takes precedence
• CPC Class Codes: G02B 6/0073 Light emitting diode [LED]

Abstract

Disclosed are pharmaceutical compositions comprising brimonidine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Claims

1. A method of treating a patient with glaucoma or ocular hypertension comprising topically administering twice daily to an affected eye a single composition comprising 0.2% w/v brimonidine tartrate and 0.68% w/v timolol maleate, wherein the method is as effective as the administration of 0.2% w/v brimonidine tartrate monotherapy three times per day and wherein the method reduces the incidence of one of more adverse events selected from the group consisting of conjunctival hyperemia, oral dryness, eye pruritus, allergic conjunctivitis, foreign body sensation, conjunctival folliculosis, and somnolence when compared to the administration of 0.2% w/v brimonidine tartrate monotherapy three times daily.

2. The method of claim 1, wherein the composition further comprises about 0.005% w/v benzalkonium chloride.

3. The method of claim 2, wherein the composition further comprises sodium phosphate monobasic monohydrate, sodium phosphate buffer, sodium hydroxide, hydrochloric acid, and water.

4. The method of claim 1, wherein the composition further comprises 0.005% w/v benzalkonium chloride, 0.43% w/v sodium phosphate monobasic monohydrate, 2.15% w/v sodium phosphate dibasic heptahydrate, sodium hydroxide, hydrochloric acid, and water.

5. The method of claim 4, wherein the composition has a pH of about 6.9.