Combination of brimonidine timolol for topical ophthalmic use

• US 7,030,149 B2
• Filed: 04/19/2002
• Issued: 04/18/2006
• Est. Priority Date: 04/19/2002
• Status: Expired due to Term

• Current Assignee: Allergan Sales LLC (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Chang, Chin-Ming, Beck, Gary J., Batoosingh, Amy L., Pratt, Cynthia C.
• Primary Examiner(s): Low, Christopher S. F.
• Assistant Examiner(s): KWON, BRIAN YONG S
• Application Number:
  US10/126,790
• Publication Number:
  US 20030199509A1
• Time in Patent Office: 1,460 Days
• Field of Search: 514/393, 514/398, 514/399, 514/236.2, 514/397, 514/226.2, 514/238.5, 514/238.8, 514/249, 514/643, 424/427
• US Class Current: 514/393
• 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 brimondine 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 glaucoma or ocular hypertension by topical administration of about 0.2% brimonidine by weight to an eye of a person in need thereof, said improvement comprising topically administering to said eye, in a single composition, about 0.2% brimonidine by weight and about 0.5% timolol by weight twice a day;

as the sole active agents;

wherein said method is as effective as administration of 0.5% timolol twice a day and 0.2% brimonidine three times a day to said eye, wherein the two compounds are administered in separate compositions.

2. The method of claim 1 wherein said composition further comprises from 0.001% to 0.01% benzalkonium chloride.

3. The method of claim 2 wherein said composition comprises about 0.005% benzalkonium chloride.

4. A method of reducing the number of daily topical ophthalmic doses of brimondine administered topically to an eye of a person in need thereof for the treatment of glaucoma or ocular hypertension from 3 to 2 times a day without loss of efficacy, wherein the concentration of brimonidine is 0.2% by weight, said method comprising administering said 0.2% brimonidine by weight and 0.5% timolol by weight in a single composition.