Ethyleneoxide butyleneoxide block copolymer compositions

• US 9,175,249 B2
• Filed: 07/07/2010
• Issued: 11/03/2015
• Est. Priority Date: 07/07/2009
• Status: Active Grant

• Current Assignee: Alcon Research, LLC (Alcon Incorporated)
• Original Assignee: Alcon Research Limited (Nestle SA)
• Inventors: Davis, James W., Ketelson, Howard Allen, Meadows, David L.
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US12/831,890
• Publication Number:
  US 20110008276A1
• Time in Patent Office: 1,945 Days
• US Class Current: 1/1
• 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 31/736 Glucomannans or galactomannans, e.g. locust bean gum, guar gum
• CPC Class Codes: A61K 31/77 of oxiranes
• CPC Class Codes: 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
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• 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: C11D 1/008 Polymeric surface-active agents
• CPC Class Codes: C11D 3/222 Natural or synthetic polysaccharides, e.g. cellulose, starch, gum, alginic acid or cyclodextrin
• CPC Class Codes: C11D 3/48 Medical, disinfecting agents, disinfecting, antibacterial, germicidal or antimicrobial compositions
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention relates to compositions comprising ethyleneoxide butyleneoxide and a galactomannan such as guar. The compositions are particularly well suited for ophthalmic applications such as contact lens disinfection and rewetting. Methods for the treatment of dry eye using the compositions of the present invention are also contemplated.

Claims

1. A sterile, aqueous ophthalmic composition comprising an ethyleneoxide butyleneoxide (EO-BO) block copolymer of the formula (EO)_m(BO)_n and a galactomannan, and wherein m has an average value of 45 and n has an average value of 9 to 18.

2. A composition according to claim 1 wherein m has an average value of 45 and n has an average value of 9 to 11.

3. A composition according to claim 1 wherein said galactomannan is guar.

4. A composition according to claim 3 wherein said guar or guar derivative is selected from the group consisting of:

native guar, hydroxypropyl guar, and hydroxypropyl guar galactomannan.

5. A composition according to claim 1 wherein said EO-BO block copolymer is present at a concentration of 0.001 to 1.0% w/v.

6. A composition according to claim 1 wherein said EO-BO block copolymer is present at a concentration of 0.01 to 0.1% w/v.

7. A composition according to claim 1 wherein said galactomannan is present at a concentration of 0.01 to 2.0% w/v.

8. A composition according to claim 1 wherein said galactomannan is present at a concentration of 0.05 to 0.25% w/v.

9. A method of delivering a pharmaceutical agent to the eye which comprises topically administering to the eye a composition comprising one or more pharmaceutically active agent(s), an ethyleneoxide butyleneoxide block copolymer of the formula (EO)_m(BO)_n and a galactomannan, and wherein m has an average value of 45 and n has an average value of 9 to 18.

10. A composition according to claim 9, wherein the pharmaceutically active agent(s) is/are selected from the group consisting of:

anti-glaucoma agents, anti-angiogenesis agents;

anti-infective agents;

anti-inflammatory agents;

growth factors;

immunosuppressant agents; and

anti-allergic agents.