Ophthalmic compositions containing galactomannan polymers and borate

• US 6,838,449 B2
• Filed: 05/14/2003
• Issued: 01/04/2005
• Est. Priority Date: 07/29/1997
• Status: Expired due to Term

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Inventors: Asgharian, Bahram
• Primary Examiner(s): Wilson, James O.
• Assistant Examiner(s): Khare, Devesh
• Application Number:
  US10/437,570
• Publication Number:
  US 20030206970A1
• Time in Patent Office: 601 Days
• Field of Search: 514/54, 514/310, 514/839, 514/912, 514/944, 536/123.1, 536/124, 536/128, 424/401, 424/402, 424/427, 424/659, 424/660, 507/209, 507/241, 507/271, 166/300, 166/308.5, 516/107
• US Class Current: 514/54
• 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 31/74 Synthetic polymeric materials
• CPC Class Codes: A61K 33/22 Boron compounds
• 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 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 25/00 Drugs for disorders of the nervous system
• 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: A61P 27/08 Mydriatics or cycloplegics
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 7/04 Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions to the eye.

Claims

1. An ocular lubricant composition, comprising:

0.1 to 5% (w/v) of one or more borate compounds selected from the group consisting of boric acid and pharmaceutically acceptable salts thereof;

0.05 to 5% (w/v) of one or more galactomannan polysaccharides having linear chains of (1-4)-β

-D-mannopyranosyl units with α

-D-galactopyranosyl units attached by (1-6) linkages; and

water;

wherein the composition does not contain a pharmaceutically active agent.

2. An ocular lubricant composition according to claim 1, wherein the ratio of D-galactose to D-mannose in the galactomannan polysaccharide is from 1:

2 to 1;

4.

3. An ocular lubricant composition according to claim 2, wherein the ratio of D-galactose to D-mannose is 1:

2.

4. An ocular lubricant composition according to claim 1, wherein the concentration of the one or more galactomannan polysaccharides is 0.1 to 3.0% (w/v), and the concentration of the one or more borate compounds is 0.1 to 2.0% (w/v).

5. An ocular lubricant composition according to any one of claims 1-4, wherein the composition is a solution having a slightly acidic to neutral pH.

6. An ocular lubricant composition according to any one of claims 1-4, wherein the composition is a solution having a pH of 6 to 7.

7. A method of lubricating or moisturizing an eye, which comprises topically applying to the eye an effective amount of an ocular lubricant composition according to any one of claims 1-4.

8. A method according to claim 7, wherein the composition is a solution and has a slightly acidic to neutral pH.

9. A method according to claim 7, wherein the composition is a solution and has a pH of 6 to 7.