Ophthalmic compositions containing galactomannan polymers and borate

• US 20030206970A1
• Filed: 05/14/2003
• Published: 11/06/2003
• Est. Priority Date: 07/29/1997
• Status: Active Grant

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Bahram Asgharian
• Inventors: Asgharian, Bahram
• Granted Patent: US 6,838,449 B2
• Time in Patent Office: Days
• US Class Current: 424/659
• 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. A topical ophthalmic composition comprising one or more galactomannan(s) and one or more borate compound(s), wherein the galactomannan and the borate compound are contained in the composition in concentrations effective to create a gel or partial gel when the composition is administered to an eye.

2. A composition of claim 1, wherein the concentration of the galactomannan is about 0.1 to 5% (w/v) and the concentration of the borate compound is about 0.05 to 5.0% (w/v).

3. A composition of claim 1, wherein the galactomannan is selected from the group consisting of guar gum, locust bean gum, tara gum and chemically modified derivatives thereof.

4. A composition of claim 1, wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.

5. A composition of claim 1, wherein the galactomannan is hydroxypropyl guar and the borate compound is boric acid.

6. A composition of claim 1, wherein the galactomannan is guar gum and the borate compound is boric acid.

7. A composition of claim 5, wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

8. A composition of claim 6, wherein the composition comprises guar gum in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

9. A composition of claim 1, further comprising one or more pharmaceutically active agent(s).

10. A composition of claim 9, wherein the concentration of the galactomannan is about 0.1 to 5% (w/v) and the concentration of the borate compound is about 0.05 to 5.0% (w/v).

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

anti-hypertensive, anti-glaucoma, neuro-protective, anti-allergy, muco-secretagogue, angiostatic, anti-microbial, pain relieving and anti-inflammatory agents.

12. A composition of claim 9, wherein the pharmaceutically active agent is selected from the group consisting of:

betaxolol, timolol, pilocarpine, carbonic anhydrase inhibitors, prostglandins;

post-surgical antihypertensive agents, apraclonidine;

ciprofloxacin, tobramycin;

naproxen, diclofenac, suprofen, ketorolac, tetrahydrocortisol, dexamethasone;

proteins and growth factors.

13. 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), one or more galactomannan(s) and one or more borate compound(s), wherein the galactomannan and the borate compound are contained in the composition in concentrations effective to create a gel or partial gel when the composition is administered to the eye.

14. A method of claim 13, wherein the composition comprises the galactomannan in a concentration of about 0.1 to 5% (w/v) and the borate compound in a concentration of about 0.05 to 5% (w/v).

15. A method of claim 13, wherein the galactomannan is selected from the group consisting of guar gum, locust bean gum, tara gum and chemically modified derivatives thereof.

16. A method of claim 13, wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.

17. A method of claim 13, wherein the galactomannan is hydroxypropyl guar and the borate compound is boric acid.

18. A method of claim 13, wherein the galactomannan is guar gum and the borate compound is boric acid.

19. A method of claim 17, wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

20. A method of claim 18, wherein the composition comprises guar gum in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

21. A composition of claim 13, wherein the pharmaceutically active agent(s) is/are selected from the group consisting of:

anti-hypertensive, anti-glaucoma, neuro-protective, anti-allergy, muco-secretagogue, angiostatic, anti-microbial, pain relieving and anti-inflammatory agents.

22. A composition of claim 13, wherein the pharmaceutically active agent is selected from the group consisting of:

betaxolol, timolol, pilocarpine, carbonic anhydrase inhibitors, prostglandins;

post-surgical antihypertensive agents, apraclonidine;

ciprofloxacin, tobramycin;

naproxen, diclofenac, suprofen, ketorolac, tetrahydrocortisol, dexamethasone;

proteins and growth factors.