Use of low molecular weight amino alcohols in ophthalmic compositions
View Patent ↗The use of low molecular weight amino alcohols in ophthalmic compositions is described. These compounds have been found to enhance the efficacy of anti-microbial preservatives.
1. A method of enhancing the antimicrobial activity of an aqueous ophthalmic composition containing a borate compound selected from the group consisting of boric acid, pharmaceutically acceptable salts of boric acid, and combinations thereof, which comprises including 0.01 to 2.0% w/v of an amino alcohol having a molecular weight of 60 to 200 grams/mole in said composition.
2. A method according to claim 1 , wherein the method further comprises adding 0.01 to 5.0% w/v of a polyol to the composition to further enhance its antimicrobial activity.
3. A method according to claim 2 wherein the polyol comprises propylene glycol.
4. A method according to claim 2 , wherein the polyol is selected from the group consisting of mannitol, glycerin, xylitol, sorbitol, and combinations thereof.
5. A method according to claim 4 , wherein the polyol comprises sorbitol.
6. A method according to claim 5 , wherein the polyol further comprises propylene glycol.
7. A method according to claim 2 , wherein the borate concentration is 0.3 to 1.2% w/v and the polyol concentration is 0.6 to 2.0% w/v.
8. A method according to claim 1 , wherein the amino alcohol is selected from the group consisting of 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-methyl-1-propanol (DMAMP), 2-amino-2-ethyl-1,3-propanediol (AEPD), 2-amino-2-methyl-1,3-propanediol (AMPD), 2-amino-1-butanol (AB), and combinations thereof.
9. A method according to claim 8 , wherein the amino alcohol comprises AMP.
10. A method according to claim 9 , wherein the method further comprises adding 0.01 to 5.0% of a polyol to the composition to further enhance the antimicrobial activity of the composition.
11. A method according to claim 10 , wherein the borate concentration is 0.3 to 1.2% w/v and the polyol concentration is 0.6 to 2.0% w/v.
12. A method according to claim 10 , wherein the polyol comprises propylene glycol.
13. A method according to claim 10 , wherein the polyol is selected from the group consisting of mannitol, glycerin, xylitol, sorbitol, and combinations thereof.
14. A method according to claim 13 , wherein the polyol comprises sorbitol.
15. A method according to claim 14 , wherein the polyol further comprises propylene glycol.
16. A method according to claim 1 , wherein the composition does not contain a conventional anti-microbial preservative.
17. A method according to claim 16 , wherein the composition is adapted for use as an artificial tear.
18. A method according to claim 16 , wherein the composition is adapted for use as an ocular lubricant.
19. A method of enhancing the antimicrobial activity of an aqueous contact lens disinfecting solution that contains an antimicrobial agent in an amount effective to disinfect a contact lens, which comprises including the following components in said solution:
(a) 0.01 to 2.0% w/v of an amino alcohol having a molecular weight of 60 to 200 grams/mole; and
(b) a borate/polyol buffer system, said buffer system comprising a borate compound in an amount of 0.01 to 2.0% w/v and a polyol in an amount of 0.01 to 5.0% w/v.
20. A method according to claim 19 , wherein the borate compound is selected from the group consisting of boric acid, pharmaceutically acceptable salts of boric acid, and combinations thereof; and the amino alcohol is selected from the group consisting of 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-methyl-1-propanol (DMAMP), 2-amino-2-ethyl-1,3-propanediol (AEPD), 2-amino-2-methyl-1,3-propanediol (AMPD), 2-amino-1-butanol (AB), and combinations thereof.
21. A method according to claim 20 , wherein the amino alcohol comprises AMP.
22. A method of enhancing the antimicrobial activity of an aqueous, multi-dose ophthalmic composition, which comprises including the following components in said composition:
(a) 0.1 to 2.0% w/v of an amino alcohol having a molecular weight of 60 to 200 grams/mole; and
(b) a borate/polyol buffer system, said buffer system comprising a borate compound in an amount of 0.01 to 2.0% w/v and a polyol in an amount of 0.01 to 5.0% w/v; wherein said composition is adapted for use as an artificial tear or ocular lubricant and does not contain a conventional anti-microbial preservative.
23. A method according to claim 22 , wherein the borate compound is selected from the group consisting of boric acid, pharmaceutically acceptable salts of boric acid, and combinations thereof; and the amino alcohol is selected from the group consisting of 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-methyl-1-propanol (DMAMP), 2-amino-2-ethyl-1,3-propanediol (AEPD), 2-amino-2-methyl-1,3-propanediol (AMPD), 2-amino-1-butanol (AB), and combinations thereof.
24. A method according to claim 23 , wherein the polyol comprises propylene glycol.
25. A method according to claim 23 , wherein the polyol is selected from the group consisting of mannitol, glycerin, xylitol, sorbitol, and combinations thereof.
26. A method according to claim 25 , wherein the amino alcohol comprises AMP.
27. A method according to claim 25 , wherein the polyol further comprises propylene glycol.
28. A method according to claim 27 , wherein the amino alcohol comprises AMP.
29. A method according to claim 22 , wherein the amino alcohol comprises AMP.