Preservative free brimonidine and timolol solutions
The present invention is directed to preservative-free solutions of brimonidine and timolol for lowering intra-ocular pressure and treatment of glaucoma.
1. A preservative free brimonidine and timolol composition for lowering intraocular pressure in a human patient comprising the following formulation: about 0.2% w/v brimonidine tartrate; about 0.68% w/v timolol maleate; about 2.15% w/v sodium phosphate dibasic heptahydrate; about 0.43% w/v sodium phosphate monobasic heptahydrate and water wherein the preservative free brimonidine and timolol composition dosed twice a day lowers intraocular pressure to a greater degree as compared to a second composition dosed twice a day comprising about 0.2% w/v brimonidine tartrate; about 0.68% w/v timolol maleate; about 0.005% benzalkonium chloride; about 2.15% w/v sodium phosphate dibasic heptahydrate; about 0.43% w/v sodium phosphate monobasic heptahydrate and water.
2. A preservative free brimonidine and timolol composition for lowering intraocular pressure in a human patient comprising the following formulation: 0.2% w/v brimonidine tartate; 0.68% w/v timolol maleate; about 2.15% w/v sodium phosphate dibasic heptahydrate; about 0.43% w/v sodium phosphate monobasic heptahydrate; hydrochloric acid, sodium hydroxide, and water and at a pH of about 6.9 wherein the preservative free brimonidine and timolol composition dosed twice a day results in fewer side effects of one selected from the group consisting of ocular pain, hyperemia, foreign body sensation, stinging or burning and dry eye sensation as compared to a second composition dosed twice a day comprising about 0.2% w/v brimonidine tartrate; about 0.68% w/v timolol maleate; about 0.005% benzalkonium chloride; about 2.15% w/v sodium phosphate dibasic heptahydrate; 0.43% w/v sodium phosphate monobasic heptahydrate, hydrochloric acid, sodium hydroxide and water and at a pH of about 6.9.
3. The preservative free composition of claim 1 wherein the timolol maleate is at 0.68% w/v.
4. A composition for use in the treatment of elevated intraocular pressure or glaucoma in a patient suffering therefrom comprising about 0.2% w/v brimonidine tartrate; about 0.68% w/v timolol maleate; about 2.15% w/v sodium phosphate dibasic heptahydrate; about 0.43% w/v sodium phosphate monobasic heptahydrate; hydrochloric acid, sodium hydroxide and water and at a pH of about 6.9 wherein the composition is preservative free.
5. The composition of claim 1 wherein the composition is a solution and is useful for treating glaucoma.
6. The composition of claim 1 wherein the composition is a solution and is contained in a unit dose kit form.
7. The composition of claim 4 wherein the composition is applied at least once a day.
8. The composition of claim 4 wherein the composition is applied at least twice a day.
9. The composition of claim 1 wherein the composition has greater bioavailability of brimonidine and timolol in the eye of the patient with fewer side-effects than brimonidine and timolol preserved with benzalkonium chloride.
10. A method of lowering intraocular pressure in a patient suffering from elevated intraocular pressure by administering the preservative free composition of claim 1 .
11. The composition of claim 2 wherein the preservative free composition dosed twice a day results in less hyperemia in the patient as compared to the composition preserved with brimonidine tartrate.
12. The composition of claim 2 wherein the preserved composition dosed twice a day results in less burning and stinging in the patient as compared to the composition preserved with brimonidine tartrate.
13. The composition of claim 2 wherein the preserved composition dosed twice a day results in less dry eye in the patient as compared to the composition preserved with brimonidine tartrate.
14. The composition of claim 4 wherein the composition is a solution.
15. The composition of claim 4 wherein the preserved composition has better efficacy in a patient as compared to the same composition preserved with 0.005% w/v benzalkonium chloride when both compositions are applied twice a day.
16. The composition of claim 15 wherein the preserved composition lowers intraocular pressure to a greater degree as compared to the same composition preserved with 0.005% w/v benzalkonium chloride when both compositions are applied twice a day.
17. The composition of claim 15 wherein the preserved composition results in fewer side effects as compared to the same composition preserved with 0.005% w/v benzalkonium chloride.