High concentration olopatadine ophthalmic composition
View Patent ↗The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis.
1. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
at least 0.67 w/v % olopatadine dissolved in the solution;
PEG having a molecular weight of 300 to 500;
polyvinylpyrrolidone;
hydroxypropyl-γ-cyclodextrin;
benzalkonium chloride; and
water.
2. A solution as in claim 1 further comprising borate.
3. A solution as in claim 2 further comprising a polyol.
4. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution;
2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500;
2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone;
at least 0.5 w/v % but no greater than 2.0 w/v % cyclodextrin derivative selected from the group consisting of SAE-β-cyclodextrin, HP-γ-cyclodextrin, HP-β-cyclodextrin and combinations thereof; and
water.
5. A solution as in claim 4 further comprising borate at a concentration of at least 0.18 w/v % but less than 0.5 w/v %.
6. A solution as in claim 5 further comprising a polyol.
7. A solution as in claim 6 wherein the polyol is propylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %.
8. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution;
2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500;
2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone;
at least 0.5 w/v % but no greater than 2.0 w/v % hydroxypropyl-γ-cyclodextrin; and
water.
9. A solution as in claim 8 further comprising borate at a concentration of at least 0.18 w/v % but less than 0.5 w/v %.
10. A solution as in claim 9 further comprising a polyol.
11. A solution as in claim 10 wherein the polyol is propylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %.
12. A method of treating at least one ocular allergy symptom in humans, the method comprising:
topically applying to an eye of a human an amount of the solution of claim 4 sufficient to treat the at least one ocular allergy symptom.
13. A method as in claim 12 wherein the step of topically applying the solution includes dispensing at least one drop of the solution to the eye.
14. A method as in claim 13 wherein the at least one ocular allergy symptom includes ocular itching.
15. A solution as in claim 1 further comprising hydroxypropylmethyl cellulose.
16. A solution as in claim 4 further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose.
17. A solution as in claim 8 further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose.
18. A solution as in claim 3 wherein the polyol is mannitol.
19. A solution as in claim 6 wherein the polyol is mannitol solution at a concentration that is at least 0.05 w/v % but no greater than 0.5 w/v %.
20. A solution as in claim 10 wherein the polyol is mannitol at a concentration that is at least 0.05 w/v % but no greater than 0.5 w/v %.
21. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution;
2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500;
2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone;
at least 0.5 w/v % but no greater than 2.0 w/v % hydroxypropyl-γ-cyclodextrin;
greater than 0.003 w/v % but less than 0.03 w/v % benzalkonium chloride; and
water;
wherein the pH of the solution is 6.0 to 7.8 and the osmolality of the solution is 200 to 400 mOsm/kg.
22. A solution as in claim 21 further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose.
23. A solution as in claim 22 wherein:
i) the concentration of PEG is at least 3.0 w/v % but no greater than 5.0 w/v %;
ii) the concentration of polyvinylpyrrolidone is at least 3.0 w/v % but no greater than 5.0 w/v %; and
iii) the concentration of hydroxypropyl methylcellulose is at least 0.3 w/v % but no greater than 0.5 w/v %.
24. A solution as in claim 23 further comprising:
at least 0.18 w/v % but less than 0.4 w/v % boric acid; and
at least 0.05 w/v % but no greater than 0.5 w/v % mannitol.
25. A method of treating ocular allergy symptoms in humans, the method comprising:
topically applying to an eye of a human an amount of the solution of claim 23 sufficient to treat ocular allergy symptoms.
26. A method as in claim 25 wherein the step of topically applying the solution includes dispensing at least one drop of the solution to the eye.
27. A method as in claim 26 wherein the ocular allergy symptoms include ocular itching.