Oxymetazoline compositions
The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.
1. An aqueous ophthalmic, sterile, preservative-free formulation comprising:
a) about 0.1 wt % oxymetazoline hydrochloride;
b) about 0.64 wt % sodium chloride;
c) about 0.075 wt % potassium chloride;
d) about 0.048 wt % calcium chloride;
e) about 0.03 wt % magnesium chloride;
f) about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate;
g) about 0.5 wt % hypromellose; and
wherein the aqueous ophthalmic formulation has a pH range from about 5.8 to about 6.8, and wherein the aqueous ophthalmic formulation has a viscosity of from about 15 cPs to about 35 cPs.
2. The ophthalmic formulation of claim 1 , wherein the 0.1 wt % oxymetazoline hydrochloride is equivalent to about 0.09 wt % of oxymetazoline free base.
3. The ophthalmic formulation of claim 1 , wherein the sodium acetate is sodium acetate trihydrate and the sodium citrate is sodium citrate dihydrate.
4. The ophthalmic formulation of claim 1 , wherein the formulation further comprises a pH adjuster.
5. The ophthalmic formulation of claim 4 , wherein the pH adjuster is hydrochloric acid.
6. The ophthalmic formulation of claim 1 , wherein the formulation has a pH range from about 6.3 to about 6.5.
7. The ophthalmic formulation of claim 1 , wherein the formulation further comprises water QS.
8. The ophthalmic formulation of claim 1 , wherein the formulation is aseptically prepared.
9. The ophthalmic formulation of claim 1 , wherein the formulation is stable at a temperature of from about 20° C. to about 30° C. and about 40% or 60% relative humidity for a period of at least 24 months.
10. The ophthalmic formulation of claim 1 , wherein the formulation has a viscosity of about 26 cPs.
11. The ophthalmic formulation of claim 1 , wherein the formulation is an eye drop.
12. The ophthalmic formulation of claim 1 , wherein the formulation is for topical application to the eye.
13. The ophthalmic formulation of claim 1 , wherein the calcium chloride is calcium chloride dihydrate and the magnesium chloride is magnesium chloride hexahydrate.
14. A single use container comprising the ophthalmic formulation of claim 1 .
15. A single use container comprising an aqueous ophthalmic, sterile, preservative-free formulation comprising:
a) about 0.1 wt % oxymetazoline hydrochloride;
b) about 0.64 wt % sodium chloride;
c) about 0.075 wt % potassium chloride;
d) about 0.048 wt % calcium chloride;
e) about 0.03 wt % magnesium chloride;
f) about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate;
g) about 0.5 wt % hypromellose;
h) a pH adjuster; and
i) water QS;
wherein the aqueous ophthalmic formulation has a pH range from about 5.8 to about 6.8, and wherein the aqueous ophthalmic formulation has a viscosity of from about 15 cPs to about 35 cPs.
16. The single use container of claim 15 , wherein the 0.1 wt % oxymetazoline hydrochloride is equivalent to about 0.09 wt % of oxymetazoline free base.
17. The single use container of claim 15 , wherein the sodium acetate is sodium acetate trihydrate and the sodium citrate is sodium citrate dihydrate.
18. The single use container of claim 15 , wherein the pH adjuster is hydrochloric acid.
19. The single use container of claim 15 , wherein the formulation has a pH range from about 6.3 to about 6.5.
20. The single use container of claim 15 , wherein the formulation is aseptically prepared.
21. The single use container of claim 15 , wherein the formulation is stable at a temperature of from about 20° C. to about 30° C. and about 40% or 60% relative humidity for a period of at least 24 months.
22. The single use container of claim 15 , wherein the formulation has a viscosity of about 26 cPs.
23. The single use container of claim 15 , wherein volume of the container is about 0.5 mL.
24. The single use container of claim 15 , wherein the fill of the container is about 0.3 mL.
25. The single use container of claim 15 , wherein the container is a low density polyethylene container.
26. The single use container of claim 15 , wherein the container is in a foil pouch.
27. The single use container of claim 15 , wherein the container is in child resistant packaging.
28. The single use container of claim 15 , wherein the container delivers about 0.035 mg of oxymetazoline hydrochloride per drop.
29. The single use container of claim 15 , wherein the calcium chloride is calcium chloride dihydrate and the magnesium chloride is magnesium chloride hexahydrate.
30. An aqueous ophthalmic, sterile, preservative-free formulation consisting of:
a) about 0.1 wt % oxymetazoline hydrochloride;
b) about 0.64 wt % sodium chloride;
c) about 0.075 wt % potassium chloride;
d) about 0.048 wt % calcium chloride;
e) about 0.03 wt % magnesium chloride;
f) about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate;
g) about 0.5 wt % hypromellose;
h) a pH adjuster; and
i) water QS;
wherein the aqueous ophthalmic formulation has a pH range from about 5.8 to about 6.8, wherein the aqueous ophthalmic formulation has a viscosity of from about 15 cPs to about 35 cPs and wherein the formulation is stable at a temperature of about 25° C. for 24 months.