Oxymetazoline compositions
The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.
1. A single use container comprising an aqueous ophthalmic, sterile, preservative-free formulation consisting of:
a) about 0.1 wt % oxymetazoline hydrochloride;
b) tonicity modifiers comprising sodium chloride, potassium chloride, calcium chloride, and magnesium chloride;
c) about 0.5 wt % to about 1.0 wt % of hypromellose or sodium carboxymethyl cellulose;
d) sodium acetate and sodium citrate;
e) hydrochloric acid; and
f) 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 15 cPs to 35 cPs, and
wherein the aqueous ophthalmic formulation has an osmolality of from about 290 to about 365 mOsm/kg.
2. The single use container of claim 1 , wherein the tonicity modifier comprises about 0.64 wt % of sodium chloride, about 0.075 wt % of potassium chloride, about 0.048 wt % of calcium chloride, and about 0.03 wt % of magnesium chloride.
3. The single use container of claim 1 , wherein the calcium chloride is calcium chloride dihydrate and the magnesium chloride is magnesium chloride hexahydrate.
4. The single use container of claim 1 , wherein the sodium acetate is sodium acetate trihydrate and the sodium citrate is sodium citrate dihydrate.
5. The single use container of claim 1 comprising about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate.
6. The single use container of claim 1 comprising about 0.5 wt % hypromellose.
7. The single use container of claim 1 comprising about 1.0 wt % sodium carboxymethyl cellulose.
8. The single use container of claim 1 , wherein the formulation has a pH range from about 6.3 to about 6.5.
9. The single use container of claim 1 , wherein the aqueous ophthalmic formulation has an osmolality of from about 290 to about 330 mOsm/kg.
10. The single use container of claim 1 , wherein the formulation is stable at a temperature of about 25° C. and about 40% or 60% relative humidity for a period of 24 months.
11. The single use container of claim 1 , wherein the formulation has a viscosity of about 26 cPs.
12. The single use container of claim 1 , wherein the fill of the container is about 0.3 mL.
13. The single use container of claim 1 , wherein the container is a low density polyethylene container.
14. The single use container of claim 1 , wherein the container delivers about 0.035 mg of oxymetazoline hydrochloride per drop.
15. The single use container of claim 1 , wherein the 0.1 wt % oxymetazoline hydrochloride is equivalent to about 0.09 wt % of oxymetazoline free base.
16. The single use container of claim 1 , wherein the formulation is aseptically prepared.
17. The single use container of claim 1 , wherein volume of the container is about 0.5 mL.
18. The single use container of claim 1 , wherein the container is in a foil pouch.
19. The single use container of claim 1 , wherein the container is in child resistant packaging.
20. The single use container of claim 1 , wherein the container is formed by a blow/fill/seal process.