IP Library Granted Patent US 11,311,515
Granted Patent B2
US 11,311,515 · App. 17/461,052 · Granted Apr 26, 2022

Oxymetazoline compositions

Inventors: Tina Devries (Bridgewater, NJ); David Jacobs (Bernardsville, NJ)
Assignee: RVL Pharmaceuticals, Inc.
A61K31/4164A61F9/0008A61K9/0048A61K47/02A61K47/12A61K47/38A61P27/02
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Quick Facts
Patent No.
US 11,311,515
App. No.
17/461,052
Granted
Apr 26, 2022
Kind
B2
Abstract

The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.

Claims (48)

1. A child-resistant packaging having a single use container enclosed therein, wherein the single use container comprises an aqueous ophthalmic, sterile, preservative-free formulation comprising:

a) about 0.1 wt % oxymetazoline or a pharmaceutically acceptable salt thereof;

b) sodium chloride, potassium chloride, calcium chloride, and magnesium chloride;

c) about 0.5 wt % hypromellose;

d) sodium acetate and sodium citrate;

e) hydrochloric acid; and

f) water,

wherein the formulation has a pH range from about 5.8 to about 6.8;

wherein the container delivers about 0.035 mg of oxymetazoline or a pharmaceutically acceptable salt thereof per drop; and

wherein the formulation has a viscosity of about 15 cPs to about 35 cPs.

2. The child-resistant packaging of claim 1 , wherein the packaging is a foil pouch.

3. The child-resistant packaging of claim 2 , wherein the foil pouch is a foil laminate pouch.

4. The child-resistant packaging of claim 1 , wherein the formulation has an osmolality of from about 290 to about 365 mOsm/kg.

5. The child-resistant packaging of claim 1 , wherein the container is formed by a blow/fill/seal process.

6. The child-resistant packaging of claim 1 , wherein the container is a low density polyethylene container.

7. The child-resistant packaging of claim 1 , wherein the pharmaceutically acceptable salt is oxymetazoline hydrochloride.

8. The child-resistant packaging of claim 1 , wherein the formulation 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.

9. The child-resistant packaging of claim 8 , wherein the calcium chloride is calcium chloride dihydrate and the magnesium chloride is magnesium chloride hexahydrate.

10. The child-resistant packaging of claim 1 , wherein the sodium acetate is sodium acetate trihydrate and the sodium citrate is sodium citrate dihydrate.

11. The child-resistant packaging of claim 1 , wherein the formulation comprises about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate.

12. The child-resistant packaging of claim 1 , wherein the formulation has a pH range from about 6.3 to about 6.5.

13. The child-resistant packaging of claim 1 , wherein the formulation maintains a pH range from about 5.8 to about 6.8, a viscosity from about 15 cPs to about 35 cPs, and an osmolality from about 290 to about 365 mOsm/kg for a period of 6 months.

14. The child-resistant packaging of claim 1 , wherein the formulation is aseptically prepared.

15. A child-resistant foil pouch having a single use low density polyethylene container enclosed therein, wherein the single use container comprises an aqueous ophthalmic, sterile, preservative-free formulation comprising:

a) about 0.1 wt % oxymetazoline hydrochloride;

b) sodium chloride, potassium chloride, calcium chloride, and magnesium chloride;

c) about 0.5 wt % hypromellose;

d) sodium acetate and sodium citrate;

e) hydrochloric acid; and

f) water,

wherein the formulation has a pH range from about 5.8 to about 6.8,

wherein the formulation has a viscosity of from about 15 cPs to about 35 cPs,

wherein the formulation has an osmolality of from about 290 to about 365 mOsm/kg, and

wherein the container delivers about 0.035 mg of oxymetazoline or a pharmaceutically acceptable salt thereof per drop.

16. The child-resistant foil pouch of claim 15 , wherein the foil pouch is a foil laminate pouch.

17. The child-resistant foil pouch of claim 15 , wherein the fill of the container is about 0.3 mL.

18. The child-resistant foil pouch of claim 15 , wherein volume of the container is about 0.5 mL.

19. The child-resistant foil pouch of claim 15 , wherein the container is formed by a blow/fill/seal process.

20. The child-resistant foil pouch of claim 15 , wherein the formulation comprises about 0.64 wt % of sodium chloride, about 0.075 wt % of potassium chloride, about 0.048 wt % of calcium chloride or calcium chloride dihydrate, and about 0.03 wt % of magnesium chloride or magnesium chloride hexahydrate.

21. The child-resistant foil pouch of claim 15 , wherein the sodium acetate is sodium acetate trihydrate and the sodium citrate is sodium citrate dihydrate.

22. The child-resistant foil pouch of claim 15 , wherein the formulation comprises about 0.39 wt % sodium acetate and about 0.17 wt % sodium citrate.

23. The child-resistant foil pouch of claim 15 , wherein the formulation maintains a pH range from about 5.8 to about 6.8, a viscosity from about 15 cPs to about 35 cPs, and an osmolality from about 290 to about 365 mOsm/kg for a period of 6 months.

24. The child-resistant packaging of claim 13 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range for a period of 12 months.

25. The child-resistant packaging of claim 13 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range for a period of 18 months.

26. The child-resistant packaging of claim 13 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range at a temperature of about 25° C. and about 60% relative humidity.

27. The child-resistant foil pouch of claim 23 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range for a period of 12 months.

28. The child-resistant foil pouch of claim 23 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range for a period of 18 months.

29. The child-resistant foil pouch of claim 23 , wherein the formulation maintains the pH range, the viscosity range and the osmolality range at a temperature of about 25° C. and about 60% relative humidity.

Assignments (4)
NOTICE OF GRANT OF SECURITY INTEREST IN PATENTS Recorded Nov 27, 2023
From: RVL PHARMACEUTICALS, INC.
To: ATHYRIUM OPPORTUNITIES IV ACQUISITION LP, AS ADMINISTRATIVE AGENT
Reel/Frame 065676/0617 →
CORRECTIVE ASSIGNMENT TO CORRECT THE THE RECEIVING PARTY DATA PREVIOUSLY RECORDED ON REEL 057393 FRAME 0621. ASSIGNOR(S) HEREBY CONFIRMS THE CHANGE OF NAME. Recorded Jun 9, 2022
From: REVITALID, INC.
To: RVL PHARMACEUTICALS, INC.
Reel/Frame 060555/0218 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2021
From: DEVRIES, TINA; JACOBS, DAVID
To: REVITALID, INC.
Reel/Frame 057357/0415 →
CHANGE OF NAME Recorded Sep 1, 2021
From: REVITALID, INC.
To: RVL PHARMCEUTICALS, INC.
Reel/Frame 057393/0621 →
Continuity (6)
Continuation 17154676 · Jan 21, 2021
Continuation 17064915 · Oct 7, 2020
Continuation 16715998 · Dec 16, 2019
Provisional Application 62844069 · May 6, 2019
Provisional Application 62843819 · May 6, 2019
Related Publication 20210386711A1 · Dec 16, 2021