IP Library Granted Patent US 11,389,416
Granted Patent B2
US 11,389,416 · App. 17/502,899 · Granted Jul 19, 2022

Aqueous formulation comprising paracetamol and ibuprofen

Inventor: Thomas Jacobsen (Windhof, LU)
Assignee: Hyloris Pharmaceuticals SA
A61K31/192A61J1/10A61J1/2093A61K9/0019A61K9/08A61K31/167A61K47/20A61K47/26A61M5/1407A61M5/19
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Quick Facts
Patent No.
US 11,389,416
App. No.
17/502,899
Granted
Jul 19, 2022
Kind
B2
Abstract

An aqueous ibuprofen and paracetamol composition has a pH 6.3-7.3. The composition can be used as a medicament, especially for the treatment of pain and/or inflammation. The composition can be formulated for intravenous injection.

Claims (31)

1. An aqueous analgesic composition comprising ibuprofen and paracetamol having a pH at the time of preparation (t 0 ) that is between 6.3 and 6.8, inclusive, wherein the ibuprofen and the paracetamol remain in solution for at least 6 months at 25±2° C. and 40±5% relative humidity.

2. The aqueous analgesic composition of claim 1 , wherein after one year of storage at 25±2°C. and 40±5% relative humidity, the level of 4-aminophenol in the composition is below 0.05% and the level of 4-nitrophenol in the composition is below 0.05%.

3. The aqueous analgesic composition of claim 1 , wherein the pH six months after the time of preparation is no higher than 7.3.

4. The aqueous analgesic composition of claim 1 , further comprising an isotonic agent.

5. The aqueous analgesic composition of claim 4 , wherein the isotonic agent is mannitol.

6. The aqueous analgesic composition of claim 1 , further comprising cysteine.

7. The aqueous analgesic composition of claim 1 , having a dissolved oxygen content below 2 ppm.

8. The aqueous analgesic composition of claim 2 , wherein the pH six months after the time of preparation is no higher than 7.3.

9. The aqueous analgesic composition of claim 2 , further comprising an isotonic agent.

10. The aqueous analgesic composition of claim 9 , wherein the isotonic agent is mannitol.

11. The aqueous analgesic composition of claim 2 , further comprising cysteine.

12. The aqueous analgesic composition of claim 2 , having a dissolved oxygen content below 2 ppm.

13. The aqueous analgesic composition of claim 8 , further comprising an isotonic agent.

14. The aqueous analgesic composition of claim 13 , wherein the isotonic agent is mannitol.

15. The aqueous analgesic composition of claim 8 , further comprising cysteine.

16. The aqueous analgesic composition of claim 8 , having a dissolved oxygen content below 2 ppm.

17. The aqueous analgesic composition of claim 10 , wherein the mass ratio (w/w) of mannitol:

paracetamol is between 2:1 and 6:1.

18. The aqueous analgesic composition of claim 17 , wherein the mass ratio (w/w) of mannitol:

paracetamol is between 3:1 and 5:1.

19. The aqueous analgesic composition of claim 18 , wherein the mass ratio (w/w) of mannitol:

paracetamol is 4:1.

20. The aqueous analgesic composition of claim 2 further comprising cysteine hydrochloride.

21. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to paracetamol is between 0.010:1 and 0.040:1.

22. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to paracetamol is between 0.020:1 and 0.030:1.

23. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to paracetamol is 0.025:1.

24. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to ibuprofen is between 0.20:1 and 0.40:1.

25. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to ibuprofen is between 0.10:1 and 0.20:1.

26. The aqueous analgesic composition of claim 20 , wherein the mass ratio (w/w) of cysteine hydrochloride to ibuprofen is 0.08:1.

27. The aqueous analgesic composition of claim 1 , wherein the ratio of ibuprofen to paracetamol is 3 to 10 wt/wt.

28. The aqueous analgesic composition of claim 2 , wherein the ratio of ibuprofen to paracetamol is 3 to 10 wt/wt.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 18, 2022
From: JACOBSEN, THOMAS
To: EVERBRIGHT PHARMACEUTICALS S.A.R.L.
Reel/Frame 058677/0890 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE NAME PREVIOUSLY RECORDED AT REEL: 055504 FRAME: 0521. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT . Recorded Jan 18, 2022
From: JACOBSON, THOMAS
To: EVERBRIGHT S.A.R.L.
Reel/Frame 058753/0286 →
CHANGE OF NAME Recorded Jan 18, 2022
From: EVERBRIGHT S.A.R.L.
To: HYLORIS PHARMACEUTICALS SA
Reel/Frame 058757/0902 →
Priority Claims (1)
WO PCT/EP2014/065544 · Jul 18, 2014 · international
Continuity (3)
Continuation 16424274 · May 28, 2019
Division 15326958
Related Publication 20220031645A1 · Feb 3, 2022