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Last Updated: October 29, 2020

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Claims for Patent: 9,072,661

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Summary for Patent: 9,072,661
Title:Injectable ibuprofen formulation
Abstract: The present invention provides a pharmaceutical composition comprising an aqueous solution of an ibuprofen solubilizing agent and ibuprofen, the ibuprofen solubilizing agent being in an effective amount such that the ibuprofen in the solution remains soluble at concentrations from 100 mg/mL to 5 mg/mL without undergoing a phase transition. The invention further provides a method of treating a condition chosen from pain, inflammation, fever, and/or patent ductus arteriosis, comprising administering to a patient in need thereof an effective amount of an aqueous solution a ibuprofen solubilizing agent and ibuprofen, the ibuprofen solubilizing agent being in an effective amount such that the ibuprofen in the solution remains soluble at concentrations from 100 mg/mL to 5 mg/mL without undergoing a phase transition, as well as a method for manufacturing the composition.
Inventor(s): Pavliv; Leo (Cary, NC), Vila; Andrew (Nashville, TN)
Assignee: Cumberland Pharmaceuticals Inc. (Nashville, TN)
Application Number:13/422,738
Patent Claims: 1. A pharmaceutical composition comprising an aqueous solution of water for injection, ibuprofen and an ibuprofen solubilizing agent consisting of tribasic sodium phosphate, wherein the molar ratio of tribasic sodium phosphate to ibuprofen is greater than 0.65:1 to about 0.9:1 and ibuprofen is in a concentration from about 4 mg/mL to about 100 mg/mL, said aqueous solution being suitable for parenteral administration.

2. The pharmaceutical composition of claim 1, wherein the tribasic sodium phosphate is in a molar ratio to ibuprofen of about 0.9:1.

3. The pharmaceutical composition of claim 1, which shows no detectable chemical degradation after incubation for one month at 40.degree. C.

4. The pharmaceutical composition of claim 1, which is sterile filtered or terminally sterilized.

5. The pharmaceutical composition of claim 1, which can be stored at ambient conditions in prefilled polyolefin bags and remains clear and colorless for at least about 12 weeks.

6. The pharmaceutical composition of claim 1, which can be stored in a bag made from a pharmaceutically acceptable polymer for at least about 12 weeks at 4.degree. C.

7. The pharmaceutical composition of claim 1, which can be stored in a bag made from a pharmaceutically acceptable polymer for at least about 12 weeks at 25.degree. C.

8. The pharmaceutical composition of claim 1, which remains clear and colorless when stored in a bag made from a pharmaceutically acceptable polymer and exposed to a freeze-thaw cycle.

9. The pharmaceutical composition of claim 1, wherein the pH of the aqueous solution of ibuprofen is from about 6.8 to about 7.8.

10. The pharmaceutical composition of claim 1, which is contained in a bag made of a pharmaceutically acceptable polymeric material.

11. The pharmaceutical composition of claim 1, wherein the ibuprofen is in a concentration of about 10 mg/mL.

12. The pharmaceutical composition of claim 10, wherein the aqueous solution contained in the bag is 80 mL at an ibuprofen concentration of 10 mg/mL.

13. The pharmaceutical composition of claim 10, wherein the aqueous solution contained in the bag is 40 mL at an ibuprofen concentration of 10 mg/mL.

14. The pharmaceutical composition of claim 10, wherein the aqueous solution contained in the bag has an ibuprofen concentration from about 4 mg/mL to about 15 mg/mL and a volume selected from about 40 mL, about 50 ml, about 80 ml and about 100 mL.

15. A pharmaceutical composition, comprising a pre-filled bag for intravenous use containing from about 40 to about 100 ml of an aqueous solution of water for injection, an effective dose of ibuprofen together with an ibuprofen solubilizing agent consisting of tribasic sodium phosphate, the molar ratio of tribasic sodium phosphate to ibuprofen being greater than 0.65:1 to about 0.9:1 and the concentration of ibuprofen in the aqueous solution is from about 4 mg/mL to about 15 mg/mL.

16. The pharmaceutical composition of claim 15, wherein the ibuprofen is at a concentration of 10 mg/mL and is contained in the bag at a volume of 80 mL or 40 mL.

17. The pharmaceutical composition of claim 15, wherein the ibuprofen is at a concentration of 8 mg/mL and is contained in the bag at a volume of 100 mL or 50 mL.

18. The pharmaceutical composition of claim 15, wherein the pH of the aqueous solution of ibuprofen is from about 6.8 to about 7.8.

19. The pharmaceutical composition of claim 18, wherein the aqueous solution of ibuprofen contained in the bag is physically and chemically stable.

20. A method of treating one or more conditions chosen from pain, inflammation, fever, and patent ductus arteriosis comprising intravenously administering to a patient in need thereof an aqueous solution comprising water for injection, an effective dose of ibuprofen together with an ibuprofen solubilizing agent consisting of tribasic sodium phosphate, wherein the molar ratio of tribasic sodium phosphate to ibuprofen is from about 0.7:1 to about 0.9:1 and the concentration of ibuprofen in the aqueous solution is from about 4 mg/mL to about 15 mg/mL.

21. The method of claim 20, wherein the aqueous solution is administered from a pre-filled bag, glass bottle, or plastic bottle containing from about 40 to about 50 ml or from about 80 to about 100 ml of the aqueous solution and the concentration of ibuprofen in the aqueous solution is from about 4 mg/mL to about 15 mg/mL.

22. The method of claim 20, further comprising adjusting the pH of the aqueous solution to a pH from about 6.8 to about 7.8.

23. The method of claim 22, wherein the aqueous solution is sterile in the pre-filled bag, glass bottle or plastic bottle.

24. The pharmaceutical composition of claim 1, wherein the ibuprofen in the aqueous solution remains soluble at concentrations from 100 mg/mL to about 4 mg/mL without turning hazy and/or precipitating.

25. An aqueous solution of ibuprofen suitable for injection, comprising water for injection, from about 400 mg to about 800 mg ibuprofen, tribasic sodium phosphate, the molar ratio of tribasic sodium phosphate to ibuprofen being greater than 0.65:1 to about 0.9:1, and about 0.9% sodium chloride for injection, the concentration of ibuprofen in the aqueous solution from about 4 mg/mL to about 15 mg/mL, wherein the pH of the aqueous solution of ibuprofen from about 6.8 to about 7.8 and the ibuprofen is solubilized in the aqueous solution such that the solution is clear and colorless, without precipitate, and suitable for injection.

26. The aqueous solution of claim 25, which is contained in a bag, a glass vial, a plastic vial, or a bottle.

27. The aqueous solution of claim 25, wherein the concentration of ibuprofen in the aqueous solution is about 4 mg/mL.

28. A single-dose vial containing an ibuprofen solution suitable for injection, comprising from about 400 mg to about 800 mg ibuprofen, tribasic sodium phosphate in a molar ratio to ibuprofen from greater than 0.65:1 to about 0.9:1, the concentration of ibuprofen in the aqueous solution from about 70 mg/ml to about 100 mg/ml, wherein the pH of the aqueous solution of ibuprofen from about 6.8 to about 7.8 and the ibuprofen is solubilized in the aqueous solution such that the solution is clear and colorless, without precipitate, and suitable for injection.

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