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Last Updated: March 28, 2024

Claims for Patent: 8,129,431


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Summary for Patent: 8,129,431
Title:Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid
Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
Inventor(s): Sawa; Shirou (Kobe, JP), Fujita; Shuhei (Kakogawa, JP)
Assignee: Senju Pharmaceutical Co., Ltd. (Osaka, JP)
Application Number:10/525,006
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,129,431
Patent Claims: 1. An aqueous liquid preparation consisting essentially of the following two components, wherein the first component is 2-amino-3-(4-bromobenzoyl)phenylaceticacid or a pharmacologically acceptable salt thereof or a hydrate thereof, wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate and the second component is tyloxapol, wherein said liquid preparation is formulated for ophthalmic administration, and wherein when a quaternary ammonium compound is included in said liquid preparation, the quaternary ammonium compound is benzalkonium chloride.

2. The aqueous liquid preparation according to claim 1, wherein the first component is a 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt.

3. The aqueous liquid preparation according to claim 1, wherein the second component is tyloxapol and the pharmacologically acceptable salt of 2-amino-3-(4-bromobenzoyl)phenylacetic acid is a sodium salt , wherein the concentration of the tyloxapol is from about 0.01 w/v % to about 0.5 w/v %; and wherein the first component is a 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is from about 0.01 to about 0.5 w/v %.

4. The aqueous liquid preparation according to claim 3, wherein the concentration of the tyloxapol is from about 0.01 w/v % to about 0.3 w/v % and the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is from about 0.05 to about 0.2 w/v %.

5. The aqueous liquid preparation according to claim 4, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is about 0.1 w/v %.

6. The aqueous liquid preparation according to claim 4, wherein the concentration of the tyloxapol is about 0.02 w/v %.

7. The aqueous liquid preparation according to claim 1, wherein the formulation further includes one or more additives selected from the group consisting of a preservative, buffer, thickener, stabilizer, chelating agent, and pH controlling agent.

8. The aqueous liquid preparation according to claim 7, wherein said preservative is benzalkonium chloride; wherein said buffer is boric acid and/or sodium borate; wherein said thickener is polyvinylpyrrolidone; wherein said stabilizer is sodium sulfite; wherein said chelating agent is sodium edetate; and wherein said pH controlling agent is sodium hydroxide.

9. The aqueous liquid preparation according to claim 8, wherein the pH is from about 7 to about 9.

10. The aqueous liquid preparation according to claim 8, wherein the pH is from about 7.5 to about 8.5.

11. The aqueous liquid preparation according to claim 4, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is about 0.2 w/v %.

12. The aqueous liquid preparation according to claim 4, wherein the concentration of the tyloxapol is about 0.3 w/v %.

13. The aqueous liquid preparation according to claim 12, wherein the formulation further includes one or more additives selected from the group consisting of a preservative, buffer, thickener, stabilizer, chelating agent, and pH controlling agent.

14. The aqueous liquid preparation according to claim 13, wherein said preservative is benzalkonium chloride; wherein said buffer is boric acid and/or sodium borate; wherein said thickener is polyvinylpyrrolidone; wherein said stabilizer is sodium sulfite; wherein said chelating agent is sodium edetate; and wherein said pH controlling agent is sodium hydroxide.

15. The aqueous liquid preparation according to claim 11, wherein the concentration of the tyloxapol is about 0.02 w/v %.

16. The aqueous liquid preparation according to claim 15, wherein the formulation further includes one or more additives selected from the group consisting of a preservative, buffer, thickener, stabilizer, chelating agent, and pH controlling agent.

17. The aqueous liquid preparation according to claim 16, wherein said preservative is benzalkonium chloride; wherein said buffer is boric acid and/or sodium borate; wherein said thickener is polyvinylpyrrolidone; wherein said chelating agent is sodium edetate; and wherein said pH controlling agent is sodium hydroxide.

18. An aqueous liquid preparation consisting essentially of: (a) 2-amino-3-(4- bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof, wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate, (b) tyloxapol, (c) boric acid, (d) sodium tetraborate, (e) EDTA sodium salt, (f) benzalkonium chloride, (g) polyvinylpyrrolidone, (h) sodium sulfite, wherein said liquid preparation is formulated for ophthalmic administration, and wherein benzalkonium chloride is the only quaternary ammonium compound which is included in said liquid preparation.

19. The aqueous liquid preparation of claim 18, wherein (a) is a 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt.

20. The aqueous liquid preparation of claim 19, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is from about 0.01 to about 0.5 w/v % and the concentration of the tyloxapol is about 0.02 w/v %.

21. The aqueous liquid preparation of claim 20, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is about 0.01 w/v %.

22. The aqueous liquid preparation of claim 20, wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is about 0.1 w/v %.

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