`Claims
`
`1. A stable aqueous liquid
`preparation consisting
`essentially of:
`(a) a first component;
`(b) a second component;
`
`INDEPENDENT CLAIMS
`7. A stable aqueous liquid
`preparation consisting
`essentially of:
`(a) a first component;
`(b) a second component;
`
`13. A stable aqueous liquid
`preparation consisting
`essentially of:
`(a) a first component; and
`(b) a second component;
`
`wherein the first component is
`2-amino-3-(4-bromobenzoyl)
`phenylacetic acid or a
`pharmacologically acceptable
`salt thereof or a hydrate
`thereof;
`
`wherein the first component is
`2-amino-3-(4-bromobenzoyl)
`phenylacetic acid or a
`pharmacologically acceptable
`salt thereof or a hydrate
`thereof;
`
`wherein the first component is
`2-amino-3-(4-bromobenzoyl)
`phenylacetic acid or a
`pharmacologically acceptable
`salt thereof or a hydrate
`thereof;
`
`(c) boric acid;
`(d) sodium tetraborate; and
`(e) water;
`
`(c) boric acid;
`(d) sodium tetraborate; and
`(e) water;
`
`(c) boric acid;
`(d) sodium tetraborate; and
`(e) water;
`
`wherein the hydrate is at least
`one selected from a 1/2
`hydrate, 1 hydrate, and 3/2
`hydrate;
`
`wherein the hydrate is at least
`one selected from a 1/2
`hydrate, 1 hydrate, and 3/2
`hydrate;
`
`wherein the hydrate is at least
`one selected from a 1/2
`hydrate, 1 hydrate, and 3/2
`hydrate;
`
`the first component is the sole
`pharmaceutical active
`ingredient contained in the
`preparation and is present in
`the preparation at a
`concentration from about 0.05
`w/v % to about 0.2 w/v %;
`
`the first component is the sole
`pharmaceutical active
`ingredient contained in the
`preparation and is present in
`the preparation at a
`concentration from about 0.05
`w/v % to about 0.2 w/v %;
`
`the first component is the sole
`pharmaceutical active
`ingredient contained in the
`preparation and is present in
`the preparation at a
`concentration from about 0.05
`w/v % to about 0.2 w/v %;
`
`the second component is
`tyloxapol and is present in
`said liquid preparation in an
`amount sufficient to stabilize
`said first component; and
`
`wherein said stable liquid
`preparation is formulated for
`ophthalmic administration.
`
`the second component is
`tyloxapol;
`
`the second component is
`tyloxapol;
`
`wherein said stable liquid
`preparation is formulated for
`ophthalmic administration;
`
`provided that the liquid
`preparation does not include
`mannitol.
`
`wherein said stable liquid
`preparation is formulated for
`ophthalmic administration;
`and
`wherein the stable aqueous
`liquid preparation is characterized
`in that greater than about 90%
`of the original amount of the
`first component remains in the
`preparation after storage at
`about 60°C. for 4 weeks.
`
`1
`
`LUPIN EX 1025
`
`
`
`U.S. Patent No. 8,871,813
`Claims
`
`STABILITY
`
`9. The stable aqueous liquid preparation of claim 7; wherein the stable aqueous liquid
`preparation is characterized in that greater than about 92% of the original amount of the first
`component remains in the preparation after storage at about 60°C. for 4 weeks.
`
`19. The stable aqueous liquid preparation of claim 13; wherein the stable aqueous liquid
`preparation is characterized in that greater than about 90% of the original amount of the first
`component remains in the preparation after storage at about 60°C. for 4 weeks.
`
`20. The stable aqueous liquid preparation of claim 19; wherein the stable aqueous liquid
`preparation is characterized in that greater than about 92% of the original amount of the first
`component remains in the preparation after storage at about 60°C. for 4 weeks.
`
`PHARMACOLOGICALLY ACCEPTABLE SALTS
`
`2. The aqueous liquid preparation according to claim 1, wherein the aqueous liquid preparation
`further consists of sodium sulfite.
`
`3. The aqueous liquid preparation according to claim 1, wherein the first component is a 2-
`amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt.
`
`8. The aqueous liquid preparation according to claim 7, wherein the aqueous liquid preparation
`further consists of sodium sulfite.
`
`14. The aqueous liquid preparation according to claim 13, wherein the aqueous liquid
`preparation further consists of sodium sulfite.
`
`15. The aqueous liquid preparation according to claim 13, wherein the first component is a 2-
`amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt.
`
`pH
`
`5. The aqueous liquid preparation according to claim 1, wherein the pH of the aqueous liquid
`preparation is from about 7.5 to about 8.5.
`
`11. The aqueous liquid preparation according to claim 10, wherein the pH is from about 7.5 to
`about 8.5.
`
`17. The aqueous liquid preparation according to claim 13, wherein the pH is from about 7.5 to
`about 8.5.
`
`22. The aqueous liquid preparation according to claim 21, wherein the pH of the aqueous liquid
`preparation is from about 7.5 to about 8.5.
`
`2
`
`
`
`U.S. Patent No. 8,871,813
`Claims
`
`CONCENTRATION OF COMPONENTS
`
`4. The aqueous liquid preparation according to claim 1, wherein the concentration of tyloxapol is
`from about 0.01 w/v % to about 0.05 w/v %.
`
`6. The stable aqueous liquid preparation of claim 1; wherein the stable aqueous liquid
`preparation consists of:
`(a) 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt;
`(b) tyloxapol;
`(c) boric acid;
`(d) sodium tetraborate;
`(e) EDTA sodium salt;
`(f) polyvinylpyrrolidone;
`(g) sodium sulfite; and
`(h) water;
`wherein said liquid preparation is formulated for ophthalmic administration,
`wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is
`from about 0.02 w/v % to about 0.1 w/v %, and
`wherein the concentration of tyloxapol is from about 0.01 w/v % to about 0.05 w/v %.
`
`10. The aqueous liquid preparation according to claim 7;
`wherein the concentration of tyloxapol is from about 0.01 w/v % to about 0.05 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 0.05 w/v % to about 0.1 w/v %.
`
`12. The stable aqueous liquid preparation of claim 7; wherein the stable aqueous liquid
`preparation consists 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) polyvinylpyrrolidone;
`(g) sodium sulfite; and
`(h) water; and
`wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is
`from about 0.05 w/v % to about 0.1 w/v %, and
`the concentration of tyloxapol is about 0.02 w/v %.
`
`3
`
`
`
`U.S. Patent No. 8,871,813
`Claims
`
`16. The aqueous liquid preparation according to claim 13, wherein the concentration of tyloxapol
`is from about 0.01 w/v % to about 0.05 w/v % and the concentration of the 2-amino-3-(4-
`bromobenzoyl)phenylacetic acid sodium salt is from about 0.05 to about 0.1 w/v %.
`
`18. The stable aqueous liquid preparation of claim 13; wherein the stable aqueous liquid
`preparation consists 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) polyvinylpyrrolidone;
`(g) sodium sulfite; and
`(h) water;
`wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is
`from about 0.02 w/v % to about 0.1 w/v %, and
`the concentration of tyloxapol is from about 0.02 w/v % to about 0.05 w/v %.
`
`21. The stable aqueous liquid preparation according to claim 20,
`wherein the concentration of tyloxapol is from about 0.01 w/v % to about 0.05 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 0.05 w/v % to about 0.1 w/v %.
`
`23. The stable aqueous liquid preparation of claim 13; wherein the stable aqueous liquid
`preparation consists 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) polyvinylpyrrolidone;
`(g) sodium sulfite; and
`(h) water;
`wherein said liquid preparation is formulated for ophthalmic administration; and
`wherein the concentration of the 2-amino-3-(4-bromobenzoyl)phenylacetic acid sodium salt is
`from about 0.05 w/v % to about 0.1 w/v %.
`
`4
`
`
`
`U.S. Patent No. 8,871,813
`Claims
`
`NO PRESERVATIVES
`
`24. The aqueous liquid preparation of claim 1, wherein the aqueous liquid preparation does not
`include any preservative.
`
`25. The aqueous liquid preparation of claim 7, wherein the aqueous liquid preparation does not
`include any preservative.
`
`26. The aqueous liquid preparation of claim 13, wherein the aqueous liquid preparation does not
`include any preservative.
`
`ADDITIVES
`
`27. The aqueous liquid preparation according to claim 1, optionally further consisting of one or
`more additives selected from the group consisting of buffers, thickeners, stabilizers, chelating
`agents, and pH controlling agents.
`
`5
`
`