Ophthalmic aqueous composition

Patent metadata

Field	Value
Publication number	US-10758554-B2
Application number	US-201515523970-A
Country	US
Kind code	B2
Filing date	Nov 5, 2015
Priority date	Nov 7, 2014
Publication date	Sep 1, 2020
Grant date	Sep 1, 2020

Abstract

An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

First claim

What is claimed is:

1. An ophthalmic aqueous composition consisting of levofloxacin, a salt thereof, or a solvate thereof; phosphate ester of dexamethasone or a salt thereof as active ingredients and one or at least two isotonic agents; and benzalkonium chloride as additives; and optionally containing a buffer and a pH adjuster, wherein the ophthalmic aqueous composition is substantially free of sodium chloride and has a pH of 6.5 to 8.8.

2. The ophthalmic aqueous composition according to claim 1 , wherein the ophthalmic aqueous composition has an osmotic pressure ratio of 1.2 or less.

3. The ophthalmic aqueous composition according to claim 1 , comprising the isotonic agent(s) at such a concentration as to adjust the osmotic pressure of the ophthalmic aqueous composition to a range of 60 to 340 mOsm.

4. The ophthalmic aqueous composition according to claim 1 , comprising the isotonic agent(s) at such a concentration as to adjust the osmotic pressure of the ophthalmic aqueous composition to a range of 60 to 230 mOsm.

5. The ophthalmic aqueous composition according to claim 1 , wherein the isotonic agent(s) are a nonionic isotonic agent or an ionic isotonic agent.

6. The ophthalmic aqueous composition according to claim 5 , wherein the nonionic isotonic agent is a polyhydric alcohol.

7. The ophthalmic aqueous composition according to claim 6 , wherein the polyhydric alcohol is one or at least two selected from the group consisting of glycerin, propylene glycol, and polyethylene glycol.

8. The ophthalmic aqueous composition according to claim 5 , wherein the ionic isotonic agent is an inorganic salt.

9. The ophthalmic aqueous composition according to claim 8 , wherein the inorganic salt is boric acid or borax.

10. The ophthalmic aqueous composition according to claim 5 , wherein the ionic isotonic agent is selected from the group consisting of inorganic salts and organic salts.

11. The ophthalmic aqueous composition according to claim 5 , wherein the ionic isotonic agent comprises an inorganic salt.

12. The ophthalmic aqueous composition according to claim 1 , which is an eye drop.

13. An ophthalmic aqueous composition according to claim 1 , which contains a buffer and a pH adjuster.

14. An ophthalmic aqueous composition consisting of levofloxacin, a salt thereof, or a solvate thereof at a concentration of 0.5% to 1.5% (w/v); phosphate ester of dexamethasone or a salt thereof at a concentration of 0.025 to 0.2% (w/v); one or at least two isotonic agents; benzalkonium chloride at a concentration of 0.001 to 0.02% (w/v); a buffer; a pH adjuster; and water, wherein the ophthalmic aqueous composition is substantially free of sodium chloride,
the ophthalmic aqueous composition has a pH of 6.5 to 8.8, and
the ophthalmic aqueous composition has an osmotic pressure ratio of 0.3 to 1.2.

15. The ophthalmic aqueous composition according to claim 14 , wherein the ophthalmic aqueous composition has an osmotic pressure ratio of 0.3 to 0.8.

16. An ophthalmic aqueous composition consisting of levofloxacin, a salt thereof, or a solvate thereof; phosphate ester of dexamethasone or a salt thereof; one or at least two isotonic agents; benzalkonium chloride; a buffer; a pH adjuster; and water wherein the ophthalmic aqueous composition is substantially free of sodium chloride and has a pH of 6.5 to 8.8.

Assignees

• Santen Pharmaceutical Co Ltd
• Daiichi Sankyo Co Ltd

Inventors

• Endo Yoko
• Takahashi Kyohei
• UMEZAKI Shinya

Classifications

• A61K47/186

  Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide · CPC title

• A61K9/0048 Primary

  Eye, e.g. artificial tears · CPC title

• A61K47/02

  Inorganic compounds · CPC title

• A61K31/573

  substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title