Ophthalmic aqueous composition

Patent metadata

Field	Value
Publication number	US-11439652-B2
Application number	US-202016937792-A
Country	US
Kind code	B2
Filing date	Jul 24, 2020
Priority date	Nov 7, 2014
Publication date	Sep 13, 2022
Grant date	Sep 13, 2022

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 essentially of:
levofloxacin, a salt thereof, or a solvate thereof; phosphate ester of dexamethasone or a salt thereof as active ingredients;
one or at least two isotonic agents; and benzalkonium chloride as additives;
water; and
optionally containing at least one of a buffer, a pH adjuster, a nonionic surfactant, or a stabilizer.

2. The ophthalmic aqueous composition according to claim 1 , wherein the ophthalmic aqueous composition has a pH of 6.5 to 8.8.

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

4. The ophthalmic aqueous composition according to claim 3 , wherein the ionic isotonic agent is an inorganic salt.

5. The ophthalmic aqueous composition according to claim 3 , wherein the ionic isotonic agent is selected from the group consisting of inorganic salts and organic salts.

6. The ophthalmic aqueous composition according to claim 3 , 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 1 , wherein the levofloxacin, a salt thereof, or a solvate thereof is levofloxacin hydrates.

9. The ophthalmic aqueous composition according to claim 8 , wherein the levofloxacin hydrates are levofloxacin hemihydrates.

10. The ophthalmic aqueous composition according to claim 1 , wherein the ophthalmic aqueous composition contains sodium chloride at the content which does not adversely influence stability of the ophthalmic aqueous composition.

11. The ophthalmic aqueous composition according to claim 9 , wherein a concentration of levofloxacin hemihydrates is 0.5% to 1.5% (w/v); a concentration of the phosphate ester of dexamethasone, or a salt of the phosphate ester of dexamethasone is 0.025% to 0.2% (w/v); a concentration of benzalkonium chloride is 0.001% to 0.02% (w/v).

12. The ophthalmic aqueous composition according to claim 11 , wherein the composition optionally further contains a preservative.

13. A method for treating inflammatory diseases of an outer ocular area or an anterior segment or bacterial infections of an outer ocular area or an anterior segment, comprising applying the ophthalmic aqueous composition according to claim 1 to an eye in need thereof.

14. The method according to claim 13 , wherein the inflammatory diseases of an outer ocular area or an anterior segment or bacterial infections of an outer ocular area or an anterior segment are selected from the group consisting of blepharitis, dacryocystitis, stye, conjunctivitis, allergic conjunctivitis, phlyctenular conjunctivitis, spring catarrh, tarsadenitis, keratitis, blepharokeratoconjunctivitis, superior limbic keratoconjunctivitis, filamentary keratitis, epidemic keratoconjunctivitis, corneal ulcer, scleritis, episcleritis, iritis, iridocyclitis, anterior uveitis, and postoperative inflammation.

Assignees

• Santen Pharmaceutical Co Ltd
• Daiichi Sankyo Co Ltd
• Daiichi Sanyo Company Ltd

Inventors

• Endo Yoko
• Takahashi Kyohei
• UMEZAKI Shinya

Classifications

• A61K31/496

  Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title

• A61K9/08 Primary

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K31/5383

  ortho- or peri-condensed with heterocyclic ring systems · 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