# US 11,439,652 B2 · Ophthalmic aqueous composition

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- Number: US 11,439,652 B2
- Document ID: US11439652B2
- Status: Granted
- Kind: B2
- Application number: 16/937,792
- Filed: 2020-07-24
- Published: 2020-11-12
- Granted: 2022-09-13
- Earliest claimed: 2014-11-07
- Assignees: Santen Pharmaceutical Co., Ltd.; Daiichi Sanyo Company, Limited
- Applicants: Santen Pharmaceutical Co., Ltd.; Daiichi Sankyo Company, Limited
- Inventors: Yoko Endo; Kyohei Takahashi; Shinya Umezaki
- Web page: https://patentgrep.com/patent/US11439652B2

## CPC

- A61K 31/661: Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion {or mevinphos}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/538: ortho- or peri-condensed with carbocyclic ring systems
- A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/186: {Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide}
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- C07J 5/0046: {substituted in position 17 alfa}
- C07C 31/18: Polyhydroxylic acyclic alcohols
- C08G 65/00: Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07J: STEROIDS (seco-steroids C07C)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS

## 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.

## Claims

### Claim 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.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 3)

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

### Claim 5 (depends on 3)

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.

### Claim 6 (depends on 3)

The ophthalmic aqueous composition according to claim 3, wherein the nonionic isotonic agent is a polyhydric alcohol.

### Claim 7 (depends on 6)

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.

### Claim 8 (depends on 1)

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

### Claim 9 (depends on 8)

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

### Claim 10 (depends on 1)

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.

### Claim 11 (depends on 9)

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).

### Claim 12 (depends on 11)

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

### Claim 13 (depends on 1)

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.

### Claim 14 (depends on 13)

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.