# US 7,612,115 B2 · Aqueous pharmaceutical compositions

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- Number: US 7,612,115 B2
- Document ID: US7612115B2
- Status: Granted
- Kind: B2
- Application number: 11/374,450
- Filed: 2006-03-13
- Published: 2006-08-03
- Granted: 2009-11-03
- Earliest claimed: 2000-08-08
- Assignees: Wakamoto Pharmaceutical Co., Ltd.
- Inventors: Hidekazu Suzuki; Takahiro Wada; Masanobu Kirita; Masanobu Takeuchi
- Web page: https://patentgrep.com/patent/US7612115B2

## CPC

- A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61P 27/02: Ophthalmic agents
- A61P 31/04: Antibacterial agents
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/38: Cellulose; Derivatives thereof
- 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

## Abstract

The present invention has an object to provide an antibacterial aqueous pharmaceutical composition and an aqueous pharmaceutical composition which have a sufficiently low gelation temperature even when new quinolone antibacterial agents such as ofloxacin as the active ingredient and can be retained at the administration site for a long time by virtue of rapid viscosity increase after administration in spite of their being liquid at administration and thereby attain high availability of pharmaceutical agent. The present invention relates to an antibacterial aqueous pharmaceutical composition which comprises: 2.8 to 4 w/v % of methylcellulose, the 2 w/v % aqueous solution of which has a viscosity of 12 mPa·s or below at 20° C.; 1.5 to 2.3 w/v % of citric acid; 2 to 4 w/v % of polyethylene glycol; and 0.1 to 0.5 w/v % of ofloxacin.

## Claims

### Claim 1

An antibacterial aqueous pharmaceutical composition which comprises: 2.8 to 4 w/v % of methylcellulose, wherein 2 w/v % aqueous solution of said methylcellulose has a viscosity of 12 mPa·s or below at 20° C.;
1.5 to 2.3 w/v % of citric acid;
2 to 4 w/v % of polyethylene glycol; and
0.1 to 0.5 w/v % of ofloxacin.

### Claim 2

An antibacterial aqueous pharmaceutical composition which comprises:
2.8 to 4 w/v % of methylcellulose, wherein a 2 w/v % aqueous solution of said methylcellulose has a viscosity of 12 mPa·s or below at 20° C.;
1.5 to 2.3 w/v % of citric acid;
2 to 4 w/v % of polyethylene glycol;
and 0.1 to 0.5 w/v % of at least one kind of new quinolone antibacterial agent selected from the group consisting of ofloxacin, levofloxacin and moxifloxacin hydrochloride.

### Claim 3

An aqueous pharmaceutical composition which comprises:
2.3 to 8 w/v % of methylcellulose, wherein a 2 w/v % aqueous solution of said methylcellulose has a viscosity of 12 mPa·s or below at 20° C.;
0.14 to 4 w/v % of at least one kind of acid selected from the group consisting of multivalent carboxylic acid, lactic acid and gluconic acid; and
an effective amount of a pharmaceutical agent, wherein said pharmaceutical agent is at least one member selected from the group consisting of ciprofloxacin hydrochloride, norfloxacin, lomefloxacin hydrochloride, gatifloxacin, carteolol hydrochloride, betaxolol hydrochloride, timolol maleate, pilocarpine hydrochloride, isopropylunoproston, nipradirol, bromfenac sodium, pranoprofen, diclofenac sodium, ketotifen fumarate, acitazanolast, disodium cromoglicate, tranilast, bethametasone sodium phosphate, prednisolone acetate, fluorometolone, fluorescein sodium, gentamicin sulfate, prienoxine, cyclosporine A. acyclovir, tropicamide and phenylephrine hydrochloride.

### Claim 4

An aqueous pharmaceutical composition which comprises:
2.3 to 8 w/v % of methylcellulose, wherein 2 w/v % aqueous solution of said methylcellulose has a viscosity of 12 mPa·s or below at 20° C.;
0.5 to 13 w/v % of polyethylene glycol; and
an effective amount of a pharmaceutical agent, wherein said pharmaceutical agent is at least one member selected from the group consisting of ciprofloxacin hydrochloride, norfloxacin, lomefloxacin hydrochloride, gatifloxacin, carteolol hydrochloride, betaxolol hydrochloride, timolol maleate, pilocarpine hydrochloride, isopropylunoproston, nipradirol, bromfenac sodium, pranoprofen, diclofenac sodium, ketotifen fumarate, acitazanolast, disodium cromoglicate, tranilast, bethametasone sodium phosphate, prednisolone acetate, fluorometolone, fluorescein sodium, gentamicin sulfate, prienoxine, cyclosporine A, acyclovir, tropicamide and phenylephrine hydrochloride.

### Claim 5

An aqueous pharmaceutical composition which comprises:
2.3 to 8 w/v % of methylcellulose, wherein a 2 w/v % aqueous solution of said methylcellulose has a viscosity of 12 mPa·s or below at 20° C.;
0.14 to 4 w/v % of at least one kind of acid selected from the group consisting of multivalent carboxylic acid, lactic acid and gluconic acid;
0.5 to 13 w/v % of polyethylene glycol; and
an effective amount of a pharmaceutical agent, wherein said pharmaceutical agent is at least one member selected from the group consisting of ciprofloxacin hydrochloride, norfloxacin, lomefloxacin hydrochloride, gatifloxacin, carteolol hydrochloride, betaxolol hydrochloride, timolol maleate, pilocarpine hydrochloride, isopropylunoproston, nipradirol, bromfenac sodium, pranoprofen, diclofenac sodium, ketotifen fumarate, acitazanolast, disodium cromoglicate, tranilast, bethametasone sodium, phosphate, prednisolone acetate, fluorometolone, fluorescein sodium, gentamicin sulfate, prienoxine, cyclosporine A, acyclovir, tropicamide and phenylephrine hydrochloride.