# US 8,784,789 B2 · Aqueous liquid preparations and light-stabilized aqueous liquid preparations

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 8,784,789 B2
- Document ID: US8784789B2
- Status: Granted
- Kind: B2
- Application number: 10/500,354
- Filed: 2003-07-30
- Published: 2005-05-19
- Granted: 2014-07-22
- Earliest claimed: 2002-07-31
- Assignees: Senju Pharmaceutical Co., Ltd.
- Applicants: Masayo Higashiyama
- Inventors: Masayo Higashiyama
- Web page: https://patentgrep.com/patent/US8784789B2

## CPC

- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 9/0043: {Nose}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 47/02: Inorganic compounds
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 17/04: Antipruritics
- A61P 27/02: Ophthalmic agents
- A61P 27/14: Decongestants or antiallergics
- A61P 27/16: Otologicals
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided.

## Claims

### Claim 1

An aqueous liquid preparation consisting of, in an aqueous solution, an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; a water-soluble metal chloride in a light-stabilizing effective amount; water; and optionally at least one material selected from the group consisting of a buffer, a preservative, a chelating agent, and a flavor; wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 1.2 w/v %.

### Claim 2 (depends on 1)

The aqueous liquid preparation of claim 1, wherein the metal chloride is at least one kind selected from sodium chloride, potassium chloride and calcium chloride.

### Claim 3 (depends on 1)

The aqueous liquid preparation of claim 1, which is an acid addition salt of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid.

### Claim 4 (depends on 3)

The aqueous liquid preparation of claim 3, wherein the acid addition salt is monobenzenesulfonate.

### Claim 5 (depends on 1)

The aqueous liquid preparation of claim 1, wherein the aqueous liquid preparation has a pH in the range of 4-8.5.

### Claim 6 (depends on 1)

The aqueous liquid preparation of claim 1, which is an eye drop.

### Claim 7 (depends on 1)

The aqueous liquid preparation of claim 1, which is a nasal drop.

### Claim 8 (depends on 1)

The aqueous liquid preparation of claim 1, wherein the metal chloride is at least one kind selected from alkali metal chlorides and alkaline earth metal chlorides.

### Claim 9

An aqueous eye drop consisting of: (a) an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; (b) a water-soluble metal chloride; (c) sodium dihydrogen phosphate buffer; (d) a preservative; (e) water; and optionally (f) disodium edetate; wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 1.2 w/v %.

### Claim 10

An aqueous liquid preparation consisting of, in an aqueous solution, an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, a water-soluble metal chloride in a light-stabilizing effective amount, wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 1.2 w/v %, benzalkonium chloride, sodium dihydrogenphosphate dihydrate, sodium hydroxide and water.

### Claim 11 (depends on 9)

The aqueous eye drop of claim 9, wherein:
(i) the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof is (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid monobenzenesufonate;
(ii) the water-soluble metal chloride is sodium chloride; and
(iii) the sodium chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 0.8 w/v %.