# US 4,393,076 A · Anti-inflammatory and analgesic gel composition

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- Number: US 4,393,076 A
- Document ID: US4393076A
- Status: Granted
- Kind: A
- Application number: 06/348,887
- Filed: 1982-02-16
- Granted: 1983-07-12
- Earliest claimed: 1980-05-14
- Assignees: Hisamitsu Pharmaceutical Co., Inc.
- Inventors: Kanji Noda; Akira Nakagawa; Tetsuya Yamagata; Hiroyuki Ide
- Web page: https://patentgrep.com/patent/US4393076A

## CPC

- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- 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)

## Abstract

An anti-inflammatory analgesic gel composition comprising (1) ketoprofen and/or flurbiprofen as the effective ingredient, as well as (2) a glycol, lower alcohol, water and/or a mixture of a lower alcohol with water, (3) a gel-forming agent and, if desired, (4) a solubilizing agent and/or non-ionic surface-active agent as the ingredients of a gel base for the gel composition.

## Claims

### Claim 1

An anti-inflammatory and analgesic gel composition comprising, by weight, 0.5-10% of ketoprofen as the effective ingredient, 2-40% of a glycol selected from the group consisting of propylene glycol, butylene glycol, polyethylene glycol, polypropylene glycol, polyethylene glycol dodecyl ether and glycerine, 20-55% of water, up to 60% of a lower alcohol selected from the group consisting of ethanol, denatured ethanol, propanol and isopropanol, 0.5-5% of a gelling agent selected from the group consisting of carboxyvinyl polymers, hydroxycellulose, methylcellulose, carboxymethylcellulose, hydroxypropylcellulose and alginic acid-propylene glycol ester and 0.1-3% of a neutralizing agent selected from the group consisting of triethanolamine, diethylamine, triethylamine, diisopropylamine and diisopropanolamine.

### Claim 2 (depends on 1)

An anti-inflammatory and analgesic gel composition according to claim 1, further comprising up to 20% by weight of a solubilizing agent selected from the group consisting of propylene carbonate, diethyl sebacate, benzyl alcohol and diisopropyl adipate.

### Claim 3 (depends on 2)

An anti-inflammatory and analgesic gel composition according to claim 2, further comprising up to 15% by weight of a surface-active agent selected from the group consisting of sesquioleic acid sorbitan, trioleic acid sorbitan, monooleic acid sorbitan, monostearic acid polyethylene glycol, monooleic polyoxyethylenesorbitan, monolauric acid polyoxyethylenesorbitan, polyoxyethylene nonylphenyl ether, polyoxyethylenecetyl ether, polyoxyethylenelauryl ether and mixtures thereof.

### Claim 4 (depends on 1, 2, 3)

An anti-inflammatory analgesic gel composition according to claim 1, 2 or 3, characterized in that it is kept at a pH value of 4.5-7.0.

### Claim 5 (depends on 1, 2)

A method of improving the anti-inflammatory analgesic effects obtainable with the gel composition of claim 1, 2, or 3 which comprises topically applying said composition to the skin of animals and human beings.

### Claim 6 (depends on 1)

A method according to claim 1, wherein the gel composition is kept at a pH value of 4.5-7.0.

### Claim 7

A method of improving the anti-inflammatory analgesic effects of an inflammatory analgesic gel compositions which comprises topically applying said composition to the skin of animals and human beings, the gel composition comprising, by weight, 0.5-10% of ketoprofen as the effective ingredient, 2-40% of a glycol selected from the group consisting of propylene glycol, butylene glycol, polyethylene glycol, polypropylene glycol, polyethylene glycol dodecyl ether and glycerine, 20-55% of water, up to 60% of a lower alcohol selected from the group consisting of ethanol, denatured ethanol, propanol and isopropanol, 0.5-5% of a gelling agent selected from the group consisting of carboxyvinyl polymers, hydroxyethylcellulose, methylcellulose, carboxymethylcellulose, hydroxypropylcellulose and alginic acid-propylene glycol ester and 0.1-3% of a neutralizing agent selected from the group consisting of triethanolamine, diethylamine, triethylamine, diisopropylamine and diisopropanolamine.

### Claim 8 (depends on 7)

A method according to claim 7, wherein the gel composition further comprises up to 20% by weight of a solubilizing agent selected from the group consisting of propylene carbonate, diethyl sebacate, diisopropyl adipate and bezyl alcohol.

### Claim 9 (depends on 8)

A method according to claim 8, wherein the gel composition further comprises up to 15% by weight of a surface-active agent selected from the group consisting of sesquioleic acid sorbitan, trioleic acid sorbitan, monooleic acid sorbitan, monostearic acid sorbitan, monolauric acid sorbitan, monostearic acid polyethylene glycol, monooleic acid polyoxyethylenesorbitan, monolauric acid polyoxyethylenesorbitan, polyoxyethylenenonylphyenyl ether, polyoxyethylenecetyl ether, polyoxyethylenelauryl ether and mixtures thereof.

### Claim 10 (depends on 1)

An anti-inflammatory and analgesic gel composition according to claim 1, wherein the alcohol is comprises in an amount by weight of 20-45%.

### Claim 11 (depends on 4)

An anti-inflammatory and analgesic gel composition according to claim 4, characterized in that the pH value is in the range of 5.0-6.5.

### Claim 12 (depends on 5)

A method of improving the anti-inflammatory analgesic effects according to claim 5, wherein the alcohol is comprised in an amount by weight of 20-45% in the gel composition.

### Claim 13 (depends on 7)

A method of improving the anti-inflammatory analgesic effects according to claim 7, wherein the alcohol is comprised in an amount by weight of 20-45% in the gel composition.

### Claim 14 (depends on 6)

A method according to claim 6, wherein the pH value is in the range of 5.0-6.5%.

### Claim 15

An anti-inflammatory and analgesic gel composition comprising by weight, 3-7% of ketoprofen as the effective ingredient 2-40% of a glycol selected from the group consisting of propylene glycol, butylene glycol, polyethylene glycol, polypropylene glycol, polyethylene glycol dodecyl ether and glycerine, 20-55% of water, up to 60% of a lower alcohol selected from the group consisting of ethanol, denatured ethanol, propanol and isopropanol, 0.5-5% of a gelling agent selected from the group consisting of carboxyvinyl polymers, hydroxyethylcellulose, methylcellulose, carboxymethylcellulose, hydroxypropylcellulose and alginic acid-propylene glycol ester and 0.1-3% of a neutralizing agent selected from the group consisting of triethanolamine, diethylamine, triethylamine, diisopropylamine and diisopropanolamine.
