# US 9,433,680 B2 · Topical compositions and methods for making and using same

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- Number: US 9,433,680 B2
- Document ID: US9433680B2
- Status: Granted
- Kind: B2
- Application number: 13/941,201
- Filed: 2013-07-12
- Published: 2014-07-31
- Granted: 2016-09-06
- Earliest claimed: 2013-01-31
- Assignees: Merz Pharmaceuticals, LLC
- Applicants: Merz Pharmaceuticals, LLC
- Inventors: Bhushan Hardas; Donna Dalton; Petra Scheppler; Anja Hensche; Peter Boderke
- Web page: https://patentgrep.com/patent/US9433680B2

## CPC

- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- 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 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 31/10: Antimycotics
- 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 relates to improved topical gel compositions comprising an active agent, and uses thereof.

## Claims

### Claim 1

A gel composition comprising from about 0.01 wt % to about 0.5 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % of a glycol solvent, from about 0.75 wt % to about 2.25 wt % of a hydroxyl cellulose, from about 1 wt % to less than about 10 wt % of a polysorbate solubilizing agent, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent; wherein the gel composition contains no alkyl alcohol, and wherein the composition contains no active agent in addition to the fluticasone, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % of a glycol solvent, from about 0.75 wt % to about 2.25 wt % of a hydroxy cellulose, from about 3 wt % to about 8 wt % of a polysorbate solubilizing agent, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent.

### Claim 3 (depends on 1)

The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 0.75 wt % to about 2.25 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent.

### Claim 4 (depends on 1)

The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent selected from an alcohol or glycol ether solubilizing agent, optionally from about 1 wt % to less than about 10 wt % of a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent.

### Claim 5 (depends on 1)

The gel composition of claim 1, wherein the fluticasone or a pharmaceutically acceptable salt or ester thereof is present in an amount of from about 0.01 wt % to about 0.1 wt %.

### Claim 6 (depends on 1)

The gel composition of claim 1, wherein the glycol solvent is present in an amount of about 18 wt % to about 22 wt %.

### Claim 7 (depends on 6)

The gel composition of claim 6, wherein the glycol solvent is propylene glycol.

### Claim 8 (depends on 1)

The gel composition of claim 1, wherein the hydroxy cellulose is present in an amount of from about 1.5 wt % to about 2.0 wt %.

### Claim 9 (depends on 1)

The gel composition of claim 1, wherein the hydroxy cellulose is hydroxyethyl cellulose.

### Claim 10 (depends on 1)

The gel composition of claim 1, wherein the polysorbate solubilizing agent is present in an amount of from about 3 wt % to about 8 wt %.

### Claim 11 (depends on 1)

The gel composition of claim 1, wherein the polysorbate solubilizing agent is Polysorbate 20.

### Claim 12 (depends on 1)

The gel composition of claim 1, wherein the polysorbate solubilizing agent is Polysorbate 80.

### Claim 13 (depends on 1)

The gel composition of claim 1, wherein the fluticasone, or pharmaceutically acceptable salt or ester thereof, is fluticasone propionate.

### Claim 14 (depends on 1)

The gel composition of claim 1, wherein the preservative is benzyl alcohol.

### Claim 15 (depends on 14)

The gel composition of claim 14, wherein the benzyl alcohol is present in an amount of about 1.0 wt %.

### Claim 16 (depends on 1)

The gel composition of claim 1, comprising from about 0.01 wt % to about 0.075 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent selected from an alcohol or glycol ether solubilizing agent, optionally from about 1 wt % to less than about 10 wt % of a third solubilizing agent selected from an alcohol or glycol ether solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent.

### Claim 17 (depends on 16)

The gel composition of claim 16, wherein the second solubilizing agent is a glycol ether solubilizing agent.

### Claim 18 (depends on 17)

The gel composition of claim 17, wherein the second solubilizing agent is diethylene glycol monoethylether.

### Claim 19 (depends on 18)

The gel composition of claim 18, wherein the diethylene glycol monoethylether is present in an amount of about 1 wt % to about 3 wt %.

### Claim 20 (depends on 19)

The gel composition of claim 19, wherein the fluticasone or pharmaceutically acceptable salt or ester thereof is fluticasone propionate.

### Claim 21 (depends on 20)

The gel composition of claim 20, wherein the preservative is benzyl alcohol.

### Claim 22 (depends on 21)

The gel composition of claim 21, wherein the benzyl alcohol is present in an amount of about 1.0 wt %.

### Claim 23 (depends on 1)

The gel composition of claim 1, comprising about 0.025 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, about 20 wt % propylene glycol, about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to about 3 wt % of a glycol ether solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent.

### Claim 24 (depends on 1)

The gel composition of claim 1, comprising about 0.025 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, about 20 wt % propylene glycol, about 1.75 wt % hydroxyethyl cellulose, about 5 wt % Polysorbate 20, about 1.5 wt % diethylene glycol monoethylether, water, 0.02 wt % ethylenediaminetetracetic acid (EDTA) or a salt thereof, and optionally a preservative, a pH adjuster, a fragrance, and a coloring agent.

### Claim 25 (depends on 24)

The gel composition of claim 24, wherein the fluticasone or pharmaceutically acceptable salt or ester thereof is fluticasone propionate.

### Claim 26 (depends on 25)

The gel composition of claim 25, wherein the preservative is benzyl alcohol.

### Claim 27 (depends on 26)

The gel composition of claim 26, wherein the benzyl alcohol is present in an amount of about 1.0 wt %.