# US 2017/0281571 A1 · Methods for the treatment of rosacea

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- Number: US 2017/0281571 A1
- Document ID: US20170281571A1
- Status: Published application
- Kind: A1
- Application number: 15/496,344
- Filed: 2017-04-25
- Published: 2017-10-05
- Earliest claimed: 2012-11-27
- Assignees: Sol-Gel Technologies Ltd.
- Applicants: Sol-Gel Technologies Ltd.
- Inventors: Hanan SERTCHOOK; Ofer TOLEDANO; Haim BAR-SIMANTOV
- Web page: https://patentgrep.com/patent/US20170281571A1

## CPC

- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- 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 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 9/501: {Inorganic compounds}
- A61K 31/327: Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 31/7052: having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K 31/7056: containing five-membered rings with nitrogen as a ring hetero atom
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 9/00: Medicinal preparations characterised by special physical form {(nuclear magnetic resonance contrast preparations or magnetic resonance imaging contrast preparations A61K49/18; preparations containing radioactive substances A61K51/12)}
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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)

## Abstract

The present invention relates to pharmaceutical compositions for topical use (including also dermatological compositions), for treating skin conditions and afflictions, such as rosacea and symptoms and conditions associated there from.

## Claims

### Claim at position 1

1-20. (canceled)

### Claim 21

A method of treating rosacea in a patient in need thereof, comprising:
topically administering to a rosacea affected skin surface of said patient a composition comprising as a sole pharmaceutical active agent 1-10% by weight benzoyl peroxide in solid form,
wherein said composition has a benzoyl peroxide dissolution rate of less than about 80% weight/h as measured in a medium of a 55%:45% mixture of water and acetonitrile at ambient temperature.

### Claim 22 (depends on 21)

The method of claim 21, wherein the benzoyl peroxide dissolution rate is less than about 60% weight/h.

### Claim 23 (depends on 21)

The method of claim 21, wherein said benzoyl peroxide comprises 5% by weight of the composition.

### Claim 24 (depends on 21)

The method of claim 21, wherein said composition is a formulation selected from the group consisting of an oil based cream formulation, an aqueous based cream formulation, an oil-in-water emulsion, and a gel formulation.

### Claim 25 (depends on 24)

The method of claim 24, wherein said composition is an oil-in-water emulsion comprising a polyoxylstearate, a glycerylstearate and at least one fatty alcohol, wherein the ratio of the polyoxylstearate to the glycerylstearate is in the range of 0.1:10 to 10:0.1.

### Claim 26 (depends on 21)

The method of claim 21, wherein said benzoyl peroxide is encapsulated as a core of a microcapsule having a shell comprising at least one inorganic polymer, the core consisting of the solid benzoyl peroxide.

### Claim 27

A method of treating rosacea in a patient in need thereof, comprising:
topically administering to a rosacea affected skin surface of said patient a composition comprising as a sole pharmaceutical active agent 1-10% by weight benzoyl peroxide in solid form,
wherein said composition is administered once daily over 12 weeks and provides more than 20% success rate of treatment, the success rate being a 2-grade improvement over baseline in an Investigator Global Assessment (IGA).

### Claim 28 (depends on 27)

The method of claim 27, wherein said benzoyl peroxide comprises 5% by weight of the composition.

### Claim 29 (depends on 27)

The method of claim 27, wherein the success rate is about 30%.

### Claim 30 (depends on 27)

The method of claim 27, wherein said composition has a benzoyl peroxide dissolution rate of less than about 80% weight/h as measured in a medium of a 55%:45% mixture of water and acetonitrile at ambient temperature.

### Claim 31 (depends on 27)

The method of claim 27, wherein said composition is a formulation selected from the group consisting of an oil based cream formulation, an aqueous based cream formulation, an oil-in-water emulsion, and a gel formulation.

### Claim 32 (depends on 31)

The method of claim 31, wherein said composition is an oil-in-water emulsion comprising a polyoxylstearate, a glycerylstearate and at least one fatty alcohol, wherein the ratio of the polyoxylstearate to the glycerylstearate is in the range of 0.1:10 to 10:0.1.

### Claim 33 (depends on 27)

The method of claim 27, wherein said benzoyl peroxide is encapsulated as a core of a microcapsule having a shell comprising at least one inorganic polymer, the core consisting of the solid benzoyl peroxide.

### Claim 34

A method of treating rosacea in a patient in need thereof, comprising:
topically administering to a rosacea affected skin surface of said patient a composition comprising as a sole pharmaceutical active agent 1-10% by weight benzoyl peroxide in solid form,
wherein said treatment has an adverse events values of not more than 40%.

### Claim 35 (depends on 34)

The method of claim 34, wherein said benzoyl peroxide comprises 5% by weight of the composition.

### Claim 36 (depends on 34)

The method of claim 34, wherein said composition is administered once daily over 12 weeks and provides more than 20% success rate of treatment, the success rate being a 2-grade improvement over baseline in an Investigator Global Assessment (IGA).

### Claim 37 (depends on 38)

The method of claim 38, wherein said composition has a benzoyl peroxide dissolution rate of less than about 80% weight/h as measured in a medium of a 55%:45% mixture of water and acetonitrile at ambient temperature.

### Claim 38 (depends on 34)

The method of claim 34, wherein said composition is a formulation selected from the group consisting of an oil based cream formulation, an aqueous based cream formulation, an oil-in-water emulsion, and a gel formulation.

### Claim 39 (depends on 38)

The method of claim 38, wherein said composition is an oil-in-water emulsion comprising a polyoxylstearate, a glycerylstearate and at least one fatty alcohol, wherein the ratio of the polyoxylstearate to the glycerylstearate is in the range of 0.1:10 to 10:0.1.

### Claim 40 (depends on 21)

The method of claim 21, wherein said benzoyl peroxide is encapsulated as a core of a microcapsule having a shell comprising at least one inorganic polymer, the core consisting of the solid benzoyl peroxide.
