Method for therapeutic treatment of rosacea

Patent metadata

Field	Value
Publication number	US-12295935-B2
Application number	US-202318123702-A
Country	US
Kind code	B2
Filing date	Mar 20, 2023
Priority date	Feb 19, 2019
Publication date	May 13, 2025
Grant date	May 13, 2025

Abstract

A regimen and a pharmaceutical composition for the treatment of a skin condition and/or skin affliction are described. The regimen includes topically applying to the skin of a subject in need of such treatment a pharmaceutical composition comprising about 2.5% w/w to about 10% w/w benzoyl peroxide as an active ingredient, and a pharmaceutically acceptable carrier or excipient.

First claim

What is claimed is:

1. A regimen for the therapeutic treatment of a skin condition and/or skin affliction, the regimen comprising topically applying to the skin of a subject in need of said treatment a pharmaceutical composition, the pharmaceutical composition comprising about 2.5% w/w to about 10% w/w benzoyl peroxide as an active ingredient, and a pharmaceutically acceptable carrier or excipient, wherein:
the benzoyl peroxide is not encapsulated within a microcapsule or microsphere consisting of a metal oxide or a semi-metal oxide; and
said pharmaceutical composition comprises a fatty phase and/or an oily phase that forms a barrier between the benzoyl peroxide and its surrounding environment in the composition.

2. The regimen of claim 1 , wherein said pharmaceutical composition comprises about 2.5% w/w to about 5% w/w of benzoyl peroxide.

3. The regimen of claim 1 , wherein the benzoyl peroxide is not encapsulated within a microcapsule.

4. The regimen of claim 1 , wherein after the topical application, skin irritation of the subject, and the amount of benzoic acid in the dermis of the skin of the subject, are decreased, compared to skin irritation of the subject and the amount of benzoic acid in the dermis of the skin of the subject, respectively, after topical application of a corresponding pharmaceutical composition without the fatty phase and/or the oily phase.

5. The regimen of claim 1 , wherein an amount of benzoic acid in the stratum corneum and the epidermis of the skin of the subject after treatment with said pharmaceutical composition is higher than an amount of benzoic acid in the dermis of the skin of the subject after treatment with said pharmaceutical composition.

6. The regimen of claim 1 , wherein the benzoyl peroxide is the sole active ingredient administered to the subject during the duration of the regimen.

7. The regimen of claim 1 , wherein the pharmaceutical composition comprises about 3% w/w or about 5% w/w of benzoyl peroxide.

8. The regimen of claim 1 , wherein the benzoyl peroxide is selected from a solid, solution or suspension form.

9. The regimen of claim 1 , wherein said pharmaceutical composition is an extended-release formulation.

10. The regimen of claim 9 , wherein the extended-release effect is obtained by encapsulation, microencapsulation, microspheres or coating.

11. The regimen of claim 1 , wherein irritation observed on the skin of the subject after treatment with said pharmaceutical composition remains constant over time.

12. The regimen of claim 9 , wherein the extended-release effect is obtained by the fatty phase and/or the oily phase that forms a barrier between the benzoyl peroxide and its surrounding environment in the composition.

13. The regimen of claim 1 , wherein the benzoyl peroxide is not encapsulated within a microcapsule comprising an inorganic polymer.

14. The regimen of claim 1 , wherein the pharmaceutical composition does not comprise a gelling agent.

15. The regimen of claim 1 , wherein:
the fatty phase and/or the oily phase is dispersed in an aqueous phase; or
the pharmaceutical composition comprises an aqueous phase dispersed in the fatty phase and/or the oily phase.

16. The regimen of claim 1 , wherein said pharmaceutical composition is a cream.

17. The regimen of claim 1 , wherein the irritation is reduced when evaluated on a 0-3 scale.

18. The regimen of claim 1 , wherein the skin condition and/or skin affliction is rosacea.

19. The regimen of claim 18 , wherein the rosacea is any of erythematotelangiectatic rosacea , papulopustular rosacea , phymatous rosacea or ocular rosacea.

20. The regimen of claim 1 , wherein the benzoyl peroxide is not encapsulated within a microcapsule or microsphere comprising a metal oxide or a semi-metal oxide.

21. A regimen for the therapeutic treatment of a skin condition and/or skin affliction, the regimen comprising topically applying to the skin of a subject in need of said treatment a pharmaceutical composition, the pharmaceutical composition comprising about 2.5% w/w to about 10% w/w benzoyl peroxide as an active ingredient, and a pharmaceutically acceptable carrier or excipient, wherein the benzoyl peroxide is encapsulated within a microcapsule, wherein said pharmaceutical composition is a cream, and wherein an amount of benzoic acid in the stratum corneum and the epidermis of the skin of the subject after treatment with said pharmaceutical composition is higher than an amount of benzoic acid in the dermis of the skin of the subject after treatment with said pharmaceutical composition.

22. The regimen of claim 21 , wherein the amount of benzoic acid in the stratum corneum and the epidermis of the skin of the subject is higher than the amount of benzoic acid in the dermis of the skin of the subject when measured by high-performance liquid chromatography (HPLC).

23. The regimen of claim 21 , wherein the amount of benzoic acid in the stratum corneum and the epidermis of the skin of the subject is higher than the amount of benzoic acid in the dermis of the skin of the subject when measured by HPLC about 24 hours following the application of the pharmaceutical composition to the skin of the subject.

24. The regimen of claim 21 , wherein the amount of benzoic acid in the stratum corneum and the epidermis of the skin of the subject is substantially higher than the amount of benzoic acid in the dermis of the skin of the subject after treatment with said pharmaceutical composition.

25. The regimen of claim 21 , wherein irritation observed on the skin of the subject after treatment with said pharmaceutical composition is reduced compared to after treatment with a corresponding pharmaceutical composition in which the benzoyl peroxide is not encapsulated within a microcapsule.

26. The regimen of claim 25 , wherein the irritation is reduced when evaluated on a 0-3 scale.

27. The regimen of claim 21 , wherein the microcapsule comprises an inorganic polymer.

28. The regimen of claim 21 , wherein the benzoyl peroxide is the sole active ingredient administered to the subject during the duration of the regimen.

29. The regimen of claim 21 , wherein the pharmaceutical composition comprises about 3% w/w or about 5% w/w of benzoyl peroxide.

30. The regimen of claim 21 , wherein the benzoyl peroxide is selected from a solid, solution or suspension form.

31. The regimen of claim 21 , wherein said pharmaceutical composition is an extended-release formulation.

32. The regimen of claim 21 , wherein the pharmaceutical composition does not comprise a gelling agent.

33. The regimen of claim 21 , wherein irritation observed on the skin of the subject after treatment with said pharmaceutical composition remains constant over time.

34. The regimen of claim 21 , wherein the skin condition and/or skin affliction is rosacea.

35. The regimen of claim 34 , wherein the rosacea is any of erythematotelangiectatic rosacea , papulopustular rosacea , phymatous rosacea or ocular rosacea.

36. A regimen for the therapeutic treatment of a skin condition and/or skin affliction, the regimen comprising topically applying to the skin of a subject in need of said treatment a pharmaceutical composition, the pharmaceutical compositi

Assignees

• Sol Gel Tech Ltd

Inventors

• Toledano Ofer
• Nov Ori

Classifications

• A61K9/10

  Dispersions; Emulsions · CPC title

• A61K9/50

  Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)} · CPC title

• A61P17/00

  Drugs for dermatological disorders · CPC title

• A61K9/107

  Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} · CPC title

• A61K9/06

  Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} · CPC title