Combinations of adapalene and benzoyl peroxide for treating acne lesions

• US 8,445,543 B2
• Filed: 11/30/2011
• Issued: 05/21/2013
• Est. Priority Date: 07/13/2006
• Status: Active Grant

• Current Assignee: Galderma Research And Development Snc (Nestle SA)
• Original Assignee: Galderma Research And Development Snc (Nestle SA)
• Inventors: Abou-Chacra Vernet, Marie-line, Gross, Denis, Loesche, Christian, Poncet, Michel
• Primary Examiner(s): Anderson, James D
• Assistant Examiner(s): SPRINGER, STEPHANIE K
• Application Number:
  US13/308,413
• Publication Number:
  US 20120136059A1
• Time in Patent Office: 538 Days
• Field of Search: None
• US Class Current: 514/725
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/194 having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• CPC Class Codes: A61K 31/327 Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: 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
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: 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
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Adapalene or a pharmaceutically acceptable salt thereof formulated into a pharmaceutical composition is useful for reducing the number of acne lesions, via daily topical application, in combination or in association with benzoyl peroxide (BPO); such treatment may be via administration of a pharmaceutical composition combining adapalene and BPO or by a concomitant application of two pharmaceutical compositions, one containing adapalene and the other containing BPO.

Claims

1. A regimen for the therapeutic treatment of acne lesions, the regimen comprising topically applying to the skin of a subject in need of said treatment, as active ingredients, 0.1% to 0.3% adapalene or a pharmaceutically acceptable salt thereof and 2.5% benzoyl peroxide, combined at fixed doses in a single formula that delivers said active ingredients together, wherein the adapalene or pharmaceutically acceptable salt thereof and the benzoyl peroxide are the only anti-acne active ingredients in said single formula, wherein the percentages of adapalene and benzoyl peroxide are percentages by weight relative to the total weight of said single formula, wherein said single formula is applied once daily for a period of 12 weeks, and wherein the net clinical benefit, expressed as success rate or reduction in total lesion counts in a group of such subjects, achieved by the single formula at week 8 is synergistic and numerically superior to the net clinical benefit achieved by the same dose of adapalene alone or of benzoyl peroxide alone at week 12.

2. The regimen of claim 1, wherein the single formula is a gel.

3. A regimen for the therapeutic treatment of acne lesions, the regimen comprising applying to the skin of a subject in need of said treatment, as active ingredients, 0.1% to 0.3% adapalene or a pharmaceutically acceptable salt thereof and 2.5% benzoyl peroxide, combined at fixed doses in a single formula that delivers said active ingredients together, wherein the adapalene or pharmaceutically acceptable salt thereof and the benzoyl peroxide are the only anti-acne active ingredients in said single formula, wherein the percentages of adapalene and benzoyl peroxide are percentages by weight relative to the total weight of said single formula, wherein said single formula is applied once daily for a period of 12 weeks, and wherein the net clinical benefit, expressed as success rate or reduction in total lesion counts in a group of such subjects, achieved by the single formula at week 1, 4 or 8 is synergistic and numerically superior to the net clinical benefit achieved by the same dose of adapalene alone or of benzoyl peroxide alone at week 4, 8 or 12, respectively.

4. The regimen of claim 3, wherein the single formula is a gel.

5. A regimen for the therapeutic treatment of acne lesions, the regimen comprising topically applying to the skin of a subject in need of said treatment, as active ingredients, 0.1% to 0.3% adapalene or a pharmaceutically acceptable salt thereof and 2.5% benzoyl peroxide, combined at fixed doses in a single formula that delivers said active ingredients together synergistically to reduce the number of non-inflammatory acne lesions by at least 40%, wherein the adapalene or pharmaceutically acceptable salt thereof and the benzoyl peroxide are the only anti-acne active ingredients in said single formula, wherein the percentages of adapalene and benzoyl peroxide are percentages by weight relative to the total weight of said single formula, wherein said single formula is applied once daily for a period of 12 weeks.

6. The regimen of claim 5, wherein the single formula is a gel.

7. A regimen for the therapeutic treatment of acne lesions, the regimen comprising applying to the skin of a subject in need of such treatment, as active ingredients, 0.1% to 0.3% adapalene or a pharmaceutically acceptable salt thereof and 2.5% benzoyl peroxide, combined at fixed doses in a single formula that delivers said active ingredients together synergistically to reduce the number of inflammatory lesions by at least 50%, wherein the adapalene or pharmaceutically acceptable salt thereof and the benzoyl peroxide are the only anti-acne active ingredients in said single formula, wherein the percentages of adapalene and benzoyl peroxide are percentages by weight relative to the total weight of said single formula, wherein said single formula is applied once daily for a period of 12 weeks.

8. The regimen of claim 7, wherein the single formula is a gel.

9. A regimen for the therapeutic treatment of acne lesions, the regimen comprising topically applying to the skin of a subject in need of said treatment, as active ingredients, 0.1% to 0.3% adapalene or a pharmaceutically acceptable salt thereof and 2.5% benzoyl peroxide, combined at fixed doses in a single formula that delivers said active ingredients together synergistically to reduce the number of total acne lesions by at least 40%, to reduce the number of non-inflammatory acne lesions by at least 40%, to reduce the number of inflammatory lesions by at least 50%, and to achieve, in a group of subjects, a degree of success of at least 20%, wherein the adapalene or pharmaceutically acceptable salt thereof and the benzoyl peroxide are the only anti-acne active ingredients in said single formula, wherein the percentages of adapalene and benzoyl peroxide are percentages by weight relative to the total weight of said single formula, wherein said single formula is applied once daily for a period of 12 weeks.

10. The regimen of claim 9, wherein the single formula is a gel.