Method and therapeutic/cosmetic topical compositions for the treatment of rosacea and skin erythema using a1-adrenoceptor agonists

Abstract

The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using α 1 -adrenergic receptor (α 1 -adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.

1 . A method for treating at least one condition selected from the group consisting of rosacea, acne, skin redness or other conditions characterized by discreet erythema of the skin in a subject in need of such treatment, comprising administering topically to said subject, for such period of time as is required to elicit the desired therapeutic response, a therapeutically or cosmetically effective amount of at least one alpha-1 adrenoreceptor agonist. 
     
     
         2 . The method according to  claim 1  wherein said, at least one alpha-1 agonist is topically applied to the skin. 
     
     
         3 . The method according to  claim 1 , wherein said, the alpha-1 adrenoreceptor agonist comprises oxymetazoline. 
     
     
         4 . The method according to  claim 1 , wherein said, the alpha-1 adrenoreceptor agonist comprises tetrahydrozoline. 
     
     
         5 . The method according to  claim 1 , wherein said, the alpha-1 adrenoreceptor agonist comprises nephazoline. 
     
     
         6 . The method according to  claim 1 , wherein said the alpha-1 adrenoreceptor agonist comprises xylometazoline. 
     
     
         7 . The method according to  claim 1 , wherein the treated condition comprises rosacea. 
     
     
         8 . The method according to  claim 1 , wherein the treated condition comprises acne. 
     
     
         9 . The method according to  claim 1 , wherein the treated condition comprises sunburn. 
     
     
         10 . The method according to  claim 1 , wherein the treated condition comprises chronic sun damage. 
     
     
         11 . The method according to  claim 1 , wherein the treated condition comprises other discreet erythemas. 
     
     
         12 . A composition for topical administration to the skin for treating rosacea comprising oxymetazoline HCl and an inert carrier. 
     
     
         13 . The method according to  claim 1 , wherein at least one alpha-1 adrenoreceptor agonist is co-administered with a therapeutically effective amount of at least one other active agent selected from the group consisting of antibacterial agents, antiparasitic agents, antifungal agents, anti-inflammatory agents, antihistamines, anti-pruriginous agents, anesthetics, antiviral agents, keratolytic agents, anti free-radical agents, antiseborrheic agents, antidandruff agents, antiacne agents, sunscreens and sun blocking agents, and active agents which modify at least one of cutaneous differentiation, proliferation, and pigmentation. 
     
     
         14 . The method according to  claim 1 , wherein said at least one alpha-1 adrenoreceptor agonist is administered in a pharmacologically or cosmetically acceptable form selected from the group consisting of solutions, gels, lotions creams, ointments, foams, emulsions, microemulsions, milks, serums, aerosols, sprays, dispersions, microcapsules, vesicles and microparticles thereof. 
     
     
         15 . The method according to  claim 1 , wherein said at least one alpha-1 adrenoreceptor agonist is administered in a pharmacologically or cosmetically acceptable form selected from the group consisting of soaps and cleansing bars. 
     
     
         16 . The method according to  claim 1 , wherein said skin redness, rosacea, or discreet erythema is elicited by at least one factor selected from the group consisting of intake of food, of hot or alcoholic drinks, temperature variations, heat, exposure to ultraviolet or infrared radiation, exposure to low relative humidity, exposure of the skin to strong winds or currents of air, exposure of the skin to surfactants, irritants, irritant dermatological topical agents, or cosmetics. 
     
     
         17 . An acne and rosacea treatment composition comprises: an effective amount of an acne and rosacea treatment composition to treat acne, which composition includes:
 (a) An acne treatment medication selected from the group consisting of benzoyl peroxide and salicylic acid;   (b) A vasoconstrictor selected from the group consisting of an alpha one adrenoreceptor agonist, and   (c) An inert carrier,   
       wherein, when said benzoyl peroxide is the acne treatment medication, it is in an amount of about 0.1% to about 20% based on the total weight of the composition, and when said salicylic acid is the acne treatment medication, it is in an amount of 0.05% to 15.0% based on the total weight of the composition;
 and, wherein said vasoconstrictor is in an amount of about 0.05% to about 20% by weight, based on the total weight of the composition. 
 
     
     
         18 . The acne treatment composition of  claim 17  wherein said acne treatment medication is benzoyl peroxide. 
     
     
         19 . The acne treatment composition of  claim 17  wherein said benzoyl peroxide is in an amount of about 1.0% to about 15% by total weight of the composition. 
     
     
         20 . The acne treatment composition of  claim 17  wherein said acne treatment medicine is salicylic acid. 
     
     
         21 . The acne treatment composition of  claim 17  wherein said salicylic acid is in an amount of about 0.1% to 10.0% by total weight of the composition. 
     
     
         22 . The acne treatment composition of  claim 17  wherein said alpha 1 vasoconstrictor is in a preferred amount of about 0.1% to about 10% by weight, based on the total weight of the composition. 
     
     
         23 . The acne treatment composition of  claim 17  wherein said vasoconstrictor is phenylephrine. 
     
     
         24 . The acne treatment composition of  claim 17  wherein said vasoconstrictor comprises oxymetazoline hydrochloride.