Compositions comprising avermectin/azelaic acid compounds useful for treating, e.g., rosacea

Abstract

Pharmaceutical/dermatological compositions useful for the prevention/treatment of disorders of the skin, especially rosacea, contain thus effective amounts of at least one avermectin compound, e.g., ivermectin, and at least one azelaic acid compound or salt or derivative thereof, formulated into a physiologically acceptable medium therefor.

1 . A pharmaceutical/dermatological topically applicable composition useful for the treatment of rosacea in the absence of irritation and intolerance, comprising anti-rosacea effective amounts of ivermectin and azelaic acid or salt thereof, formulated into a topically applicable, physiologically acceptable medium therefor. 
     
     
         2 . The pharmaceutical/dermatological composition as defined by  claim 1 , said ivermectin comprising from 0.001% to 10% by weight thereof. 
     
     
         3 . The pharmaceutical/dermatological composition as defined by  claim 2 , said azelaic acid or salt thereof comprising from 0.01% to 40% by weight thereof. 
     
     
         4 . The pharmaceutical/dermatological composition as defined by  claim 1 , formulated as a gel. 
     
     
         5 . The pharmaceutical/dermatological composition as defined by  claim 1 , formulated as an emulsion. 
     
     
         6 . The pharmaceutical/dermatological composition as defined by  claim 1 , formulated as an aqueous or aqueous-alcoholic solution, a lotion, a serum, a cream, an ointment, a milk, a suspension, a dispersion, microcapsules or microparticles. 
     
     
         7 . The pharmaceutical/dermatological composition as defined by  claim 1 , further comprising at least one active agent selected from the group consisting of antibiotics, anti-bacterial agents, anti-viral agents, anti-parasitic agents, anti-fungal agents, anaesthetics, analgesics, anti-allergic agents, retinoids, free-radical scavengers, anti-pruritic agents, keratolytic agents, anti-seborrhoeic agents, anti-histamines, sulfides, immunosuppressant products and anti-proliferative products. 
     
     
         8 . The pharmaceutical/dermatological composition as defined by  claim 1 , further comprising at least one additive selected from the group consisting of chelating agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, mineral acids, organic acids, mineral bases, organic bases, fragrances, essential oils, cosmetic active agents, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, calmatives, skin-protecting agents, pro-penetrating agents, gelling agents, and mixtures thereof. 
     
     
         9 . A regime or regimen for the treatment of rosacea, comprising topically administering to an individual in need of such treatment, anti-rosacea effective amounts of ivermectin and azelaic acid or salt thereof, formulated into a topically applicable, physiologically acceptable medium therefor. 
     
     
         10 . The pharmaceutical/dermatological composition as defined by  claim 1 , said ivermectin comprising from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof comprising from 1% to 20% by weight thereof. 
     
     
         11 . The pharmaceutical/dermatological composition as defined by  claim 5 , formulated as a cream. 
     
     
         12 . The pharmaceutical/dermatological composition as defined by  claim 10 , formulated as an emulsion. 
     
     
         13 . The pharmaceutical/dermatological composition as defined by  claim 12 , formulated as a cream. 
     
     
         14 . The pharmaceutical/dermatological composition as defined by  claim 10 , formulated as a gel. 
     
     
         15 . The pharmaceutical/dermatological composition as defined by  claim 12 , said ivermectin comprising from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof comprising from 1% to  20 % by weight thereof. 
     
     
         16 . The pharmaceutical/dermatological composition as defined by  claim 14 , comprising from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof comprising from 1% to 20% by weight thereof. 
     
     
         17 . A pharmaceutical/dermatological topically applicable composition useful for the treatment of rosacea in the absence of irritation and intolerance, comprising anti-rosacea effective amounts of ivermectin and azelaic acid or salt thereof, formulated into a topically applicable, physiologically acceptable medium therefor, said ivermectin and azelaic acid being the only therapeutic active anti-rosacea agents in the composition. 
     
     
         18 . The pharmaceutical/dermatological composition as defined by  claim 17 , said ivermectin comprising from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof comprising from 1% to 20% by weight thereof. 
     
     
         19 . The pharmaceutical/dermatological composition as defined by  claim 18 , formulated as an emulsion. 
     
     
         20 . The pharmaceutical/dermatological composition as defined by  claim 19 , formulated as a cream. 
     
     
         21 . The pharmaceutical/dermatological composition as defined by  claim 18 , formulated as a gel. 
     
     
         22 . A pharmaceutical/dermatological topically applicable composition useful for the treatment of rosacea in the absence of irritation and intolerance, consisting of anti-rosacea effective amounts of ivermectin and azelaic acid or salt thereof, formulated into a topically applicable, physiologically acceptable medium therefor. 
     
     
         23 . The pharmaceutical/dermatological composition as defined by  claim 22 , said ivermectin being from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof being from 1% to 20% by weight thereof. 
     
     
         24 . A pharmaceutical/dermatological topically applicable composition useful for the treatment of rosacea in the absence of irritation and intolerance, consisting of anti-rosacea effective amounts of ivermectin and azelaic acid or salt thereof, formulated into a topically applicable, physiologically acceptable medium therefor, said medium consisting of: (a) at least one member selected from the group consisting of water, alcohols, oils, fatty substances and waxes, and (b) at least one additive selected from the group consisting of chelating agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, mineral acids, mineral bases, organic acids, organic bases, fragrances, essential oils, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, calmatives, skin-protecting agents, pro-penetrating agents, gelling agents, emulsifiers, co-emulsifiers, and mixtures thereof. 
     
     
         25 . The pharmaceutical composition as defined by  claim 24 , said ivermectin being from 0.01% to 5% by weight thereof and said azelaic acid or salt thereof being from 1% to 20% by weight thereof. 
     
     
         26 . The pharmaceutical/dermatological composition as defined by  claim 25 , formulated as an emulsion. 
     
     
         27 . The pharmaceutical/dermatological composition as defined by  claim 26 , formulated as a cream. 
     
     
         28 . The pharmaceutical/dermatological composition as defined by  claim 25 , formulated as a gel. 
     
     
         29 . A regime or regimen for the treatment of rosacea, comprising topically administering to an individual in need of such treatment, an anti-rosacea effective amount of a composition as defined by  claim 17 . 
     
     
         30 . A regime or regimen for the treatment of rosacea, comprising topically administering to an individual in need of such treatment, an anti-rosacea effective amount of a composition as defined by  claim 22 . 
     
     
         31 . A regime or regimen for the treatment of rosacea, comprising topically administering to an individual in need of such treatment, an anti-rosacea effective amount of a composition as defined by  claim 24 .