Topical compositions comprising ascomycins

Abstract

The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin.

1 . A composition for topical administration of an ascomycin for treatment of skin disorders which composition comprises a carrier vehicle comprising 
 (i) means to retain water in the outer skin layer comprising a urea, an inorganic salt, or a carboxylic acid, and    (ii) means to hinder water evaporating from the skin.    
     
     
         2 . A composition for topical administration of 33-epi-chloro-33-desoxy-ascomycin which composition comprises a carrier vehicle comprising 
 (i) means to retain water in the outer skin layer, and    (ii) means to hinder water evaporating from the skin.    
     
     
         3 . A composition as claimed in    claim 1    or    2    wherein the means to retain water in the outer skin layer is an inorganic salt.  
     
     
         4 . A composition as claimed in any one of    claims 1    to    3    wherein the means to hinder water evaporating from the skin is a hydrocarbon.  
     
     
         5 . A composition as claimed in    claim 4    wherein the hydrocarbon comprises petrolatum, liquid paraffin, microcrystalline wax, solid paraffin, or a reaction product of paraffin and polyethylene.  
     
     
         6 . A composition as claimed in any preceding claim wherein the carrier vehicle further comprises 
 (iii) liquid means to solubilize ascomycin.    
     
     
         7 . A composition as claimed in    claim 6    wherein the liquid means comprises a wax, a fatty alcohol, a fatty acid, or a fatty oil.  
     
     
         8 . A composition as claimed in    claim 7    wherein the liquid means is isopropyl myristate.  
     
     
         9 . A composition as claimed in any preceding claim wherein the ascomycin is present in an amount of 0.1 to 2.0% by weight of the composition.  
     
     
         10 . A composition as claimed in any preceding claim wherein the means to retain water in the outer skin layer is present in an amount of 0.1 to 20% by weight of the composition.  
     
     
         11 . Use of the carrier vehicle as claimed in    claim 1   or 2 to enhance penetration of an ascomycin through human skin.  
     
     
         12 . Use of a composition according to any preceding claim in the preparation of a medicament for the treatment of inflammatory and hyperproliferative skin diseases and of cutaneous manifestations of immunologically-mediated diseases.  
     
     
         13 . Use of a composition according to any preceding claim in the preparation of a medicament for administering to the skin of a patient in need thereof.