Topical pharmaceutical composition based on semifluorinated alkanes

Abstract

The invention provides liquid or semi-solid pharmaceutical compositions for topical administration comprising a semifluorinated alkane. The compositions are useful for the delivery of active ingredients into the deep layers of the skin or skin appendages. Various active ingredients may be incorporated, such as immunosuppressants, anti-infectives, antifungal agents, anti-inflammatory agents, and retinoids.

1 - 15 . (canceled) 
     
     
         16 . A topical composition comprising a local anesthetic agent and a semifluorinated alkane, wherein the local anesthetic agent is selected from the group consisting of benzocaine, butamben, dibucaine, lidocaine, oxybuprocaine, pramoxine, proparacaine, proxymetacaine, and tetracaine, and wherein the semifluorinated alkane is a semifluorinated alkane according to formula RFRH, wherein RF is a perfluorinated hydrocarbon segment with 20 or less carbon atoms and RH is a non-fluorinated hydrocarbon segment with 3 to 20 carbon atoms. 
     
     
         17 . The composition of  claim 16 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10. 
     
     
         18 . The composition of  claim 16 , wherein the local anesthetic agent is lidocaine. 
     
     
         19 . The composition of  claim 16 , further comprising a co-solvent selected from ethanol, acetone, ethyl acetate, isopropyl alcohol, glycerol, propylene glycol, pentylene glycol, polyethylene glycol, liquid paraffin, triglyceride oils, hydrofluorocarbons and liquid mono- or diglycerides. 
     
     
         20 . The composition of  claim 16 , being in liquid or semi-solid form. 
     
     
         21 . The composition of  claim 16 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F6H6 and F6H8, or wherein the semifluorinated alkane is F6H8. 
     
     
         22 . The composition of  claim 16 , wherein the composition delivers the local anesthetic into the deeper layers of the skin. 
     
     
         23 . The composition of  claim 16 , wherein the composition is packaged in bottle, spray bottles, or tubes. 
     
     
         24 . The composition of  claim 16 , wherein the composition consists of an effective amount of a local anesthetic, a semifluorinated alkane selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10, and optionally a co-solvent selected from ethanol, acetone, ethyl acetate, isopropyl alcohol, glycerol, propylene glycol, pentylene glycol, polyethylene glycol, liquid paraffin, triglyceride oils, hydrofluorocarbons and liquid mono- or diglycerides. 
     
     
         25 . A method for the treatment of a disease or a condition affecting the skin, comprising topically administering to the skin a composition according to  claim 16 . 
     
     
         26 . The method of  claim 25 , wherein the local anesthetic agent is lidocaine. 
     
     
         27 . The method of  claim 26 , wherein the composition delivers the local anesthetic into the deeper layers of the skin. 
     
     
         28 . A method of delivering an active ingredient to the deeper layers of the skin, comprising topically administering a composition according to  claim 16  to the skin, wherein the active ingredient is a local anesthetic agent, and wherein the active ingredient is delivered to deeper layers of the skin. 
     
     
         29 . The method of  claim 28 , wherein the local anesthetic agent is lidocaine. 
     
     
         30 . A method for the relief of pain or itching, comprising administering topically a composition according to  claim 16  to the skin. 
     
     
         31 . The method according to  claim 30 , wherein the pain or itching is caused by sunburn or other minor burns, insect bites or stings, or in preparation of minor surgical procedures. 
     
     
         32 . The method of  claim 30 , wherein the local anesthetic agent is lidocaine. 
     
     
         33 . The method of  claim 30 , wherein the local anesthetic is delivered into the deeper layers of the skin.