Compositions comprising lecithin oils and nsaids for protecting the gastrointestinal tract and providing enhanced therapeutic activity

Abstract

A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulsion for internal, oral, direct or topical administration.

We claim: 
     
         1 . A composition comprising:
 a non-steroidal anti-inflammatory drug (NSAID); and   a non-aqueous carrier comprising a phospholipid;   wherein the weight ratio of the NSAID to the non-aqueous carrier is relatively high.   
     
     
         2 . The composition according to  claim 1 , wherein the weight ratio of NSAID to non-aqueous carrier is about 10:1 to about 1:10. 
     
     
         3 . The composition according to  claim 1 , wherein the weight ratio of NSAID to non-aqueous carrier is about 2:1 to about 1:2. 
     
     
         4 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises 10 wt. % to 90 wt. % phospholipid. 
     
     
         5 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises 20 wt. % to 80 wt. % phospholipid. 
     
     
         6 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises 20 wt. % to 60 wt. % phospholipid. 
     
     
         7 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises a bio-compatible oil or a mixture of bio-compatible oils. 
     
     
         8 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises a lecithin oil, essential oil, vegetable oil, animal oils, vitamin A, vitamin D, vitamin E, fish oil, or mixtures and combinations thereof. 
     
     
         9 . The composition according to  claim 8 , wherein the vegetable oil comprises peanut oil, canola oil, avocado oil, safflower oil, olive oil, corn oil, soy bean oil, sesame oil, or mixtures and combinations thereof. 
     
     
         10 . The composition according to  claim 1 , wherein the non-aqueous carrier comprises a lecithin oil. 
     
     
         11 . The composition according to  claim 1 , wherein the phospholipid comprises a zwitterionic phospholipid. 
     
     
         12 . The composition of  claim 11 , wherein the zwitterionic phospholipid comprises phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, sphingomyelin, dipalmitoylphosphatidylcholine, or combinations thereof. 
     
     
         13 . The composition according to  claim 11 , wherein the zwitterionic phospholipid comprises phosphatidylcholine. 
     
     
         14 . A composition comprising:
 a non-steroidal anti-inflammatory drug (NSAID); and   a non-aqueous carrier comprising 10 wt. % to 90 wt. % phospholipid, wherein the weight ratio of the NSAID to the non-aqueous carrier is about 10:1 to about 1:10.   
     
     
         15 . The composition according to  claim 14 , wherein the weight ratio of NSAID to non-aqueous carrier is about 2:1 to about 1:2. 
     
     
         16 . The composition according to  claim 14 , wherein the non-aqueous carrier comprises 20 wt. % to 80 wt. % phospholipid. 
     
     
         17 . The composition according to  claim 14 , wherein the non-aqueous carrier comprises 20 wt. % to 60 wt. % phospholipid. 
     
     
         18 . The composition according to  claim 14 , wherein the non-aqueous carrier comprises a bio-compatible oil or a mixture of bio-compatible oils. 
     
     
         19 . The composition according to  claim 14 , wherein the non-aqueous carrier comprises a lecithin oil, essential oil, vegetable oil, animal oils, vitamin A, vitamin D, vitamin E, fish oil, or combinations thereof. 
     
     
         20 . The composition according to  claim 19 , wherein the vegetable oil comprises peanut oil, canola oil, avocado oil, safflower oil, olive oil, corn oil, soy bean oil, sesame oil, or mixtures and combinations thereof. 
     
     
         21 . The composition according to  claim 14 , wherein the non-aqueous carrier comprises a lecithin oil. 
     
     
         22 . The composition according to  claim 14 , wherein the phospholipid comprises a zwitterionic phospholipid. 
     
     
         23 . The composition of  claim 22 , wherein the zwitterionic phospholipid comprises phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, sphingomyelin, dipalmitoylphosphatidylcholine, or combinations thereof. 
     
     
         24 . The composition according to  claim 22 , wherein the zwitterionic phospholipid comprises phosphatidylcholine. 
     
     
         25 . A composition comprising:
 a non-steroidal anti-inflammatory drug (NSAID); and   a non-aqueous carrier comprising a soy lecithin oil and 20 wt. % to 80 wt. % phospholipid, wherein the weight ratio of the NSAID to the non-aqueous carrier is about 2:1 to about 1:2.