Oral formulations of bipolar trans carotenoids

Abstract

The subject invention relates to a variety of formulations of bipolar trans carotenoids including pharmaceutical compositions for oral delivery of a bipolar trans carotenoid comprising i) a bipolar trans carotenoid, ii) a cyclodextrin, and iii) a coating. The invention also relates to preparation of such formulations and their uses.

1 - 23 . (canceled) 
     
     
         24 . A method of treating a mammal having peripheral vascular disease comprising administering to such mammal a therapeutically effective amount of an oral dosage pharmaceutical composition comprising a bipolar trans carotenoid salt having the structure:
   YZ-TCRO-ZY   
       where
 Y=a cation which can be the same or different, 
 Z=a polar group which can be the same or different and which is associated with the cation, and 
 TCRO=a linear transcarotenoid skeleton with conjugated carbon-carbon double bonds and single bonds and having pendant groups X, wherein the pendant groups X which can be the same or different, are (1) a linear or branched hydrocarbon group having 10 or less carbon atoms, or (2) a halogen. 
 
     
     
         25 . A method as in  claim 24 , wherein the bipolar trans carotenoid salt is trans sodium crocetinate. 
     
     
         26 . A method as in  claim 24 , wherein the pharmaceutical composition further comprises a cyclodextrin. 
     
     
         27 . A method as in  claim 24 , wherein the pharmaceutical composition further comprises a cyclodextrin and a coating, and is administered orally. 
     
     
         28 . A method of treating a mammal having a condition selected from multiple sclerosis, diabetes, cerebral palsey and critical limb ischemia comprising administering to such mammal a therapeutically effective amount of a pharmaceutical composition comprising a bipolar trans carotenoid salt having the structure:
   YZ-TCRO-ZY   
       where
 Y=a cation which can be the same or different, 
 Z=a polar group which can be the same or different and which is associated with the cation, and 
 TCRO=a linear transcarotenoid skeleton with conjugated carbon-carbon double bonds and single bonds and having pendant groups X, wherein the pendant groups X which can be the same or different, are (1) a linear or branched hydrocarbon group having 10 or less carbon atoms, or (2) a halogen. 
 
     
     
         29 . A method as in  claim 28 , wherein the bipolar trans carotenoid salt is trans sodium crocetinate. 
     
     
         30 . A method as in  claim 28 , wherein the pharmaceutical composition further comprises a cyclodextrin. 
     
     
         31 . A method as in  claim 28 , wherein the pharmaceutical composition further comprises a cyclodextrin and a coating, and is administered orally.