US2013012482A1PendingUtilityA1

Intravenous formulation with water-soluble cocrystals of acetylsalicylic acid and theanine

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Assignee: THEAPRIN PHARMACEUTICALS INCPriority: May 8, 2009Filed: Sep 14, 2012Published: Jan 10, 2013
Est. expiryMay 8, 2029(~2.8 yrs left)· nominal 20-yr term from priority
A61P 9/00A61P 35/00A61K 31/60C07B 2200/13A61K 31/198C07C 67/52A61K 45/06C07C 231/22A61K 9/0019A61K 31/616A61K 9/14A61P 29/00A61K 9/08A61K 47/30
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Claims

Abstract

A water-soluble cocrystal composition contains a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from an alpha variant of theanine or a beta variant of theanine or other form of theanine.

Claims

exact text as granted — not AI-modified
1 . A water-soluble composition comprising:
 a cocrystal composition containing a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from the group consisting of an alpha variant of theanine and a beta variant of theanine.   
     
     
         2 . The composition of  claim 1 , wherein said alpha variant of theanine is selected from the group consisting of L-northeanine, D-northeanine, DL-northeanine, L-homotheanine, D-homotheanine, DL-homotheanine, L-bishomotheanine, D-bishomotheanine, and DL-bishomotheanine. 
     
     
         3 . The method of  claim 2 , wherein said composition is used in the treatment of a medical condition. 
     
     
         4 . The method of  claim 3 , wherein said treatment is a treatment selected from the group consisting of providing an anti-inflammatory effect, use in pain management, use as an anti-pyretic, and treatment of symptoms of premenstrual syndrome. 
     
     
         5 . The method of  claim 2 , wherein said composition is used in the prevention of a medical condition. 
     
     
         6 . The method of  claim 5 , wherein said prevention is substantial protection against hepatotoxic effects. 
     
     
         7 . The composition of  claim 1 , wherein said alpha variant of theanine is a homologous analog of theanine. 
     
     
         8 . The composition of  claim 1 , wherein said alpha variant of theanine contains a functional group selected from the group consisting of linear, cyclic, or branched alkyl and derivatives thereof; linear, cyclic, or branched alkenyl and derivatives thereof; and aromatic radicals and derivatives thereof. 
     
     
         9 . The composition of  claim 8 , wherein said aromatic radicals are aryl radicals. 
     
     
         10 . The composition of  claim 1 , wherein said theanine enantiomer is a racemic mixture of a beta variant of theanine containing a functional group selected from the group consisting of linear, cyclic, or branched alkyl groups and derivatives thereof; linear, cyclic, or branched alkenyl groups and derivatives thereof; and aromatic radicals and derivatives thereof. 
     
     
         11 . The composition of  claim 10 , wherein said aromatic radicals are aryl radicals. 
     
     
         12 . The composition of  claim 1 , wherein said theanine enantiomer is an S enantiomer of a beta variant of theanine containing a functional group selected from the group consisting of linear, cyclic, or branched alkyl groups and derivatives thereof; linear, cyclic, or branched alkenyl groups and derivatives thereof; and aromatic radicals and derivatives thereof. 
     
     
         13 . The composition of  claim 12 , wherein said aromatic radicals are aryl radicals. 
     
     
         14 . The composition of  claim 1 , wherein said theanine enantiomer is an R enantiomer of a beta variant of theanine containing a functional group selected from the group consisting of linear, cyclic, or branched alkyl groups and derivatives thereof; linear, cyclic, or branched alkenyl groups and derivatives thereof; and aromatic radicals and derivatives thereof. 
     
     
         15 . The composition of  claim 14  wherein said aromatic radicals are aryl radicals. 
     
     
         16 . A water-soluble composition comprising a cocrystal composition containing a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer made by a process comprising the steps of:
 providing a quantity of acetylsalicylic acid;   adding a quantity of a theanine enantiomer selected from the group consisting of an alpha variant of theanine and a beta variant of theanine to said quantity of acetylsalicylic acid to form a mixture comprising said quantity of acetylsalicylic acid and said enantiomer of theanine;   wetting said mixture; and   grinding said mixture for a length of time sufficient to produce a dried crystalline mass.   
     
     
         17 . The water-soluble composition of  claim 16 , wherein said alpha variant of theanine is selected from the group consisting of L-northeanine, D-northeanine, DL-northeanine, L-homotheanine, D-homotheanine, DL-homotheanine, L-bishomotheanine, D-bishomotheanine, and DL-bishomotheanine. 
     
     
         18 . A water-soluble composition comprising a cocrystal composition containing a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer made by a process comprising the steps of:
 providing a quantity of acetylsalicylic acid;   adding a quantity of a theanine enantiomer selected from the group consisting of an alpha variant of theanine and a beta variant of theanine to said quantity of acetylsalicylic acid to form a mixture comprising said quantity of acetylsalicylic acid and said quantity of a theanine enantiomer;   dissolving said mixture in a quantity of a first solvent to form a solution; and   drying said solution for a length of time sufficient to produce a dried crystalline mass of an aspirin-theanine cocrystal composition.   
     
     
         19 . The water-soluble composition of  claim 18 , wherein said alpha variant of theanine is selected from the group consisting of L-northeanine, D-northeanine, DL-northeanine, L-homotheanine, D-homotheanine, DL-homotheanine, L-bishomotheanine, D-bishomotheanine, and DL-bishomotheanine. 
     
     
         20 . A method of making a water-soluble aspirin-theanine cocrystal composition comprising the steps of:
 providing a quantity of acetylsalicylic acid;   adding a quantity of a theanine enantiomer selected from the group consisting of an alpha variant of theanine and a beta variant of theanine to said quantity of acetylsalicylic acid to form a mixture comprising said quantity of acetylsalicylic acid and said enantiomer of theanine;   wetting said mixture; and   grinding said mixture for a length of time sufficient to produce a dried crystalline mass.   
     
     
         21 . The method  claim 20 , wherein said alpha variant of theanine is selected from the group consisting of L-northeanine, D-northeanine, DL-northeanine, L-homotheanine, D-homotheanine, DL-homotheanine, L-bishomotheanine, D-bishomotheanine, and DL-bishomotheanine. 
     
     
         22 . A method of making a water-soluble aspirin-theanine cocrystal composition, comprising the steps of:
 providing a quantity of acetylsalicylic acid;   adding a quantity of a theanine enantiomer selected from the group consisting of an alpha variant of theanine and a beta variant of theanine to said quantity of acetylsalicylic acid to form a mixture comprising said quantity of acetylsalicylic acid and said quantity of a theanine enantiomer;   dissolving said mixture in a quantity of a first solvent to form a solution; and   drying said solution for a length of time sufficient to produce a dried crystalline mass of an aspirin-theanine cocrystal composition.   
     
     
         23 . The method of  claim 22 , wherein said alpha variant of theanine is selected from the group consisting of L-northeanine, D-northeanine, DL-northeanine, L-homotheanine, D-homotheanine, DL-homotheanine, L-bishomotheanine, D-bishomotheanine, and DL-bishomotheanine.

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