Thioureylene liquid compositions

Abstract

The present invention relates to novel liquid compositions and formulations containing a thioureylene compound, a polysaccharide and a liquid vehicle. The compositions and formulations of the invention are useful for dealing with diseases and conditions associated with abnormally high thyroid hormone levels in mammals, such as humans and cats.

1 . A composition comprising:
 i) about 0.25% to about 1% w/v of a thioureylene compound, a pharmaceutically acceptable salt, solvate, prodrug or combination thereof,   ii) at least about 0.2% w/v of a polysaccharide, and   iii) a liquid vehicle.   
     
     
         2 . The composition according to  claim 1 , wherein the thioureylene compound is selected from the group consisting of carbimazole, methimazole, methylthiouracil, propylthiouracil, their pharmaceutically acceptable salts, solvates, prodrugs and combinations thereof. 
     
     
         3 . The composition according to  claim 1  or  2  comprising at least about 0.4% w/v of the polysaccharide. 
     
     
         4 . The composition according to any of the preceding claims, wherein the polysaccharide is selected from the group consisting of amphoteric, anionic, cationic, hydrophobic and non-ionic polysaccharides and the combinations thereof. 
     
     
         5 . The composition according to any one of  claims 1  to  4 , wherein the polysaccharide is anionic. 
     
     
         6 . The composition according to any of the preceding claims, wherein the polysaccharide is a gum. 
     
     
         7 . The composition according to  claim 6 , wherein the polysaccharide is xanthan gum. 
     
     
         8 . The composition according to any of the preceding claims, wherein the liquid vehicle is selected from the group consisting of a hydrophobic oily carrier and water. 
     
     
         9 . The composition according to  claim 8 , wherein the hydrophobic oily carrier comprises a triglyceride of C 6 -C 18  chain fatty acid. 
     
     
         10 . The composition according to  claim 9 , wherein the triglyceride is selected from the group consisting of capric triglyceride, caprylic triglyceride and combinations thereof. 
     
     
         11 . The composition according to any of the preceding claims, further comprising a thickening agent. 
     
     
         12 . The composition according to  claim 11 , wherein the thickening agent is at least about 0.5% w/v of the total composition volume. 
     
     
         13 . The composition according to  claim 11  or  12 , wherein the thickening agent is selected from the group consisting of aluminum distearate, glycerol, hydrogenated castor oil, polyvinylpyrrolidone and combinations thereof. 
     
     
         14 . The composition according to any of the preceding claims, further comprising a wetting agent. 
     
     
         15 . The composition according to  claim 14 , wherein the wetting agent is 0.1% to about 1.0% w/v of the total composition volume. 
     
     
         16 . The composition according to  claim 14  or  15 , wherein the wetting agent is selected from the group consisting of polysorbate 80, simethicone emulsion and combinations thereof. 
     
     
         17 . The composition according to any of the preceding claims, further comprising a pH buffer solution. 
     
     
         18 . The composition according to  claim 17 , wherein the pH buffer solution is selected from the group consisting of citric acid, disodium phosphate dihydrate, sodium dihydrogen phosphate dihydrate and combinations thereof. 
     
     
         19 . The composition according to  claim 17 , wherein the pH of the composition is at least about 4.3 or more. 
     
     
         20 . The composition according to any of the preceding claims, further comprising a preservative. 
     
     
         21 . The composition according to  claim 20 , wherein the preservative comprises sodium benzoate. 
     
     
         22 . A pharmaceutical formulation comprising the composition of any one of  claims 1 - 21 . 
     
     
         23 . The composition according to any one of  claims 1 - 21 , or the pharmaceutical formulation as in  claim 22 , for use as a medicament. 
     
     
         24 . The composition according to any one of  claims 1 - 21 , or the pharmaceutical formulation as in  claim 22 , for use in the treatment or prevention of a disease or condition associated with an increased thyroid hormone level. 
     
     
         25 . The use of the composition according to any one of  claims 1 - 21  in the manufacture of a medicament for the treatment or prevention of a disease or condition associated with an increased thyroid hormone level. 
     
     
         26 . A method for reducing the thyroid hormone level in a subject, which comprises administering to the subject a therapeutically effective amount of the composition according to any one of  claims 1 - 21 , or the pharmaceutical formulation as in  claim 22 . 
     
     
         27 . The method as in  claim 26 , wherein the subject is human. 
     
     
         28 . The method as in  claim 26 , wherein the subject is a cat.