Aqueous Pharmaceutical Formulation of Tapentadol for Oral Administration

Abstract

An aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof and being adapted for oral administration. The composition has excellent storage stability without relying on the presence of high amounts of preservatives.

1 . An aqueous pharmaceutical composition comprising water and tapentadol or a physiologically acceptable salt thereof, wherein said composition is orally administrable. 
     
     
         2 . The composition according to  claim 1 , further comprising a buffer. 
     
     
         3 . The composition according to  claim 2 , wherein said composition is buffered to a pH value within the range from 3.0 to 6.5. 
     
     
         4 . The composition according to  claim 1 , wherein said composition has a pH value within the range from 3.0 to 6.5. 
     
     
         5 . The composition according to  claim 1 , wherein said composition contains tapentadol in a concentration of 50 mg/mL or less, based on the total volume of the composition. 
     
     
         6 . The composition according to  claim 1 , wherein said composition is free of any preservative. 
     
     
         7 . The composition according to  claim 1 , further comprising a preservative. 
     
     
         8 . The composition according to  claim 7 , wherein said preservative is selected from the group consisting of benzalkonium chloride, benzethonium chloride, benzoic acid, sodium benzoate, benzyl alcohol, bronopol, cetrimide, cetylpyridinium chloride, chlorhexidine, chlorbutanol, chlorocresol, chloroxylenol, cresol, ethyl alcohol, glycerin, hexetidine, imidurea, phenol, phenoxyethanol, phenylethyl alcohol, phenylmercuric nitrate, propylene glycol, sodium propionate, thimerosal, methyl paraben, ethyl paraben, propyl paraben, butyl paraben, isobutyl paraben, benzyl paraben, sorbic acid, and potassium sorbate. 
     
     
         9 . The composition according to  claim 7 , wherein the content of said preservative is at most 5.0 wt.-%, based on the total weight of the composition. 
     
     
         10 . The composition according to  claim 7 , wherein the sum of the concentration of tapentadol and the concentration of preservative is 50 mg/mL or less, based on the total volume of the composition. 
     
     
         11 . The composition according to  claim 7 , wherein the preservative content is at most 90% of the content that would be needed according to Ph. Eur. in order to sufficiently preserve the pharmaceutical composition in the absence of tapentadol. 
     
     
         12 . The composition according to  claim 1 , wherein said composition exhibits a shelf-life under accelerated storage conditions of at least 3 months. 
     
     
         13 . The composition according to  claim 1 , wherein said composition is selected from the group consisting of syrups, drops, solutions, dispersions, suspensions and emulsions. 
     
     
         14 . A pharmaceutical dosage form comprising a pharmaceutical composition according to  claim 1 . 
     
     
         15 . The dosage form according to  claim 14 , wherein said dosage form is selected from the group consisting of oral solutions, oral gels, suspensions, emulsions and liquid or gel filled capsules. 
     
     
         16 . The dosage form according to  claim 15 , wherein said dosage form is adapted for administration to pediatric patients. 
     
     
         17 . A method of treating pain in a subject in need thereof, said method comprising administering to said subject a pharmaceutically effective amount of a composition according to  claim 1 . 
     
     
         18 . A method according to  claim 17 , wherein said pain is selected from the group consisting of acute pain and chronic pain.