Abuse-proofed dosage form

Abstract

A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.

1 . A solid dosage form for oral administration with reduced potential for parenteral abuse, said dosage form comprising:
 (a) one or more active ingredients having potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol, and pharmaceutically acceptable salts and solvates thereof; and   (b) at least one viscosity-increasing agent in a quantity such that an aqueous extract of a total content of the dosage form when comminuted and combined with 10 ml of water at 25° C. forms a gel that can be drawn up into and injected back out of a hypodermic needle having a diameter of 0.9 mm, into a further quantity of water, wherein threads of the gel injected from said needle remain visible to the naked eye in said further quantity of water at 37° C.   
     
     
         2 . The dosage form according to  claim 1 , wherein the active ingredient is oxycodone or a salt or solvate thereof. 
     
     
         3 . The dosage form according to  claim 1 , wherein the active ingredient is hydrocodone or a salt or solvate thereof. 
     
     
         4 . The dosage form according to  claim 1 , wherein the active ingredient is morphine or a salt or solvate thereof. 
     
     
         5 . The dosage form according to  claim 1 , comprising one or more viscosity-increasing agents selected from the group consisting of microcrystalline cellulose with 11 wt. % carboxymethylcellulose sodium, carboxymethylcellulose sodium, polyacrylic acid, locust bean flour, citrus pectin, waxy maize starch, sodium alginate, guar flour, iota-carrageenan, karaya gum, gellan gum, galactomannan, tara stone flour, propylene glycol alginate, apple pectin, lemon peel pectin, sodium hyaluronate, tragacanth, tara gum, fermented polysaccharide welan gum and xanthan gum. 
     
     
         6 . The dosage form according to  claim 1 , in particulate form. 
     
     
         7 . The dosage form according to  claim 1 , comprising at least one active ingredient in controlled release form. 
     
     
         8 . The dosage form according to  claim 1 , comprising a coating resistant to gastric juices. 
     
     
         9 . The dosage form according to  claim 1 , in multiparticulate form, wherein said multiparticulate form is in the form of microtablets, microcapsules, micropellets, granules, spheroids, beads or pellets, packaged in capsules or press-molded into tablets. 
     
     
         10 . The dosage form according to  claim 1 , wherein said threads remain visible to the naked eye in said further quantity of water for at least one minute. 
     
     
         11 . The dosage form according to  claim 1 , wherein said threads remain visible to the naked eye in said further quantity of water for at least ten minutes. 
     
     
         12 . The dosage form according to  claim 1 , which further comprises microcrystalline cellulose. 
     
     
         13 . The dosage form according to  claim 1 , which further comprises hydroxypropylmethylcellulose. 
     
     
         14 . A solid dosage form for oral administration with reduced potential for parenteral abuse, said dosage form comprising:
 (a) one or more active ingredients having potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol, and pharmaceutically acceptable salts and solvates thereof; and   (b) one or more components having at least a viscosity-increasing influence, in a total quantity, for all said components combined, that is equal to or greater than 5 mg per dosage form, that quantity being selected such that an aqueous extract of a total content of the dosage form, when comminuted and combined with 10 ml of water at 25° C., forms a gel that is capable of being drawn into and then expelled from a hypodermic needle having a diameter of 0.9 mm, wherein threads of said gel, formed upon exit from said needle into a further quantity of water at 37° C., remain substantially coherent and visible to the naked eye.   
     
     
         15 . The dosage form according to  claim 14 , wherein the active ingredient is oxycodone or a salt or solvate thereof. 
     
     
         16 . The dosage form according to  claim 14 , wherein the active ingredient is hydrocodone or a salt or solvate thereof. 
     
     
         17 . The dosage form according to  claim 14 , wherein the active ingredient is morphine or a salt or solvate thereof. 
     
     
         18 . The dosage form according to  claim 14 , wherein said threads remain substantially coherent and visible to the naked eye in said further quantity of water for at least one minute. 
     
     
         19 . The dosage form according to  claim 14 , wherein said threads remain substantially coherent and visible to the naked eye in said further quantity of water for at least ten minutes. 
     
     
         20 . The dosage form according to  claim 14 , comprising at least one active ingredient in controlled release form. 
     
     
         21 . The dosage form according to  claim 14 , which further comprises microcrystalline cellulose. 
     
     
         22 . The dosage form according to  claim 14 , which further comprises hydroxypropylmethylcellulose. 
     
     
         23 . A solid dosage form for oral administration with reduced potential for parenteral abuse, said dosage form comprising:
 (a) one or more active ingredients with potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol and pharmaceutically acceptable salts and/or solvates thereof; and   (b) one or more viscosity-increasing agents;   wherein the dosage form when its total content is comminuted and combined with 10 ml of water at 25° C. forms an injectable gel that can be drawn up into and injected back out of a syringe having a diameter of 0.9 mm, but wherein the injectable gel cannot be safely injected from said syringe into a blood vessel of an abuser because the presence of the injectable gel in the abuser's blood vessels would probably obstruct one or more of said abuser's blood vessels.   
     
     
         24 . The dosage form according to  claim 23 , wherein the active ingredient is oxycodone or a salt or solvate thereof. 
     
     
         25 . The dosage form according to  claim 23 , wherein the active ingredient is hydrocodone or a salt or solvate thereof. 
     
     
         26 . The dosage form according to  claim 23 , wherein the active ingredient is morphine or a salt or solvate thereof. 
     
     
         27 . The dosage form according to  claim 23 , which further comprises microcrystalline cellulose. 
     
     
         28 . The dosage form according to  claim 23 , which further comprises hydroxypropylmethylcellulose. 
     
     
         29 . The dosage form according to  claim 23 , comprising at least one active ingredient in controlled release form.