Pharmaceutical dosage form

Abstract

The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B 1 of at least 500 N in direction of extension E 1 and having a breaking strength B 2 of less than 500 N in direction of extension E 2 .

1 . A pharmaceutical dosage form comprising at least one pharmaceutically active ingredient, and having a shape comprising a longitudinal axis and two opposite longitudinal edges, a transversal axis perpendicular to the longitudinal axis and two opposite transversal edges, a front side, an opposite back side and a circumferential rim between said front and back side, wherein the front side and/or the back side comprise a basis area and wherein the front side and/or the back side comprise at least one bulge which extends above said basis area, said at least one bulge being present at and/or adjacent to at least a section of one or both longitudinal edges and/or at and/or adjacent to at least a section of one or both transversal edges and/or between both longitudinal edges and both transversal edges. 
     
     
         2 . The pharmaceutical dosage form according to  claim 1 , which is a tablet having an oblong shape. 
     
     
         3 . The pharmaceutical dosage form according to  claim 1 , wherein the front side and the back side each comprise at least one bulge at least along a section at and/or adjacent to both longitudinal edges and/or at least along a section at and/or adjacent to both transversal edges. 
     
     
         4 . The pharmaceutical dosage form according to  claim 1 , wherein said front side and said back side comprise an at least essentially continuous bulge at and/or adjacent to at least two third of both opposite longitudinal edges. 
     
     
         5 . The pharmaceutical dosage form according to  claim 1 , wherein one or both longitudinal edges are essentially straight over at least a major part of their length and/or wherein one or both transversal edges are curved over a major part of their length. 
     
     
         6 . The pharmaceutical dosage form according to  claim 1 , wherein the front side and/or the back side comprise an essentially circumferential bulge at and/or adjacent to the circumferential edge of the front side and/or the back side of said pharmaceutical dosage form. 
     
     
         7 . The pharmaceutical dosage form according to  claim 1 , wherein said pharmaceutical dosage form in its oblong form comprises at and/or adjacent to major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge at and/or adjacent to major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge at and/or adjacent to the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge at and/or adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         8 . The pharmaceutical dosage form according to  claim 7 , wherein said pharmaceutical dosage form in its oblong form comprises at major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge at major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge at the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge at the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         9 . The pharmaceutical dosage form according to  claim 7 , wherein said pharmaceutical dosage form in its oblong form comprises adjacent to major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge adjacent to major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge adjacent to the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         10 . The pharmaceutical dosage form according to  claim 7 , wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         11 . The pharmaceutical dosage form according to  claim 1 , wherein the front side and/or the back side comprise, in addition to at least one bulge on the front side and/or the back side, at least one indentation. 
     
     
         12 . The pharmaceutical dosage form according to  claim 11 , wherein the front and the back side comprise at least one indentation. 
     
     
         13 . The pharmaceutical dosage form according to  claim 12 , wherein the indentation(s) in the front side and the back side are at least once at least partially off-set. 
     
     
         14 . The pharmaceutical dosage form according to  claim 12 , wherein all the indentations of the front side and all the indentations of the back side are at least partially off-set. 
     
     
         15 . The pharmaceutical dosage form according to  claim 12 , wherein at least one indentation of the front side and at least one indentation of the back side are positioned in a congruent manner. 
     
     
         16 . The pharmaceutical dosage form according to  claim 15 , wherein all indentations of the front side and all indentations of the back side are positioned in a congruent manner. 
     
     
         17 . The pharmaceutical dosage form according to  claim 11 , wherein the indentations have a cylindrical or cube-like or cuboid-like shape or the shape of a half-sphere. 
     
     
         18 . The pharmaceutical dosage form according to  claim 1 , comprising one or more hydrophilic polymers. 
     
     
         19 . The pharmaceutical dosage form according to  claim 18 , wherein the one or more hydrophilic polymers are hydroxypropyl methyl cellulose and/or hydroxypropyl cellulose. 
     
     
         20 . The pharmaceutical dosage form according to  claim 18 , further comprising pregelatinized starch. 
     
     
         21 . The pharmaceutical dosage form according to  claim 1 , wherein the longitudinal length of the pharmaceutical dosage form does not exceed 30 mm. 
     
     
         22 . The pharmaceutical dosage form according to  claim 1 , having an average thickness over the basis areas of the front and the back side of about at least 1 mm. 
     
     
         23 . The pharmaceutical dosage form according to  claim 1 , wherein the bulge extends perpendicular from the basis area of the front side and/or from the basis area of the back side in average from about 0.5 mm to about 2 mm. 
     
     
         24 . The pharmaceutical dosage form according to  claim 1 , having a length in the longitudinal direction in the range of about 5 mm to about 30 mm, a width in the range of about 5 mm to about 15 mm, and a thickness over the basis areas in the range of about 1 mm to about 6 mm. 
     
     
         25 . The pharmaceutical dosage form according to  claim 1 , further comprising at least partially a coating. 
     
     
         26 . Tamper-resistant pharmaceutical dosage form, which has a retarded release profile for pharmaceutical application as an oral dosage form, comprising at least one pharmaceutically active ingredient with potential for abuse, and having a shape comprising a longitudinal axis and two opposite longitudinal edges, a transversal axis perpendicular to the longitudinal axis and two opposite transversal edges, a front side, an opposite back side and a circumferential rim between said front and back side, wherein the front side and/or the back side comprise a basis area and wherein the front side and/or the back side comprise at least one bulge which extends above said basis area, said at least one bulge being present at and/or adjacent to at least a section of one or both longitudinal edges and/or at and/or adjacent to at least a section of one or both transversal edges and/or between both longitudinal edges and both transversal edges. 
     
     
         27 . The pharmaceutical dosage form according to  claim 26 , which is a tablet having an oblong shape. 
     
     
         28 . The pharmaceutical dosage form according to  claim 26 , wherein the front side and the back side each comprise at least one bulge at least along a section at and/or adjacent to both longitudinal edges and/or at least along a section at and/or adjacent to both transversal edges. 
     
     
         29 . The pharmaceutical dosage form according to  claim 26 , wherein said front side and said back side comprise an at least essentially continuous bulge at and/or adjacent to at least two third of both opposite longitudinal edges. 
     
     
         30 . The pharmaceutical dosage form according to  claim 26 , wherein one or both longitudinal edges are essentially straight over at least a major part of their length and/or wherein one or both transversal edges are curved over a major part of their length. 
     
     
         31 . The pharmaceutical dosage form according to  claim 26 , wherein the front side and/or the back side comprise an essentially circumferential bulge at and/or adjacent to the circumferential edge of the front side and/or the back side of said pharmaceutical dosage form. 
     
     
         32 . The pharmaceutical dosage form according to  claim 26 , wherein said pharmaceutical dosage form in its oblong form comprises at and/or adjacent to major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge at and/or adjacent to major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge at and/or adjacent to the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge at and/or adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         33 . The pharmaceutical dosage form according to  claim 32 , wherein said pharmaceutical dosage form in its oblong form comprises at major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge at major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge at the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge at the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         34 . The pharmaceutical dosage form according to  claim 32 , wherein said pharmaceutical dosage form in its oblong form comprises adjacent to major portions of both opposite longitudinal edges of the front side at least one bulge, or wherein said pharmaceutical dosage form in its oblong form comprises at least one bulge adjacent to major portions of both opposite longitudinal edges of both the front side and the back side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form comprises in its oblong form a circumferential bulge adjacent to the circumferential edge of the front side of said pharmaceutical dosage form, or wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         35 . The pharmaceutical dosage form according to  claim 32 , wherein said pharmaceutical dosage form in its oblong form comprises a circumferential bulge adjacent to the circumferential edge of both the front side and the back side of said pharmaceutical dosage form. 
     
     
         36 . The pharmaceutical dosage form according to  claim 26 , wherein the front side and/or the back side comprise, in addition to at least one bulge on the front side and/or the back side, at least one indentation. 
     
     
         37 . The pharmaceutical dosage form according to  claim 36 , wherein the front and the back side comprise at least one indentation. 
     
     
         38 . The pharmaceutical dosage form according to  claim 37 , wherein the indentation(s) in the front side and the back side are at least once at least partially off-set. 
     
     
         39 . The pharmaceutical dosage form according to  claim 37 , wherein all the indentations of the front side and all the indentations of the back side are at least partially off-set. 
     
     
         40 . The pharmaceutical dosage form according to  claim 36 , wherein at least one indentation of the front side and at least one indentation of the back side are positioned in a congruent manner. 
     
     
         41 . The pharmaceutical dosage form according to  claim 40 , wherein all indentations of the front side and all indentations of the back side are positioned in a congruent manner. 
     
     
         42 . The pharmaceutical dosage form according to  claim 36 , wherein the indentations have a cylindrical or cube-like or cuboid-like shape or the shape of a half-sphere. 
     
     
         43 . The pharmaceutical dosage form according to  claim 26 , comprising a polyalkylene oxide. 
     
     
         44 . The pharmaceutical dosage form according to  claim 26 , comprising at least one cellulose ether derivative. 
     
     
         45 . The pharmaceutical dosage form according to  claim 44 , wherein the cellulose ether derivative is HPMC. 
     
     
         46 . The pharmaceutical dosage form according to  claim 43 , wherein the polyalkylene oxide is polyethylene oxide. 
     
     
         47 . The pharmaceutical dosage form according to  claim 46 , wherein the polyethylene oxide has a molecular weight in the range of about 2,000,000 to about 7,000,000. 
     
     
         48 . The pharmaceutical dosage form according to  claim 26 , wherein the pharmaceutical dosage form further comprises a polyalkylene glycol. 
     
     
         49 . The pharmaceutical dosage form according to  claim 48 , wherein the polyalkylene glycol is polyethylene glycol. 
     
     
         50 . The pharmaceutical dosage form according to  claim 26 , wherein the pharmaceutically active ingredient with potential for abuse is a pain-killing drug. 
     
     
         51 . The pharmaceutical dosage form according to  claim 50 , wherein the pharmaceutically active ingredient is tapentadol. 
     
     
         52 . The pharmaceutical dosage form according to  claim 26 , comprising at least one pharmaceutically active ingredient with potential for abuse; at least one poly(alkylene oxide); at least one cellulose ether derivative; and at least one polyalkylene glycol; and optionally an additive. 
     
     
         53 . The pharmaceutical dosage form according to  claim 52 , wherein the active ingredient with potential for abuse is present in an amount of at least 5 weight percent; poly(alkylene oxide) is present in an amount of at least 15 weight percent; cellulose ether derivative is present in an amount of at least 5 weight percent; and polyalkylene glycol is present in an amount of at least 5 weight percent. 
     
     
         54 . The pharmaceutical dosage form according to  claim 26 , wherein the longitudinal length of the pharmaceutical dosage form does not exceed 30 mm. 
     
     
         55 . The pharmaceutical dosage form according to  claim 26 , having an average thickness over the basis areas of the front and the back side of about at least 1 mm. 
     
     
         56 . The pharmaceutical dosage form according to  claim 26 , wherein the bulge extends perpendicular from the basis area of the front side and/or from the basis area of the back side in average from about 0.5 mm to about 2 mm. 
     
     
         57 . The pharmaceutical dosage form according to  claim 26 , having a length in the longitudinal direction in the range of about 5 mm to about 30 mm, a width in the range of about 5 mm to about 15 mm, and a thickness over the basis areas in the range of about 1 mm to about 6 mm. 
     
     
         58 . The pharmaceutical dosage form according to  claim 26 , wherein said pharmaceutical dosage form is a monolith. 
     
     
         59 . The pharmaceutical dosage form according to  claim 26 , which has been prepared via compression using a die and a punch from a monolithic mass obtained by melt extrusion. 
     
     
         60 . The pharmaceutical dosage form according to  claim 58 , wherein said pharmaceutical dosage form has been obtained by compressing a melt extruded monolithic mass which exhibits ambient temperature. 
     
     
         61 . The pharmaceutical dosage form according to  claim 58 , wherein the extruded monolithic mass has been cut prior to compression. 
     
     
         62 . The pharmaceutical dosage form according to  claim 58 , wherein melt extrusion has been conducted with a twin-screw extruder. 
     
     
         63 . The pharmaceutical dosage form according to  claim 26 , further comprising at least partially a coating. 
     
     
         64 . A method of treating pain in a patient in need of such treatment, said method comprising administering to said patient an effective amount therefor of a pharmaceutical dosage form according to  claim 1 , wherein the pharmaceutically active ingredient, the pharmaceutically active ingredient with potential for abuse and the pharmacologically active compound (A) are each selected from the group consisting of analgesics.