US2003203007A1PendingUtilityA1

Pharmaceutical composition reduced in bitter taste and the like

Assignee: EISAI CO LTDPriority: Aug 28, 1998Filed: Apr 7, 2003Published: Oct 30, 2003
Est. expiryAug 28, 2018(expired)· nominal 20-yr term from priority
A61K 47/32A61K 9/0095
55
PatentIndex Score
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Claims

Abstract

The present invention provides a composition alleviated in a bitter taste or the like of a medicament. The present invention relates to a composition comprising a basic medicament having an unpleasant taste and polyvinylpyrrolidone and/or copolyvidone; or a method for alleviating an unpleasant taste of a basic medicament having the unpleasant taste by adding polyvinylpyrrolidone and/or copolyvidone. The present invention further provides a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (3) propylene glycol and/or D-sorbitol; a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (4) an antioxidant; and a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (5) a colorant or flavor containing a sulfuric acid or sulfurous acid group.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition comprising a basic medicament characterized by having a proton existing as a positive charge under acidic conditions and at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone, said composition comprising 5 to 200 parts by weight of polyvinylpyrrolidone and/or copolyvidone per 1 part by weight of the medicament.  
     
     
         2 . The composition as claimed in  claim 1 , which is in the form of syrups, jellies, dry syrups, liquids, effervescent preparations, lemonades, elixirs, liniments or fine granules.  
     
     
         3 . A method for alleviating an unpleasant taste of a basic medicament characterized by having a proton existing as a positive charge under acidic conditions comprising adding thereto at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone in an amount of from 5 to 200 parts by weight of polyvinylpyrrolidone and/or copolyvidone per 1 part by weight of the medicament.  
     
     
         4 . A composition comprising a basic medicament characterized by having a proton existing as a positive charge under acidic conditions, at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone and at least one component selected from the group consisting of propylene glycol and D-sorbitol, said composition comprising 5 to 200 parts by weight of polyvinylpyrrolidone and/or copolyvidone per 1 part by weight of the medicament.  
     
     
         5 . A method for suppressing the formation of analogues of a basic medicament characterized by having a proton existing as a positive charge under acidic conditions caused by the addition of polyvinylpyrrolidone or copolyvidone thereto, comprising further adding at least one component selected from propylene glycol and D-sorbitol, said polyvinylpyrrolidone and/or copolyvidone being added in an amount of from 5 to 200 parts by weight per 1 part by weight of the medicament.  
     
     
         6 . The method of  claim 5 , wherein said medicament is in the form of syrups, jellies, dry syrups, liquids, effervescent preparations, lemonades, elixirs, liniments or fine granules.  
     
     
         7 . A composition comprising a basic medicament characterized by having a proton existing as a positive charge under acidic conditions, at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone, and an antioxidant, said composition comprising 5 to 200 parts by weight of polyvinylpyrrolidone and/or copolyvidone per 1 part by weight of the medicament.  
     
     
         8 . The composition as claimed in  claim 7 , wherein the antioxidant is selected from the group consisting of sodium bisulfite, sodium sulfite, sodium pyrosulfite, cysteine, citric acid, sodium edetate, ascorbic acid and erythorbic acid.  
     
     
         9 . A method for suppressing the formation of analogues of a basic medicament characterized by having a proton existing as a positive charge under acidic conditions caused by the addition of polyvinylpyrrolidone or copolyvidone thereto, comprising further adding an antioxidant, said polyvinylpyrrolidone and/or copolyvidone being added in an amount of from 5 to 200 parts by weight per 1 part by weight of the medicament.  
     
     
         10 . The method of  claim 9 , wherein said medicament is in the form of syrups, jellies, dry syrups, liquids, effervescent preparations, lemonades, elixirs, liniments or fine granules.  
     
     
         11 . The method of  claim 9 , wherein said antioxidant is selected from the group consisting of sodium bisulfite, sodium sulfite, sodium pyrosulfite, cysteine, citric acid, sodium edetate, ascorbic acid and erythorbic acid.  
     
     
         12 . A composition comprising a basic medicament characterized by having a proton existing as a positive charge under acidic conditions, at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone, and a colorant or flavor containing a sulfuric acid or sulfurous acid group, said composition comprising 5 to 200 parts by weight of polyvinylpyrrolidone and/or copolyvidone per 1 part by weight of the medicament.  
     
     
         13 . The composition as claimed in  claim 12 , wherein the colorant or flavor containing a sulfuric acid or sulfurous acid group is selected from the group consisting of trisodium 2-hydroxyazonaphthalene-4′,6,8-trisulfonate, 2′,4′,5′,7′-tetraiodofluorescein disodium salt, trisodium 2-hydroxyazonahthalene-3,4′,6-trisulfonate, disodium 3-[N-ethyl-N-[4-[[-N-ethyl-N-(3-sulfonatobenzyl)amino]phenyl](2-sulfonatophenyl)methylene]-2,5-cyclohexadienyliden]ammoniomethyl]benzenesulfonate, disodium 2-(1,3-dihydro-3-oxo-5-sulfo-2H-indol-2-ylidene)-2,3-dihydro-3-oxo-1H-indole-5-sulfonate, disodium N-ethyl-N-[4-[[ethyl[(3-sulfophenyl)methyl]amino]phenyl](4-hydroxyl-2-sulfophenyl)methylene)-2,5-cyclohexadien-1-ylidene]-3-sulfobenzenemethaneaminiumhydroxide, trisodium 3-carbonato-5-hydroxy-1-(4-sulfonatophenyl)-1H-pyrazol-4-azo-4′-(benzenesulfonate) and disodium 2-hydroxy-6-sulfonatonaphthalen-1-azo-(4′-benzenesulfonate).  
     
     
         14 . A method for suppressing the formation of an insoluble precipitate of a basic medicament characterized by having a proton existing as a positive charge under acidic conditions caused by the addition of a colorant or flavor containing a sulfuric acid or sulfurous acid group thereto, comprising adding at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone in an amount of from 5 to 200 parts by weight per 1 part by weight of the medicament.  
     
     
         15 . The method of  claim 14 , wherein said medicament is in the form of syrups, jellies, dry syrups, liquids, effervescent preparations, lemonades, elixirs, liniments or fine granules.  
     
     
         16 . The method of  claim 14 , wherein said colorant is selected from the group consisting of trisodium 2-hydroxyazonaphthalene-4′,6,8-trisulfonate, 2′,4′,5′,7′-tetraiodofluorescein disodium salt, trisodium 2-hydroxyazonahthalene-3,4′,6-trisulfonate, disodium 3-[N-ethyl-N-[4-[[-N-ethyl-N-(3-sulfonatobenzyl)amino]phenyl](2-sulfonatophenyl)methylene]-2,5-cyclohexadienyliden]ammoniomethyl]benzenesulfonate, disodium 2-(1,3-dihydro-3-oxo-5-sulfo-2H-indol-2-ylidene)-2,3-dihydro-3-oxo-1H-indole-5-sulfonate, disodium N-ethyl-N-[4-[[ethyl[(3-sulfophenyl)methyl]amino]phenyl](4-hydroxyl-2-sulfophenyl)methylene)-2,5-cyclohexadien-1-ylidene]-3-sulfobenzenemethaneaminiumhydroxide, trisodium 3-carbonato-5-hydroxy-1-(4-sulfonatophenyl)-1H-pyrazol-4-azo-4′-(benzenesulfonate) and disodium 2-hydroxy-6-sulfonatonaphthalen-1-azo-(4′-benzenesulfonate).  
     
     
         17 . The method as claimed in  claim 14 , further comprising adding at least one component selected from propylene glycol and D-sorbitol.  
     
     
         18 . The method as claimed in  claim 14 , further comprising adding a colorant or flavor containing a sulfuric acid or sulfurous acid group.  
     
     
         19 . The method as claimed in  claim 14 , further comprising adding an antioxidant.  
     
     
         20 . A method for alleviating an unpleasant taste of a basic medicament characterized by having a proton existing as a positive charge under acidic conditions comprising adding thereto at least one component selected from the group consisting of polyvinylpyrrolidone and copolyvidone, said composition being in the form of syrups, jellies, dry syrups, liquids, effervescent preparations, lemonades, elixirs, liniments or fine granules, said polyvinylpyrrolidone and/or copolyvidone being added in an amount of from 5 to 200 parts by weight per 1 part by weight of the medicament.

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