Pharmaceutical preparation containing copolyvidone

Abstract

A stabilized preparation which comprises: a unstable drug in a polyethylene glycol-containing preparation; and a coating agent comprising a copolyvidone instead of polyethylene glycol with which the drug is coated.

1 . A stabilized preparation comprising a unstable drug in a polyethylene glycol-containing preparation and a copolyvidone-containing coating agent with which the drug is coated.  
     
     
         2 . The preparation according to  claim 1 , wherein the drug is a unstable drug in a preparation coated with a polyethylene glycol-containing. coating agent.  
     
     
         3 . The preparation according to  claim 1 , wherein the coating agent is soluble in water.  
     
     
         4 . The preparation according to  claim 1 , wherein the coating agent further contains a light-protecting agent.  
     
     
         5 . The preparation according to  claim 1 , wherein the unstable drug in the polyethylene glycol-containing preparation is a compound represented by the formula:  
       
         
           
           
               
               
           
         
         wherein R 1  represents an optionally substituted hydrocarbon group, an optionally substituted amino group or an optionally substituted heterocyclic group,  
         R 2  represents a hydrogen atom or an optionally substituted hydrocarbon group,  
         R 3  represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group,  
         X represents CHR 4 , NR 4 , O or S (R 4  represents a hydrogen atom or an optionally substituted hydrocarbon group),  
         Y represents C, CH or N (provided that, when X represents CH 2 , Y is C or CH),  
            represents a single bond or a double bond,  
         ring A represents an optionally substituted 5- to 7-membered heterocyclic ring containing an oxygen atom,  
         ring B represents an optionally substituted benzene ring, and  
         m represents an integer of 1 to 4, or a salt thereof.  
       
     
     
         6 . The preparation according to  claim 1 , wherein the unstable drug in the polyethylene glycol-containing preparation is a compound represented by the formula:  
       
         
           
           
               
               
           
         
       
       wherein Ar represents an optionally substituted aromatic group, X′ represents a divalent C 1-6  aliphatic hydrocarbon group which optionally have 1 or 2 divalent groups selected from —O—, —S—, —CO—, —SO—, —SO 2 — and —COO—, Y′ represents a divalent C 1-6  aliphatic hydrocarbon group, R′ and R″ are the same or different and each represents a hydrogen atom or an optionally substituted C 1-6  alkyl, ring A′ represents a benzene ring which may be further substituted, and ring B′ represents a 4- or 8-membered ring which may be further substituted, or a salt thereof.  
     
     
         7 . The preparation according to  claim 1 , wherein the unstable drug in the polyethylene glycol-containing preparation is selected from N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]acetylamide, N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]butylamide, 6-(4-biphenylyl)methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin, 6-(4-biphenylyl)methoxy-2-(N,N-dimethylamino)methyltetralin, 6-(4-biphenylyl)methoxy-2-(N,N-dipropylamino)methyltetralin, 2-(N,N-dimethylamino)methyl-6-(4′-methoxybiphenyl-4-yl)methoxytetralin, (+)-6-(4-biphenylyl)methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin, (+)-6-(4-biphenylyl)methoxy-2-[2-(N,N-diethylamino)ethyl]tetralin, (+)-2-[2-(N,N-dimethylamino)ethyl]-6-(4′-methylbiphenyl-4-yl)methoxytetralin, (+)-2-[2-(N,N-dimethylamino)ethyl]-6-(4′-methoxybiphenyl-4-yl)methoxytetralin, (+)-6-(2′,4′-dimethoxybiphenyl-4-yl)methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin, (+)-6-[4-(1,3-benzodioxazol-5-yl)phenyl]methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin, (+)-6-(3′,4′-dimethoxybiphenyl-4-yl)methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin, an optically active substance thereof and a salt thereof.  
     
     
         8 . A method for stabilizing a preparation, which comprises coating a unstable drug in a polyethylene glycol-containing preparation with a coating agent containing copolyvidone.  
     
     
         9 . Use of a copolyvidone-containing coating agent for stabilizing a unstable drug in a polyethylene glycol-containing preparation.  
     
     
         10 . Use of copolyvidone in a coating agent for stabilizing a unstable drug in a polyethylene glycol-containing preparation.  
     
     
         11 . Use of copolyvidone according to  claim 10  for stabilizing a unstable drug in a polyethylene glycol-containing preparation in a coating agent.