IP Library Patent Application 12459551
Patent Application
App. No. 12/459,551

Pharmaceutical preparation containing copolyvidone

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Quick Facts
Patent No.
US None
App. No.
12/459,551
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.

Claims (21)

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.

Assignments (2)
CHANGE OF NAME Recorded May 27, 2010
From: TAKEDA CHEMICAL INDUSTRIES, LTD
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 024462/0450 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 11, 2009
From: ISHIDA, HAJIME; FUKUTA, MAKOTO
To: TAKEDA CHEMICAL INDUSTRIES, LTD.
Reel/Frame 023233/0421 →