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Active-substance vector multiparticulate system, production and use thereof

  • US 6,916,481 B1
  • Filed: 04/12/2000
  • Issued: 07/12/2005
  • Est. Priority Date: 04/12/1999
  • Status: Expired due to Term
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Assignment
First Claim
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1. A multiparticulate carrier system (S) in a solid form for active material(s) comprising at least one active material enclosed in a hydrophilic organic matrix (OM) comprising at least one water-soluble or water-dispersible anionic polymer (K) rendered insoluble by a metal cation, and wherein said copolymer (K) is a sulfonated anionic copolymer comprising:

  • identical or different, aromatic, aliphatic or cycloaliphatic, nonsulfonated dicarbonyl units (DCus), of formula;


    —

    C(O)-A-C(O)—

    wherein A is a polyvalent aromatic, aliphatic or cycloaliphatic hydrocarbon group,identical or different, aliphatic, cycloaliphatic or aromatic, nonsulfonated polyfunctional units (PFus), which are devoid of sulfo functional groups, of formula;


    —

    X-E-Y—

     

    wherein X and Y which are identical or different, are selected from the group consisting of the following groups;

    oxy—

    O—

    imino—

    NH—

    , and(R)imino—

    N(R)—

    wherein R is a C1-C4 alkyl group,
    E represents a polyvalent aliphatic, cycloaliphatic or aromatic hydrocarbon group, optionally interrupted by one or more oxygen or tertiary nitrogen heteroatom(s), said polyvalent group being bonded to at least one X group and to at least one Y group, sulfonated units (Sus), selected from the group consisting of;

    identical or different, aromatic, aliphatic or cycloaliphatic, sulfonated polyfunctional units (SPFus), exhibiting at least one sulfo functional group, of formula;


    —

    V-Q(L-SO3M)n—

    W—

     

    wherein;

    V and W, which are identical or different, are selected from the group consisting of the following groups;

    carbonyl—

    C(O)—

    ,oxy—

    O—

    ,imino—

    NH—

    , and(R)imino—

    N(R)—

    wherein R is a C1-C4 alkyl group,
    Q is an aromatic, aliphatic or cycloaliphatic hydrocarbona group, L is a valency bond or an alkylene, alkoxyalkylene, oxyalkylene, arylene, alkylarylene or alkoxyarylene group, M is a hydrogen atom or an alkaline cation, and n is greater than or equal to 1, and identical or different, aromatic, aliphatic or cycloaliphatic, sulfonated monofunctional units (SMFus), exhibiting at least one sulfo functional group, of formula;


    —

    V′

    -Q′

    (L-SO3M)n  

    wherein;

    V′

    is a group selected from group consisting of the following groups;

    carbonyl—

    C(O)—

    , andoxy—

    O—

    ,
    Q′

    is an aromatic, aliphatic or cycloaliphatic hydrocarbon group, optionally interrupted by one or more oxygen heteroatom(s), L is a valency bond or an alkylene, alkoxyalkylene, oxyalkylene, arylene, alkylarylene or alkoxyarylene group, M a hydrogen atom or an alkaline cation, and n is greater than or equal to 1, optionally, identical or different, aliphatic, cycloaliphatic or aromatic, nonsulfonated polyfunctional monocarbonyl units (MCus), which are devoid of sulfo functional groups, of formula;


    —

    C(O)-D-Z-  

    wherein;

    Z is a group selected from the group consisting of the following groups;

    oxy—

    O—

    ,imino—

    NH—

    , and(R)imino—

    N(R)—

    wherein R is a C1-C4 alkyl group, and
    D is an aliphatic, cycloaliphatic or aromatic hydrocarbon group, and identical or different bonding groups (L) selected from the group consisting of groups of formula;


    —

    C(O)—

    O—

    , —

    O—

    C(O)—

    , —

    C(O)—

    N(R′

    )—

    , and —

    N(R′

    )—

    C(O)—

    , whereinR′

    is H or a C1-C4 alkyl group.

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