Modified release preparations containing oxcarbazepine and derivatives thereof

CAFC
  • US 8,617,600 B2
  • Filed: 05/21/2012
  • Issued: 12/31/2013
  • Est. Priority Date: 04/26/2006
  • Status: Active Grant
First Claim
Patent Images

1. A solid oral pharmaceutical formulation for once-a-day administration of oxcarbazepine comprising a homogeneous matrix comprising:

  • (a) oxcarbazepine;

    (b) 1-50%, by weight of the formulation, a matrix-forming polymer selected from the group consisting of cellulosic polymers, alginates, gums, cross-linked polyacrylic acid, carageenan, polyvinyl pyrrolidone, polyethylene oxides, and polyvinyl alcohol;

    (c) 1-80%, by weight of the formulation, at least one agent that enhances the solubility of oxcarbazepine selected from the group consisting of surface active agents, complexing agents, cyclodextrins, pH modifying agents, and hydration promoting agents;

    (d) 10-90%, by weight of the formulation, at least one release promoting agent comprising a polymer having pH-dependent solubility selected from the group consisting of cellulose acetate phthalate, cellulose acetate succinate, methylcellulose phthalate, ethylhydroxycellulose phthalate, polyvinylacetate phthalate, polyvinylbutyrate acetate, vinyl acetate-maleic anhydride copolymer, styrene-maleic mono-ester copolymer, Eudagrit L100-55 (Methacrylic Acid—

    Ethyl Acrylate Copolymer (1;

    1)), and methyl acrylate-methacrylic acid copolymers,wherein, in vitro;

    (i) between 20 and 74% of the total oxcarbazepine is released by 2 hours; and

    (ii) between 44 and 96% of the total oxcarbazepine is released by 4 hours.

View all claims
    ×
    ×

    Thank you for your feedback

    ×
    ×