Modified release dosage forms of skeletal muscle relaxants

  • US 7,544,372 B2
  • Filed: 02/06/2008
  • Issued: 06/09/2009
  • Est. Priority Date: 11/14/2003
  • Status: Expired due to Fees
First Claim
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1. A method of relieving muscle spasms in a patient in need thereof comprising administering a pharmaceutical dosage form of a skeletal muscle relaxant comprising a population of extended release beads,wherein said extended release beads comprise:

  • an active-containing core particle comprising a skeletal muscle relaxant selected from the group consisting of cyclobenzaprine, pharmaceutically acceptable salts or derivatives thereof and mixtures thereof; and

    an extended release coating comprising a water insoluble polymer membrane surrounding said core,wherein said dosage form when dissolution tested using United States Pharmacopoeia Apparatus 2 (paddles @ 50 rpm) in 900 mL of 0.1N HCl at 37°

    C. exhibits a drug release profile substantially corresponding to the following pattern;

    after 2 hours, no more than about 40% of the total active is released;

    after 4 hours, from about 40-65% of the total active is released;

    after 8 hours, from about 60-85% of the total active is released;

    wherein said dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions; and

    wherein said water insoluble polymer membrane comprises a water insoluble polymer selected from the group consisting of ethers of cellulose, esters of cellulose, cellulose acetate, ethyl cellulose, polyvinyl acetate, neutral copolymers based on ethylacrylate and methylmethacrylate, copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups, pH-insensitive ammonio methacrylic acid copolymers, and mixtures thereof;

    and a plasticizer selected from the group consisting of triacetin, tributyl citrate, tri-ethyl citrate, acetyl tri-n-butyl citrate, diethyl phthalate, dibutyl sebacate, polyethylene glycol, polypropylene glycol, castor oil, acetylated mono- and di-glycerides and mixtures thereof.

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