Modified release dosage forms of skeletal muscle relaxants

  • US 7,820,203 B2
  • Filed: 02/06/2008
  • Issued: 10/26/2010
  • Est. Priority Date: 11/14/2003
  • Status: Active Grant
First Claim
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1. A multi-particulate pharmaceutical dosage form comprising a population of extended release beads, wherein said extended release beads comprise:

  • an active-containing core particle comprising cyclobenzaprine hydrochloride as the active; and

    an extended release coating comprising a water insoluble polymer membrane surrounding said core, wherein said water insoluble polymer membrane comprises a polymer selected from the group consisting of ethers of cellulose, esters of cellulose, cellulose acetate, ethyl cellulose, polyvinyl acetate, neutral copolymers based on ethyl acrylate and methyl methacrylate, copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups, pH-insensitive ammonio methacrylic acid copolymers, and mixtures thereof;

    wherein the total amount of cyclobenzaprine hydrochloride in the pharmaceutical dosage form is 30 mg;

    wherein said pharmaceutical 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 release profile substantially corresponding to the following pattern;

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

    after 4 hours, from about 40-65% of the total amount of the cyclobenzaprine hydrochloride is released; and

    after 8 hours, from about 60-85% of the total amount of the cyclobenzaprine hydrochloride is released; and

    wherein following a single oral administration, said pharmaceutical dosage form provides a maximum blood plasma concentration (Cmax) within the range of about 80% to 125% of about 20 ng/mL of cyclobenzaprine and an AUC0-168 within the range of about 80% to 125% of about 740 ng·

    hr/mL.

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