Pharmaceutical composition

  • US 7,682,633 B2
  • Filed: 03/06/2009
  • Issued: 03/23/2010
  • Est. Priority Date: 06/19/2006
  • Status: Active Grant
First Claim
Patent Images

1. A method of treating moderate to severe pain in a human, the method comprising:

  • the human orally taking an intact composition in an amount sufficient to treat the moderate to severe pain,wherein the composition comprises a plurality of multi-layer pellets comprising;

    a. a water-soluble core;

    b. an antagonist containing layer comprising naltrexone HCl coating the core;

    c. a sequestering polymer layer coating the antagonist containing layer;

    d. an agonist layer comprising morphine sulfate coating the sequestering polymer layer;

    e. a controlled release layer coating the agonist layer; and

    f. immediately beneath the agonist layer, an osmotic pressure regulating agent layer comprising sodium chloride;

    wherein the sequestering polymer layer comprises copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups, sodium lauryl sulfate in an amount from 1.6% to 6.3% of the copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups on a weight-to-weight basis, and talc in an amount of from 75% to 125% of the copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups on a weight-to-weight basis;

    wherein the agonist layer comprises morphine sulfate and hydroxypropyl cellulose;

    wherein in the multi-layer pellets, the sodium lauryl sulfate is only contained in the sequestering polymer layer;

    andwherein the composition sequesters at least 80% of the naltrexone HCl as determined at 73 hours by first placing the composition in 500 mL of a 0.1 N HCl solution for 1 hour at 37°

    C. using USP paddle method, 100 rotations per minute, and then placing the composition in 500 mL of a pH 7.5, 0.05 M phosphate buffer, for 72 hours at 37°

    C. using USP paddle method, 100 rotations per minute, and then determining the amount of the naltrexone HCl sequestered.

View all claims
    ×
    ×

    Thank you for your feedback

    ×
    ×