Pharmaceutical compositions
DCFirst Claim
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1. A composition comprising 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 the 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.
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Abstract
Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.
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Citations
10 Claims
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1. A composition comprising a plurality of multi-layer pellets comprising:
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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 the morphine sulfate and hydroxypropyl cellulose; wherein in the multi-layer pellets, the sodium lauryl sulfate is only contained in the sequestering polymer layer; and wherein 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 Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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Specification