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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.|
|Inventor(s):||Matthews; Frank (Edison, NJ), Boehm; Garth (Westfield, NJ), Tang; Lijuan (Flemington, NJ), Liang; Alfred (Edison, NJ)|
|Assignee:||Alpharma Pharmaceuticals, LLC (Bridgewater, NJ)|
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; 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.degree. 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.degree. C. using USP paddle method, 100 rotations per minute, and then determining the amount of the naltrexone HCl sequestered.
2. The composition of claim 1, wherein the composition, after being orally taken by a human in the fed state, results in the human having an area under the plasma concentration versus time curve for 6-beta-naltrexol, at 168 hours (AUC.sub.last), of 1057 pg*wmL.
3. The composition of claim 2, wherein the composition, after being orally taken by the human in the fed state, results in the human having a time to maximum concentration for 6-beta-naltrexol (T.sub.max), in the human's plasma, of 57.29 hours.
4. The composition of claim 2, wherein the composition, after being orally taken by the human in the fed state, results in the human having a maximum concentration of 6-beta-naltrexol (C.sub.max) in the human's plasma, of 25 pg/mL.
5. The composition of claim 1, wherein the controlled release layer comprises a cellulose; a polyalkylene glycol; an anionic copolymer based on methacrylic acid and ethylacrylate; and a plasticizer.
6. The composition of claim 1, wherein the composition does not contain a bittering agent, a gelling agent, an irritant, or an emetic.
7. The composition of claim 1, wherein in said multi-layer pellets, antagonist is contained only in the antagonist containing layer.
8. The composition of claim 1, wherein in said multi-layer pellets, agonist is contained only in the agonist layer.
9. The composition of claim 1, wherein in said multi-layer pellets, the only agonist is the morphine sulfate.
10. The composition of claim 1, wherein in said multi-layer pellets, the only antagonist is the naltrexone HCl.
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