US2012189705A1PendingUtilityA1

Pharmaceutical Compositions

59
Assignee: MATTHEWS FRANKPriority: Jun 19, 2006Filed: Mar 23, 2012Published: Jul 26, 2012
Est. expiryJun 19, 2026(expired)· nominal 20-yr term from priority
Inventors:Frank MatthewsGarth BoehmLijuan TangAlfred Liang
A61P 43/00A61P 25/04A61P 29/00A61P 25/36A61K 9/5015A61K 31/485G01N 33/15A61K 9/5078A61K 9/5073A61K 9/167A61K 9/50A61K 9/1676A61K 9/4808A61K 9/5026A61K 9/20A61K 9/16G01N 33/48
59
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Claims

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.

Claims

exact text as granted — not AI-modified
1 - 79 . (canceled) 
     
     
         80 . A composition comprising a plurality of multi-layer pellets comprising:
 a. a core;   b. an opioid antagonist comprising layer coating the core in which said antagonist is naltrexone, or a pharmaceutically acceptable salt thereof;   c. a sequestering polymer layer coating said opioid antagonist;   d. said polymer layer contains a sufficient quantity of a polymer, a surfactant, and talc so that when tested by a method, the formulation sequesters at least 98% of said naltrexone as determined at 73 hours, and;   e. the testing method consists of 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 opioid antagonist sequestered.   
     
     
         81 . The composition according to  claim 80  in which said polymer is an acrylic polymer. 
     
     
         82 . The composition according to  claim 80  in which said acrylic polymer is selected from the group consisting of methacrylic polymers, acrylic acid and methacrylic acid copolymers, methyl methacrylate copolymers, ethoxyethyl methacrylates, cyanoethyl methacrylate, poly(acrylic add), poly(methacrylic acid), methacrylic acid alkylamide copolymer, poly(methyl methacrylate), polymethacrylate, poly(methyl methacrylate) copolymer, polyacrylamide, aminoalkyl methacrylate copolymer, poly(methacrylic acid anhydride), and glycidyl methacrylate copolymers, 
     
     
         83 . The composition according to  claim 80  in which said surfactant is selected from the group consisting of alkylaryl sulphonates, alcohol sulphates, sulphosuccinates, sulphosuccinamates, sarcosinates, taurates, ethoxylated castor oil, benzalkoniurn chloride, colyglycolyzed glycerides, acetylated monoglycerides, sorbitan fatty acid esters, poloxamers, polyoxyethylene fatty acid esters, sodium docusate, sodium lauryl sulfate, dioctyl sodium sulphosuccinate, sodium lauryl sarcosinate, sodium methyl cocoyl taurate, magnesium lauryl sulfate, triethanolamine, cetrimide, sucrose laurate, dioctyl sodium sulfosuceinate, sodium dodecyl benzene sulfonate, dialkyl sodium sulfosuccinate, lecithins, and phospholipids. 
     
     
         84 . The composition according to  claim 80  in which said surfactant is selected from the group consisting of sodium lauryl sulfate, sodium docusate, dioctyl sodium sulphosuccinate, sodium lauryl sarcosinate, sodium methyl cocyl taurate, magnesium lauryl sulfate, dioctyl sodium sulfosuceinate, and sodium dodecylbenzene sulfonate 
     
     
         85 . The composition according to  claim 80  in which said acrylic polymer is a copolymer of acrylic and methacrylic acid esters with quaternary ammonium groups. 
     
     
         86 . The composition according to  claim 80  in which said surfactant is sodium lauryl sulfate. 
     
     
         87 . The composition according to  claim 85  in which said surfactant is sodium lauryl sulfate. 
     
     
         88 . The composition according to  claim 84  in which said surfactant is present in the quantity of 6.3%, or less, on a w/w basis, relative to the quantity of polymer present. 
     
     
         89 . The composition according to  claim 86  in which said sodium lauryl sulfate is present in the quantity of 6.3%, or less, on a w/w basis, relative to the quantity of polymer present. 
     
     
         90 . The composition according to  claim 87  in which said sodium lauryl sulfate is present in the quantity of 6.3%, or less, on a w/w basis, relative to the quantity of polymer present. 
     
     
         91 . The composition according to  claim 80  in which said talc is present in the quantity of from 75% to 125%, on a w/w basis, relative to the quantity of polymer present. 
     
     
         92 . The composition according to  claim 85  in which said talc is present in the quantity of from 75% to 125%, on a w/w basis, relative to the quantity of polymer present. 
     
     
         93 . The composition according to  claim 86  in which said talc is present in the quantity of from 75% to 125%, on a w/w basis, relative to the quantity of polymer present. 
     
     
         94 . The composition according to  claim 87  in which said talc is present in the quantity of from 75% to 125%, on a w/w basis, relative to the quantity of polymer present. 
     
     
         95 . The composition according to  claim 90  in which said talc is present in the quantity of from 75% to 125%, on a w/w basis, relative to the quantity of polymer present. 
     
     
         96 . The composition according to  claim 80  in which said sequestering polymer layer contains
 a. copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups; 
 b. a surfactant 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; 
 c. 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. 
 
     
     
         97 . The composition according to  claim 96  in which the surfactant is selected from the group consisting of sodium lauryl sulfate, sodium docusate, dioctyl sodium sulphosuccinate, sodium lauryl sarcosinate, sodium methyl cocyl taurate, magnesium lauryl sulfate, dioctyl sodium sulfosuceinate, and sodium dodecylbenzene sulfonate. 
     
     
         98 . The composition of  claim 96  in which said surfactant is sodium lauryl sulfate. 
     
     
         99 . The composition according to  claim 80  which further comprises an opioid agonist. 
     
     
         100 . The composition according to  claim 99  in which said agonist is oxycodone, morphine, or a pharmaceutically acceptable salt thereof. 
     
     
         101 . The composition according to  claim 99  in which said agonist is selected from the group consisting of morphine, oxycodone, hydrocodone, hydromorphone, dihydrocodeine, codeine, dihydromorphine, buprenorphine, or a pharmaceutically acceptable salt thereof. 
     
     
         102 . The composition according to  claim 80  which further comprises an osmotic pressure regulating agent layer exterior to said sequestering polymer layer. 
     
     
         103 . The composition according to  claim 85  which further comprises an osmotic pressure regulating agent layer exterior to said sequestering polymer layer. 
     
     
         104 . The composition according to  claim 88  which further comprises an osmotic pressure regulating agent layer exterior to said sequestering polymer layer. 
     
     
         105 . The composition according to  claim 95  which further comprises an osmotic pressure regulating agent layer exterior to said sequestering polymer layer. 
     
     
         106 . A composition comprising a plurality of multi-layer pellets comprising:
 a. a core;   b. an opioid antagonist comprising layer coating the core, wherein the opioid antagonist is naltrexone, or a pharmaceutically acceptable salt thereof;   c. a sequestering polymer layer coating the opioid antagonist layer;   wherein the sequestering polymer layer comprises:
 i) copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups, 
 ii) a surfactant 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, 
 iii) 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; and 
 iv) the surfactant is selected from the group consisting of sodium lauryl sulfate, sodium docusate, dioctyl sodium sulphosuccinate, sodium lauryl sarcosinate, sodium methyl cocyl taurate, magnesium lauryl sulfate, dioctyl sodium sulfosuceinate, sodium dodecylbenzene sulfonate, and combinations. 
   
     
     
         107 . The composition of  claim 106 , wherein when tested by a testing method, the composition sequesters at least 80% of the opioid antagonist as determined at 73 hours from the start of the testing method, wherein the testing method consists of 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 opioid antagonist sequestered.

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