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Details for Patent: 7,070,806

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Details for Patent: 7,070,806

Title:Controlled release formulations coated with aqueous dispersions of acrylic polymers
Abstract: A stable solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic acrylic polymer includes a substrate including an active agent selected from the group consisting of a systemically active therapeutic agent, a locally active therapeutic agent, a disinfecting and sanitizing agent, a cleansing agent, a fragrance agent and a fertilizing agent, overcoated with an aqueous dispersion of the plasticized water-insoluble acrylic polymer. The formulation provides a stable dissolution of the active agent which is unchanged after exposure to accelerated storage conditions.
Inventor(s): Oshlack; Benjamin (New York, NY), Chasin; Mark (Manalapan, NJ), Pedi, Jr.; Frank (Yorktown Heights, NY)
Assignee: Purdue Pharma LP (Stamford, CT)
Filing Date:Oct 17, 2002
Application Number:10/273,434
Claims:1. A method for preparing a controlled release formulation comprising: preparing a solid substrate comprising a therapeutically active agent, overcoating said substrate with an aqueous dispersion of a plasticized water-insoluble acrylic polymer, and curing said coated substrate at a temperature greater than the glass transition temperature of the coating for at least 24 hours, until a curing endpoint is reached, at which endpoint said cured coated substrate when subjected to accelerated storage conditions of at least one month at 37.degree. C./80% RH releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than 20% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated storage conditions.

2. The method of claim 1, wherein said water-insoluble acrylic polymer is comprised of monomers selected from the group consisting of an ester of acrylic acid, an ester of methacrylic acid, an alkyl ester acrylic acid, an alkyl ester of methacrylic acid, and mixtures of any of the foregoing.

3. The method of claim 1, wherein said therapeutically active agent is selected from the group consisting of antihistamines, analgesics, non-steroidal anti-inflammatory agents, gastro-intestinals, anti-emetics, anti-epileptics, vaso-dilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, anti-hypertensives, bronchodilators, antibiotics, antivirals, antihemorrhoidals, steroids, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

4. The method of claim 1, wherein said active agent is an opioid analgesic selected from the group consisting of hydromorphone, oxycodone, morphine, levorphanol, methadone, meperidine, heroin, dihydrocodeine, codeine, hydrocodone, tramadol, dihydromorphine, buprenorphone, mixed opiate receptor agonist-antagonists, salts, hydrates and solvents of any of the foregoing, and mixtures of any of the foregoing.

5. The method of claim 1, wherein said substrate is a tablet core.

6. The method of claim 1, wherein said formulation provides therapeutically effective blood levels of said systemically active therapeutic agent for about 24 hours.

7. The method of claim 1, wherein said step of comprises curing said coated substrate for a time period from about 24 to about 48 hours, until said endpoint is reached.

8. The method of claim 1, wherein said step of overcoating said substrate comprises including a portion of the amount of said active agent included in said formulation into a coating on said substrate.

9. The method of claim 1, wherein said water-insoluble acrylic polymer comprises a mixture of copolymers of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters from about 1:20 to about 1:40.

10. The method of claim 1, wherein said step of overcoating said substrate comprises coating said substrate with said aqueous dispersion of water-insoluble acrylic polymer to a weight gain from about 2 to about 25 percent.

11. The method of claim 1, wherein said water-insoluble acrylic polymer comprises a mixture of a first copolymer of acrylic and methacrylic esters having a molar ratio of ammoniuni groups to (meth)acrylic esters of about 1:20 and a second copolymer of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters of about 1:40, the ratio of said first copolymer to said second copolymer being from about 0:100 to about 100:0.

12. A method for preparing a controlled release formulation, comprising: preparing a solid substrate comprising a therapeutically active agent, overcoating said substrate with an aqueous dispersion of a plasticized water-insoluble acrylic polymer, and curing said coated substrate at a temperature greater than the glass transition temperature of the coating for at least 24 hours, until a curing endpoint is reached, at which endpoint said cured coated substrate when subjected to accelerated storage conditions of at least one month at 37.degree. C./80% RH and at least one month at 37.degree. C./dry releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than 20% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated storage conditions.

13. The method of claim 12, wherein said water-insoluble acrylic polymer is comprised of monomers selected from the group consisting of an ester of acrylic acid, an ester of methacrylic acid, an alkyl ester acrylic acid, an alkyl ester of methacrylic acid, and mixtures of any of the foregoing.

14. The method of claim 12, wherein said therapeutically active agent is selected from the group consisting of antihistamines, analgesics, non-steroidal anti-inflammatory agents, gastro-intestinals, anti-emetics, anti-epileptics, vaso-dilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, anti-hypertensives, bronchodilators, antibiotics, antivirals, antihemorrhoidals, steroids, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

15. The method of claim 12, wherein said active agent is an opioid analgesic selected from the group consisting of hydromorphone, oxycodone, morphine, levorphanol, methadone, meperidine, heroin, dihydrocodeine, codeine, hydrocodone, tramadol, dihydromorphine, buprenorphone, mixed opiate receptor agonist-antagonists, salts, hydrates and solvents of any of the foregoing, and mixtures of any of the foregoing.

16. The method of claim 12, wherein said substrate is a tablet core.

17. The method of claim 12, wherein said formulation provides therapeutically effective blood levels of said systemically active therapeutic agent for about 24 hours.

18. The method of claim 12, wherein said step of curing comprises curing said coated substrate for a time period from about 24 to about 48 hours, until said endpoint is reached.

19. The method of claim 12, wherein said step of overcoating said substrate comprises including a portion of the amount of said active agent included in said formulation is incorporated into a coating on said substrate.

20. The method of claim 12, wherein said water-insoluble acrylic polymer comprises a mixture of copolymers of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters from about 1:20 to about 1:40.

21. The method of claim 12, wherein said step of overcoating said substrate comprises coating said substrate with said aqueous dispersion of water-insoluble acrylic polymer to a weight gain from about 2 to about 25 percent.

22. The method of claim 12, wherein said water-insoluble acrylic polymer comprises a mixture of a first copolymer of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters of about 1:20 and a second copolymer of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters of about 1:40, the ratio of said first copolymer to said second copolymer being from about 0:100 to about 100:0.

23. A method for preparing a controlled release formulation, comprising: preparing a solid substrate comprising a therapeutically active agent, overcoating said substrate with an aqueous dispersion of a plasticized water-insoluble acrylic polymer, and curing said coated substrate at a temperature greater than the glass transition temperature of the coating for at least 24 hours, until a curing endpoint is reached, at which endpoint said cured coated substrate when subjected to storage conditions of at least one month at 37.degree. C./80% RH and at least one month at room temperature releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than 20% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated storage conditions.

24. The method of claim 23, wherein said water-insoluble acrylic polymer is comprised of monomers selected from the group consisting of an ester of acrylic acid, an ester of methacrylic acid, an alkyl ester acrylic acid, an alkyl ester of methacrylic acid, and mixtures of any of the foregoing.

25. The method of claim 23, wherein said therapeutically active agent is selected from the group consisting of antihistamines, analgesics, non-steroidal anti-inflammatory agents, gastro-intestinals, anti-emetics, anti-epileptics, vaso-dilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, anti-hypertensives, bronchodilators, antibiotics, antivirals, antihemorrhoidals, steroids, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

26. The method of claim 23, wherein said active agent is an opioid analgesic selected from the group consisting of hydromorphone, oxycodone, morphine, levorphanol, methadone, meperidine, heroin, dihydrocodeine, codeine, hydrocodone, traniadol, dihydromorphine, buprenorphone, mixed opiate receptor agonist-antagonists, salts, hydrates and solvents of any of the foregoing, and mixtures of any of the foregoing.

27. The method of claim 23, wherein said substrate is a tablet core.

28. The method of claim 23, wherein said formulation provides therapeutically effective blood levels of said systemically active therapeutic agent for about 24 hours.

29. The method of claim 23, wherein said step of curing comprises curing said coated substrate for a time period from about 24 to about 48 hours, until said endpoint is reached.

30. The method of claim 23, wherein said step of overcoating said substrate comprises including a portion of the amount of said active agent included in said formulation is incorporated into a coating on said substrate.

31. The method of claim 23, wherein said water-insoluble acrylic polymer comprises a mixture of copolymers of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters from about 1:20 to about 1:40.

32. The method of claim 23, wherein said step of overcoating said substrate comprises coating said substrate with said aqueous dispersion of water-insoluble acrylic polymer to a weight gain from about 2 to about 25 percent.

33. The method of claim 23, wherein said water-insoluble acrylic polymer comprises a mixture of a first copolymer of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters of about 1:20 and a second copolymer of acrylic and methacrylic esters having a molar ratio of ammonium groups to (meth)acrylic esters of about 1:40, the ratio of said first copolymer to said second copolymer being from about 0:100 to about 100:0.

34. The method of claim 1, wherein said plasticized water-insoluble acrylic polymer has a permeability that is unaffected by pH conditions prevailing in the gastrointestinal tract and is present in said overcoating in an amount sufficient to obtain a controlled release of said therapeutically active agent, after curing of the coated substrate, when measured by the USP Paddle or Basket Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 0% to about 42.5% (by wt.) active agent released after 1 hour, from about 5% to about 60% (by wt.) active agent release after 2 hours, from about 15% to about 75% (by wt.) active agent release after 4 hours, and from about 20% to about 90% % (by wt.) active agent released after 8 hours.

35. The method of claim 1, wherein said cured coated substrate, after being subjected to said accelerated conditions, releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than about 15% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated conditions.

36. The method of claim 12, wherein said plasticized water-insoluble acrylic polymer has a permeability that is unaffected by pH conditions prevailing in the gastrointestinal tract and is present in said overcoating in an amount sufficient to obtain a controlled release of said therapeutically active agent, after curing of the coated substrate, when measured by the USP Paddle or Basket Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 0% to about 42.5% (by wt.) active agent released after 1 hour, from about 5% to about 60% (by wt.) active agent release after 2 hours, from about 15% to about 75% (by wt.) active agent release after 4 hours, and from about 20% to about 90% % (by wt.) active agent released after 8 hours.

37. The method of claim 12, wherein said cured coated substrate, after being subjected to said accelerated conditions, releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than about 15% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated conditions.

38. The method of claim 23, wherein said plasticized water-insoluble acrylic polymer has a permeability that is unaffected by pH conditions prevailing in the gastrointestinal tract and is present in said overcoating in an amount sufficient to obtain a controlled release of said therapeutically active agent, after curing of the coated substrate, when measured by the USP Paddle or Basket Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 0% to about 42.5% (by wt.) active agent released after 1 hour, from about 5% to about 60% (by wt.) active agent release after 2 hours, from about 15% to about 75% (by wt.) active agent release after 4 hours, and from about 20% to about 90% (by wt.) active agent released after 8 hours.

39. The method of claim 23, wherein said cured coated substrate, after being subjected to said accelerated conditions, releases an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than about 15% of the total amount of active agent released, when compared to the in-vitro dissolution of said cured coated substrate prior to being subjected to said accelerated conditions.
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