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Details for Patent: 5,273,760

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Details for Patent: 5,273,760

Title: Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer
Abstract:A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active agent with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.
Inventor(s): Oshlack; Benjamin (New York, NY), Pedi, Jr.; Frank (Yorktown Heights, NY), Chasin; Mark (Manalapan, NJ)
Assignee: Euroceltigue, S.A. (Luxembourg, LU)
Filing Date:Dec 24, 1991
Application Number:07/814,111
Claims:1. A method for obtaining a stabilized controlled release formulation comprising a substrate coated with an aqueous dispersion of ethylcellulose, comprising

preparing a solid substrate comprising a therapeutically active agent,

overcoating said substrate with a sufficient amount of an aqueous dispersion of plasticized ethylcellulose to obtain a predetermined controlled release of said therapeutically active agent when said coated substrate is exposed to aqueous solutions,

curing said coated substrate at a temperature greater than the glass transition temperature of the aqueous dispersion of ethylcellulose and at a relative humidity from about 60% to about 100 %, and continuing the curing until an endpoint is reached at which said cured coated substrate provides a stable dissolution profile, said endpoint being determined by comparing the dissolution profile of the formulation immediately after curing to the dissolution profile of the formulation after exposure to accelerated storage conditions of one month at a temperature of 37.degree. C. and at a relative humidity of 80%.

2. The method of claim 1, further comprising preparing said solid substrate for oral administration by overcoating said therapeutically active agent onto the surface of pharmaceutically acceptable inert beads, and after overcoating and curing said beads, preparing an oral dosage form by placing a sufficient quantity of cured coated beads into a capsule to provide a therapeutic effect when administered.

3. The method of claim 2, wherein said coated beads are coated to a weight gain from about 5 to about 15 percent, and are thereafter cured for about 48 to about 72 hours, until the endpont is reached.

4. The product prepared according to the method of claim 2.

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

6. The product prepared according to the method of claim 1.

7. The method of claim 1, further comprising overcoating said substrate comprising said therapeutically active agent with a barrier agent prior to overcoating with said aqueous dispersion of ethylcellulose.

8. The method of claim 7, wherein said barrier agent comprises hydroxypropyl methylcellulose.

9. 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

10. The method of claim 1, wherein said therapeutically active agent is selected from the group consisting of hydromorphone, oxycodone, dihydrocodeine, codeine, dihydromorphine, morphine, buprenorphine, salts of any of the foregoing, and mixtures of any of the foregoing.

11. The method of claim 1, wherein said therapeutically active agent is theophylline.

12. The product prepared according to the method of claim 1.

13. A stabilized solid controlled release dosage form comprising a substrate comprising a therapeutically active agent, said substrate overcoated with an aqueous dispersion of plasticized ethylcellulose and cured at a temperature greater than the glass transition temperature of the aqueous dispersion of the plasticized ethylcellulose and at a relative humidity from about 60% to about 100% until an endpoint is reached at which said cured coated substrate provides a stable dissolution profile, said endpoint being determined by comparing the dissolution profile of the formulation immediately after curing to the dissolution profile of the formulation after exposure to accelerated storage conditions of one month at a temperature of 37.degree. C. and at a relative humidity of 80%.

14. The stabilized solid controlled release dosage form of claim 13, wherein said therapeutically active agent is overcoated with said aqueous dispersion of ethylcellulose to a weight gain level from about 5 to about 15 percent.

15. The stabilized solid controlled release dosage form of claim 14, wherein said substrate further comprises inert pharmaceutically acceptable beads onto which said therapeutically active agent is coated.

16. The stabilized solid controlled release dosage form of claim 15, wherein a plurality of said coated, cured beads are placed in a capsule in an amount sufficient to provide an effective controlled release dose when contacted by an aqueous solution.

17. The stabilized solid controlled release dosage form of claim 13, 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

18. The stabilized solid controlled release dosage form of claim 13, wherein said therapeutically active agent is selected from the group consisting of hydromorphone, oxycodone, dihydrocodeine, codeine, dihydromorphone, morphine, buprenorphine, salts of any of the foregoing, and mixtures of any of the foregoing.

19. The stabilized solid controlled release dosage form of claim 13, wherein said therapeutically active agent is theophylline.

20. A stabilized controlled release solid dosage form for oral administration, comprising a plurality of inert pharmaceutically acceptable beads coated with a therapeutically active agent, and overcoated with an aqueous dispersion of plasticized ethylcellulose to a thickness effective to obtain a controlled release of said therapeutically active agent when said solid dosage form is exposed to aqueous solutions, said overcoated beads included in said formulation in an amount sufficient to provide a desired therapeutic effect,

said overcoated beads cured at a temperature greater than the glass transition temperature of the aqueous dispersion of plasticized ethylcellulose and at a relative humidity from about 60% to about 100%, until an endpoint is reached at which said cured overcoated beads provide a stable dissolution profile, said endpoint being determined by comparing the dissolution profile of the formulation immediately after curing to the dissolution profile of the formulation after exposure to accelerated storage conditions of one month at a temperature of 37.degree. C. and at a relative humidity of 80%.

21. The stabilized controlled release solid dosage form of claim 20, wherein said beads are coated with said aqueous dispersion of plasticized ethylcellulose to a weight gain from about 5 to about 15 percent, and said beads are thereafter cured for about 48 to about 72 hours, until the endpoint is reached.

22. The stabilized solid controlled release dosage form of claim 20, wherein a plurality of said coated, cured beads are placed in a capsule in an amount sufficient to provide an effective controlled release dose when contacted by an aqueous solution.

23. The stabilized solid controlled release dosage form of claim 20, 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, hormones, diuretics, anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

24. The stabilized solid controlled release dosage form of claim 20, wherein said therapeutically active agent is selected from the group consisting of hydromorphone, oxycodone, dihydrocodeine, codeine, dihydromorphine, morphine, buprenorphine, salts of any of the foregoing, and mixtures of any of the foregoing.

25. The stabilized solid controlled release dosage form of claim 20, wherein said therapeutically active agent is theophylline.

26. A solid dosage form comprising a plurality of inert pharmaceutically acceptable beads comprising a therapeutically active agent overcoated with an aqueous dispersion of ethylcellulose to a weight gain sufficient to obtain a controlled release of said therapeutically active agent when said dosage form is exposed to aqueous solutions, said solid dosage form being cured after said overcoating is applied at a temperature greater than the glass transition temperature of said aqueous dispersion of ethylcellulose and at a relative humidity from about 60% to about 100% for a time period from about 48 hours to about 72 hours, until said cured coated dosage form exhibits a stable in-vitro release of said therapeutically active agent when exposed to accelerated storage conditions of one month at about 37.degree. C. and 80% relative humidity.

27. The solid dosage form of claim 26, wherein said beads are coated with said aqueous dispersion of plasticized ethylcellulose to a weight gain from about 5 to about 15 percent.

28. The solid dosage form of claim 27, wherein said coated beads are cured at a temperature of about 60.degree. C. and at a relative humidity of about 85%.

29. The solid dosage form of claim 26, 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, diuretics, anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

30. A method of stabilizing a substrate comprising a therapeutically active agent overcoated with an aqueous dispersion of plasticized ethylcellulose in an amount sufficient to obtain a controlled release of the therapeutically active agent when the coated substrate is exposed to aqueous solutions, comprising subjecting the coated substrate to curing at a temperature greater than the glass transition temperature of said aqueous dispersion of plasticized ethylcellulose and at a relative humidity from about 60% to about 100%, for a period of time necessary to obtain a final product which exhibits a stable in-vitro release of said therapeutically active agent when exposed to accelerated storage conditions of one month at 37.degree. C. and 80% relative humidity.

31. The method of claim 30, further comprising preparing the coated substrate by applying said therapeutically active agent onto the surface of a pharmaceutically inert bead, and conducting said curing step by oven curing.

32. The method of claim 30, 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, diuretics anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.

33. A stabilized solid controlled release dosage form comprising a substrate comprising a therapeutically active agent, said substrate overcoated with an aqueous dispersion of plasticized ethylcellulose to a sufficient weight gain such that a controlled release of said therapeutically active agent is obtained when said dosage form is exposed to aqueous solutions, said overcoated substrate cured at a temperature greater than the glass transition temperature of said aqueous dispersion of plasticized ethylcellulose and at a relative humidity from about 60 to about 100 percent for a time period necessary to obtain a final product which exhibits a stable in-vitro release of said therapeutically active agent when exposed to accelerated storage conditions of one month at 37.degree. C. and 80% relative humidity.

34. The stabilized solid controlled release dosage form of claim 33, 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, vasodilators, anti-tussive agents, expectorants, anti-asthmatics, diuretics, anti-hypotensives, bronchodilators, antibiotics, antihemorrhoidals, hypnotics, psychotropics, antidiarrheals, mucolytics, sedatives, decongestants, laxatives, vitamins, and stimulants.
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