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Claims for Patent: 6,613,357

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Claims for Patent: 6,613,357

Title: Osmotic device containing pseudoephedrine and an H1 antagonist
Abstract:The present invention provides an osmotic device containing controlled release pseudoephedrine in the core in combination with a rapid release H1 antagonist in an external coat. A wide range of H1 antagonist antihistamines, especially fexofenadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of respiratory congestion related disorders and allergy related disorders. The present devices provide PS and an H1 antagonist according to specific release profiles in combination with specific formulations.
Inventor(s): Faour; Joaquina (Buenos Aires, AR), Ricci; Marcelo A. (Buenos Aires, AR)
Assignee: Osmotica Corp. (Tortola, VG)
Application Number:09/725,655
Patent Claims: 1. An osmotic device comprising: (a) a core comprising a therapeutically effective amount of pseudoephedrine which is delivered at a controlled rate over a period of about 18-24 hours; (b) a semipermeable membrane surrounding the core and a passageway through the semipermeable membrane; (c) an inert water soluble or erodible coating surrounding the semipermeable membrane and plugging the passageway; and (d) a fexofenadine-containing water soluble or erodible coating surrounding the inert water soluble coating for delivering all of the fexofenadine at a rapid rate over a period of less than about 90 min, wherein: 1) 10-25% of the PS is released within 3 hours; 2) 25-50% of the PS is released within 7 hours; 3) 50-66% of the PS is released within 11 hours; 4) 66-79% of the PS is released within 15 hours; and 5) 79-100% of the PS is released within 23 hours after exposure to an aqueous environment.

2. The osmotic device of claim 1, wherein about 60-240 mg of pseudoephedrine are present and about 60-180 mg of fexofenadine are present.

3. The osmotic device of claim 1, wherein the drug-containing water soluble or erodible coating is present in an amount of at least about 25% wt. based upon the total weight of the osmotic device.

4. The osmotic device of claim 1, wherein the drug-containing water soluble or erodible coating is present in an amount of about 25-40% wt. based upon the total weight of the osmotic device.

5. The osmotic device of claim 1, wherein the drug-containing water soluble or erodible coating is present in an amount of about 30-40% wt. based upon the total weight of the osmotic device.

6. The osmotic device of claim 1, wherein the pseudoephedrine is released at a zero-order or pseudo-zero order rate.

7. The osmotic device of claim 1, wherein all of the fexofenadine is released over a period of less than about 60 min.

8. The osmotic device of claim 1, wherein all of the fexofenadine is released over a period of less than about 45 min.

9. The osmotic device of claim 1, wherein all of the fexofenadine is released over a period of less than about 30 min.

10. The osmotic device of claim 1, wherein all of the fexofenadine is released over a period of less than about 20 min.

11. The osmotic device of claim 1, wherein all of the fexofenadine is released over a period of less than about 10 min.

12. The osmotic device of claim 2, wherein: the core further comprises an osmagent, a diluent and a binder; the semipermeable membrane comprises a cellulose ester and a plasticizer; the inert water soluble or erodible coating comprises a water soluble polymer, an opaquant and a filler; and the fexofenadine-containing water soluble or erodible coating further comprises a film forming polymer and a disintegrant.

13. The osmotic device of claim 12, wherein: the osmagent is selected from the group consisting of sodium chloride, salt, mannitol, acid, sugar, base, calcium salt, sodium salt, and lactose; the diluent is selected from the group consisting of microcrystalline cellulose, lactose, sucrose, mannitol, cellulose, starch, sorbitol, dibasic calcium phosphate, and calcium carbonate; the binder is selected from the group consisting of poly(vinylpyrrolidone), povidone, sodium carboxymethylcellulose, alginic acid, poly(ethylene glycol), guar gum, polysaccharide, bentonite clay, sugar, poloxamer, collagen, albumin, gelatin, poly(propylene glycol), and poly(ethylene oxide); the cellulose ester is selected from the group consisting of cellulose acetate, cellulose acylate, cellulose fatty acid ester, and cellulose acetate phthalate; the plasticizer is independently selected at each occurrence from the group consisting of poly(ethylene glycol), low molecular weight polymer, citrate ester, triacetin, propylene glycol, glycerin, sorbitol lactate, ethyl lactate, butyl lactate, ethyl glycolate, and dibutylsebacate; the water soluble polymer is independently selected at each occurrence from the group consisting of hydroxypropyl methylcellulose, poly(vinlypyrrolidone)-(vinyl acetate) copolymer, poly(vinylpyrrolidone), methyl methacrylate, calcium pectinate, poly(ethylene-vinyl acetate), hydroxylalkyl alkylcellulose, polyvinylalcohol, polyethylene oxide, a blend of gelatin and polyvinyl-pyrrolidone, gelatin, glucose, saccharide, povidone, copovidone, and polysaccharide gum; the film forming polymer is selected from the group consisting of hydroxypropyl methylcellulose, and poly(vinylpyrrolidone); the disintegrant is selected from the group consisting of crospovidone, bentonite clay, microcrystalline cellulose, starch, carboxymethylcellulose, alginate, sodium starch glycolate, and gum.

14. The osmotic device of claim 13, wherein: the opaquant is selected from the group consisting of titanium dioxide and talc; and the filler is selected from the group consisting of talc and starch.

15. The osmotic device of claim 12, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 35-45 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-25 mg; and the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 50-70 mg.

16. The osmotic device of claim 12, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 40-50 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 10-20 mg; the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 5-10 mg; and the fexofenadine-containing water soluble or erodible coating further comprises a water soluble copolymer present in an amount ranging from 20-30 mg.

17. The osmotic device of claim 12, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 35-45 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-40 mg; and the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-30 mg.

18. A method of treating a respiratory congestion related disorder in a mammal comprising the step of administering an osmotic device according to any one of claims 1-3, 6-7, 12-13, 15-17.

19. An osmotic device comprising: (a) a core comprising a therapeutically effective amount of pseudoephedrine which is delivered at a controlled rate over a period of about 18-24 hours; (b) a semipermeable membrane surrounding the core and a passageway through the semipermeable membrane; (c) an inert water soluble or erodible coating surrounding the semipermeable membrane and plugging the passageway; and (d) a fexofenadine-containing water soluble or erodible coating surrounding the inert water soluble coating for delivering all of the fexofenadine at a rapid rate over a period of less than about 90 min, wherein: 1) 9-11% of the PS is released within 3 hours; 2) 19-22% of the PS is released within 5 hours; 3) 28-31% of the PS is released within 7 hours; 4) 35-40% of the PS is released within 9 hours; 5) 45-50% of the PS is released within 11 hours; 6) 50-55% of the PS is released within 13 hours; 7) 60-65% of the PS is released within 15 hours; and 8) at least 75% of the PS is released within 23 hours after exposure to an aqueous environment.

20. The osmotic device of claim 19, wherein about 60-240 mg of pseudoephedrine are present and about 60-180 mg of fexofenadine are present.

21. The osmotic device of claim 19, wherein the drug-containing water soluble or erodible coating is present in an amount of at least about 25% wt. based upon the device.

22. The osmotic device of claim 19, wherein the drug-containing water soluble or erodible coating is present in an amount of about 25-40% wt. based upon the total weight of the osmotic device.

23. The osmotic device of claim 19, wherein the drug-containing water soluble or erodible coating is present in an amount of about 30-40% wt. based upon the total weight of the osmotic device.

24. The osmotic device of claim 19, wherein the pseudoephedrine is released at a zero-order or pseudo-zero order rate.

25. The osmotic device of claim 19, wherein all of the fexofenadine is released over a period of less than about 60 min.

26. The osmotic device of claim 19, wherein all of the fexofenadine is released over period of less than about 45 min.

27. The osmotic device of claim 19, wherein all of the fexofenadine is released ever a period of less than about 30 min.

28. The osmotic device of claim 19, wherein all of the fexofenadine is released over a period of less than about 20 min.

29. The osmotic device of claim 19, wherein all of the fexofenadine is released over a period of less than about 10 min.

30. The osmotic device of claim 20, wherein: the core further comprises an osmagent, a diluent and a binder; the semipermeable membrane comprises a cellulose ester and a plasticizer; the inert water soluble or erodible coating comprises a water soluble polymer, an opaquant and a filler; and the fexofenadine-containing water soluble or erodible coating further comprises a film forming polymer and a disintegrant.

31. The osmotic device of claim 30, wherein: the osmagent is selected from the group consisting of sodium chloride, salt, mannitol, acid, sugar, base, calcium salt, sodium salt, and lactose; the diluent is selected from the group consisting of microcrystalline cellulose, lactose, sucrose, mannitol, cellulose, starch, sorbitol, dibasic calcium phosphate, and calcium carbonate; the binder is selected from the group consisting of poly(vinylpyrrolidone), povidone, sodium carboxymethylcellulose, alginic acid, poly(ethylene glycol), guar gum, polysaccharide, bentonite clay, sugar, poloxamer, collagen, albumin, gelatin, poly(propylene glycol), and poly(ethylene oxide); the cellulose ester is selected from the group consisting of cellulose acetate, cellulose acylate, cellulose fatty acid ester, and cellulose acetate phthalate; the plasticizer is independently selected at each occurrence from the group consisting of poly(ethylene glycol), low molecular weight polymer, citrate ester, triacetin, propylene glycol, glycerin, sorbitol lactate, ethyl lactate, butyl lactate, ethyl glycolate, and dibutylsebacate; the water soluble polymer is independently selected at each occurrence from the group consisting of hydroxypropyl methylcellulose, poly(vinlypyrrolidone)-(vinyl acetate) copolymer, poly(vinylpyrrolidone), methyl methacrylate, calcium pectinate, poly(ethylene-vinyl acetate), hydroxylalkyl alkylcellulose, polyvinylalcohol, polyethylene oxide, a blend of gelatin and polyvinyl-pyrrolidone, gelatin, glucose, saccharide, povidone, copovidone, and polysaccharide gum; the film forming polymer is selected from the group consisting of hydroxypropyl methylcellulose, and poly(vinylpyrrolidone); the disintegrant is selected from the group consisting of crospovidone, bentonite clay, microcrystalline cellulose, starch, carboxymethyleellulose, alginate, sodium starch glycolate, and gum.

32. The osmotic device of claim 31 wherein: the opaquant is selected from the group consisting of titanium dioxide and talc; and the filler is selected from the group consisting of talc and starch.

33. The osmotic device of claim 30, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 35-45 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-25 mg; and the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 50-70 mg.

34. The osmotic device of claim 30, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 40-50 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 10-20 mg; the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 5-10 mg; and the fexofenadine-containing water soluble or erodible coating further comprises a water soluble copolymer present in an amount ranging from 20-30 mg.

35. The osmotic device of claim 30, wherein: the osmagent is present in an amount ranging from 70-90 mg; the diluent is present in an amount ranging from 30-40 mg; the binder is present in an amount ranging from 40-60 mg; the cellulose ester is present in an amount ranging from 35-45 mg; the film-forming polymer in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-40 mg; and the disintegrant in the fexofenadine-containing water soluble or erodible coating is present in an amount ranging from 20-30 mg.

36. An osmotic device comprising: (a) a core comprising a therapeutically effective amount of pseudoephedrine which is delivered at a controlled rate over a period of about 18-24 hours; (b) a semipermeable membrane surrounding the core and a passageway through the semipermeable membrane; (c) an inert water soluble or erodible coating surrounding the semipermeable membrane and plugging the passageway; and (d) a fexofenadine-containing water soluble or erodible coating surrounding the inert water soluble coating for delivering all of the fexofenadine at a rapid rate over a period of less than about 90 min, wherein: 1) 5-23% of the PS is released within 3 hours; 2) 20-52% of the PS is released within 7 hours; 3) 36-72% of the PS is released within 11 hours; 4)53-82% of the PS is released within 15 hours; and 5) at least 75% of the PS is released within 23 hours after exposure to an aqueous environment.

37. A method of treating a respiratory congestion related disorder in a mammal rising the step of administering an osmotic device according to any one of claims 19-35 or 36.
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