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Claims for Patent: 7,410,978

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Claims for Patent: 7,410,978

Title:Once daily dosage forms of trospium
Abstract:A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C.sub.min) and maximum (C.sub.max) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.
Inventor(s): Kidane; Argaw (Montgomery Village, MD), Flanner; Henry H. (Montgomery Village, MD), Bhatt; Padmanabh (Rockville, MD), Raoufinia; Arash (McLean, VA)
Assignee: Supernus Pharmaceuticals, Inc. (Rockville, MD)
Application Number:10/980,818
Patent Claims: 1. A pharmaceutical composition suitable for a once-a-day administration of trospium chloride comprising controlled release solid, trospium chloride-bearing particulates, at least a portion of which releases trospium chloride in the lower gastrointestinal (GI) tract, such that once-a-day administration of said pharmaceutical composition provides steady state blood levels of trospium that are comparable to steady state blood levels of trospium achieved with twice daily administration of 20 mg immediate release trospium chloride tablets, said particulates comprising at least one polymer selected from enteric polymers, release controlling polymers, or combinations thereof.

2. The composition of claim 1, in which once-a-day administration of said controlled release pharmaceutical composition provides steady state blood levels of trospium in the range of about 0.5 ng/ml to about 6.0 ng/ml.

3. The composition of claim 2, in which once-a-day administration of said controlled release pharmaceutical composition provides steady state blood C.sub.max levels of trospium in the range of about 2.5 ng/ml to about 4.5 ng/ml and C.sub.min levels of trospium in the range of about 0.5 ng/ml to about 1.5 ng/ml.

4. The composition of claim 2, in which once-a-day administration of said controlled release pharmaceutical composition provides steady state areas under the curve (AUCs) in the range of about 30 to about 60 ng/ml*hr.

5. The composition of claim 4, in which once-a-day administration of said controlled release pharmaceutical composition provides steady state areas under the curve in the range of about 35 to about 45 ng/ml*hr.

6. The composition of claim 1, in which once-a-day administration of said controlled release pharmaceutical composition provides single dose % F values in the range of about 80 to about 120.

7. The composition of claim 6 in which once-a-day administration of said controlled release pharmaceutical composition provides single dose % F values in the range of about 90 to about 110.

8. The composition of claim 1, in which said particulates are selected from the group consisting of (a) an extended release, (b) a delayed release, (c) a combination of extended release and delayed release, (d) a combination of either an extended release or a delayed release with an immediate release and (e) a combination of both an extended release and a delayed release with an immediate release formulation.

9. The composition of claim 8, in which the particulates are all of a delayed release formulation.

10. The composition of claim 8, in which the particulates are all of an extended release formulation that allows release of about 80% trospium chloride at 3.5 hours post ingestion.

11. The composition of claim 8, in which the particulates are all of an extended release formulation that allows release of about 80% trospium chloride at 4.5 hours post ingestion.

12. The composition of claim 8, which comprises particulates of an extended release formulation that allows release of about 80% trospium chloride at 3.5 hours post ingestion, and delayed release particulates.

13. The composition of claim 12, wherein the delayed release particulates are ones that release trospium chloride when they reach the area of the GI tract where the pH is about 7.

14. The composition of claim 1 in which said release controlling polymers are selected from a group consisting of copolymer of acrylic and methacrylic acid esters, ethylcellulose aqueous dispersions, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone/vinyl acetate copolymer, polyethylene glycols and combinations thereof.

15. The composition of claim 1 in which said enteric polymers are selected from a group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, polyvinyl acetate phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate trimellitate, hydroxypropyl methylcellulose succinate, cellulose acetate succinate, cellulose acetate hexahydrophthalate, cellulose propionate phthalate, copolymer of methylmethacrylic acid and methyl methacrylate, copolymer of methyl acrylate, methylmethacrylate and methacrylic acid, copolymer of methylvinyl ether and maleic anhydride, ethyl methyacrylate-methylmethacrylate-chlorotrimethylammonium ethyl acrylate copolymer, zein, shellac, copal collophorium, carboxymethyl ethylcellulose, co-polymerized methacrylic acid/methacrylic acid methyl esters and combinations thereof.

16. The composition of claim 1 in which at least some of said particulates are comprised of a trospium-containing core, which is coated with at least one polymer selected from enteric polymers, release controlling polymers, or combinations thereof.

17. A pharmaceutical composition comprising trospium chloride as at least one active pharmaceutical ingredient in which at least a portion of said trospium chloride is contained in a delayed release formulation, which does not release trospium chloride at a pH of below about 7.0, said delayed release formulation comprising at least one enteric polymer.

18. A pharmaceutical composition comprising trospium chloride as at least one active pharmaceutical ingredient in which at least a portion of said trospium chloride is contained in a delayed release formulation, which releases trospium chloride in the lower GI tract, said delayed release formulation comprising at least one enteric polymer.

19. The composition of claim 1 or claim 18, wherein said lower GI tract is the colon.

20. A pharmaceutical composition suitable for a once-a-day administration of trospium chloride comprising controlled release solid, trospium chloride-bearing particulates, at least a portion of which releases trospium chloride in the ileum, colon or both, such that once-a-day administration of said pharmaceutical composition provides steady state blood levels of trospium in the range of about 0.5 ng/ml to about 6.0 ng/ml, said particulates comprising at least one polymer selected from enteric polymers, release controlling polymers, or combinations thereof.

21. The pharmaceutical composition of claim 20 such that once-a-day administration of said pharmaceutical composition provides steady state blood levels of trospium in the range of about 0.5 ng/ml to about 3.0 ng/ml.

22. The pharmaceutical composition of claim 20 in which said particulates are in a formulation selected from the group consisting of (a) an extended release, (b) a delayed release, (c) a combination of extended release and delayed release, (d) a combination of either an extended release or a delayed release with an immediate release and (e) a combination of both an extended release and a delayed release with an immediate release formulation.

23. A once-a-day dosage form of trospium chloride comprising one or more controlled release particulates, at least a portion of which releases trospium chloride in the ileum, colon, or both, which upon once daily oral administration to a subject in need thereof provides effective amounts of trospium chloride to treat said subject's condition while minimizing the occurrence of adverse side effects following oral administration of an immediate release formulation containing 40 mg of trospium chloride, said particulates comprising at least one polymer selected from enteric polymers, release controlling polymers, or combinations thereof.

24. The once-a-day dosage form of claim 23, which provides a minimum blood or plasma trospium concentration at steady state which is above the minimum therapeutically effective blood or plasma concentration.

25. The once-a-day dosage form of claim 24, which provides a minimum steady state blood or plasma concentration that does not fall below about 0.5 ng/ml.

26. The once-a-day dosage form of claim 23, which provides a maximum blood or plasma trospium concentration at steady state which is below the maximum toxic blood or plasma concentration.

27. The once-a-day dosage form of claim 26, which provides a maximum steady state blood or plasma concentration that does not exceed about 6.0 ng/ml.

28. The once-a-day dosage form of claim 27 which provides a maximum steady state blood or plasma concentration that does not exceed about 3.0 ng/ml.

29. The once-a-day dosage form of claim 23, which provides effective amounts of trospium chloride to treat one or more bladder dysfunctions selected from the group consisting of urinary frequency, urgency, nocturia, and urge-incontinence due to detrusor instability, urge syndrome, and detrusor hyperreflexia.

30. The once-a-day dosage form of claim 23, which provides effective amounts of trospium chloride to treat one or more bladder dysfunctions selected from the group consisting of urinary frequency, urgency, nocturia, and urge-incontinence due to detrusor instability, urge syndrome, and detrusor hyperreflexia.

31. The once-a-day dosage form of claim 23 in which the adverse side effects comprise at least one of dry mouth, headache, constipation, dyspepsia, abdominal pain, or combinations thereof.

32. The once-a-day dosage form of claim 23 which comprises between about 25 mg and about 80 mg of trospium chloride.

33. The once-a-day dosage form of claim 23, which comprises between about 30 mg and about 60 mg of trospium chloride.

34. The once-a-day dosage form of claim 23, which comprises about 30 mg of trospium chloride.

35. The once-a-day dosage form of claim 23, which comprises about 40 mg of trospium chloride.

36. The once-a-day dosage form of claim 23, which comprises about 50 mg of trospium chloride.

37. The once-a-day dosage form of claim 23, which comprises about 60 mg of trospium chloride.
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