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Claims for Patent: 7,781,449

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Claims for Patent: 7,781,449

Title:Trospium chloride treatment method
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:11/889,963
Patent Claims: 1. A method of treating a bladder dysfunction in a mammal comprising an oral administration to said mammal of a once-daily dose of a pharmaceutical composition comprising 25 to 80 mg of trospium chloride for at least a time sufficient to ameliorate said dysfunction, wherein at least part of the trospium chloride is contained in an extended release (XR) component or in a delayed release (DR) component, wherein said composition comprises at least one polymer selected from enteric polymers, release controlling polymers, or combinations thereof, wherein at least a portion of said composition releases trospium chloride in the lower gastrointestinal (GI) tract, wherein said administration provides steady state blood levels of trospium of a minimum of about 0.5 ng/ml and a maximum of about 6.0 ng/ml, and results in minimizing the occurrence of side effects as compared to twice daily administration of 20 mg of immediate release trospium chloride tablets; and wherein said bladder dysfunction is selected from the group consisting of urinary frequency, urgency, nocturia, and urge-incontinence due to detrusor instability, urge syndrome, and detrusor hyperreflexia.

2. The method of claim 1, wherein said administration results in steady state blood levels of trospium which are comparable to steady state blood levels of trospium achieved with twice daily administration of 20 mg of immediate release trospium chloride tablets.

3. The method of claim 1, wherein said XR component comprises at least one release controlling polymer selected from copolymers 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.

4. The method of claim 1, wherein said DR component comprises at least one enteric polymer selected from 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 methacrylate-methylmethacrylate-chlorotrimethylammonium ethyl acrylate copolymer, zein, shellac, copal collophorium, carboxymethyl ethylcellulose, co-polymerized methacrylic acid/methacrylic acid methyl esters and combinations thereof.

5. The method of claim 1, wherein said composition additionally comprises an immediate release (IR) trospium component.

6. The method of claim 5, wherein the IR component contains not more than about 20 mg of trospium chloride.

7. The method of claim 6, wherein said composition is a combination of an IR trospium chloride component and a DR trospium chloride component.

8. The method of claim 6, wherein said composition is a combination of an IR trospium chloride component and an XR trospium chloride component.

9. The method of claim 6, wherein said composition is a combination of an IR trospium chloride component, an XR trospium chloride component, and a DR trospium component.

10. The method of claim 1, wherein said composition is a combination of an XR trospium chloride component and a DR trospium chloride component.

11. The method of claim 10, wherein the DR component comprises trospium chloride and an enteric polymer, and the XR component comprises trospium chloride and a release controlling polymer.

12. The method of claim 11, wherein each one of XR component and DR component is in the form of pellets.

13. The method of claim 12, wherein said DR component is composed of DR pellets consisting essentially of trospium chloride, a sugar core, hydroxypropyl methylcellulose, a coating of the enteric polymer that delays release of the trospium chloride from the pellet for a period of time after administration, triethyl citrate, a protective overcoating, and talc; and wherein said XR component is composed of XR pellets consisting essentially of trospium chloride, a sugar core, hydroxypropyl methylcellulose, a surface coating that controls a release profile of the trospium chloride from the pellet after administration, a protective overcoating, and talc.

14. The method of claim 13, wherein the XR component contains about 30 mg of trospium chloride, and the DR component contains about 30 mg of trospium chloride.

15. The method of claim 1, wherein said DR component releases trospium chloride at a pH of about 7.0.

16. The method of claim 1, wherein said DR component releases trospium in the lower intestine.

17. The method of claim 1, wherein said DR component releases trospium chloride in the colon.

18. The method of claim 1, wherein said side effects are selected from a group consisting of dry mouth, headache, constipation, dyspepsia, abdominal pain, and a combination thereof.

19. The method of claim 1, wherein said composition is administered as an oral dosage form selected from a granule, tablet, pellet, beadlet, powder, sachet, capsule, gel, dispersion, solution or suspension.

20. The method of claim 19, wherein said tablet is a rapidly dispersible tablet.

21. The method of claim 19, wherein said tablet, pellet or beadlet is a layered tablet, pellet or beadlet comprising at least two trospium-containing layers, wherein each layer comprises at least one component selected from an XR component, a DR component or an immediate release (IR) component.

22. The method of claim 1, wherein said oral administration is carried out without the intake of high-fat food.

23. A method of treating a bladder dysfunction in a mammal comprising orally administering to said mammal a once-daily dose of a pharmaceutical composition of trospium chloride comprising a combination of a DR component and an XR component, wherein at least a portion of which releases trospium chloride in the lower gastrointestinal (GI) tract, wherein said DR component is composed of enteric coated pellets consisting essentially of: trospium chloride, a sugar core, hydroxypropyl methylcellulose, a coating of the enteric polymer that delays release of the trospium chloride from the pellet for a period of time after administration, triethyl citrate, a protective overcoating, and talc; and wherein said XR component is composed of extended release pellets consisting essentially of: trospium chloride, a sugar core, hydroxypropyl methylcellulose, a surface coating that controls a release profile of the trospium chloride from the pellet after administration, a protective overcoating, and talc, wherein said administration provides steady state blood levels of trospium of a minimum of about 0.5 ng/ml and a maximum of about 6.0 ng/ml and wherein the bladder dysfunction is selected from the group consisting of urinary frequency, urgency, nocturia, urge-incontinence associated with detrusor instability, urge syndrome, and detrusor hyperreflexia.

24. A method of treating a bladder dysfunction in a mammal comprising orally administering to said mammal a once-daily dose of a pharmaceutical composition comprising a mixture of enteric coated pellets and extended release pellets in a ratio of 1:1, wherein at least a portion of which releases trospium chloride in the lower gastrointestinal (GI) tract, the enteric coated pellets consisting essentially of trospium chloride, sugar spheres, hydroxypropyl methylcellulose, methacrylic acid copolymer, triethyl citrate, and talc and wherein the extended release pellets consist essentially of trospium chloride, sugar spheres, hydroxypropyl methylcellulose, ethyl cellulose, and talc, wherein said administration provides steady state blood levels of trospium of a minimum of about 0.5 ng/ml and a maximum of about 6.0 ng/ml, and wherein the bladder dysfunction is selected from the group consisting of urinary frequency, urgency, nocturia, urge-incontinence associated with detrusor instability, urge syndrome, and detrusor hyperreflexia.

25. The method of one of claim 23 or 24, wherein 60 mg of trospium chloride is in the pharmaceutical composition.

26. The method of claim 25, wherein the 60 mg of trospium chloride is equally divided between the enteric coated pellets and extended release pellets.
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