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Details for Patent: 8,211,464

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Details for Patent: 8,211,464

Title:Modified release preparations containing oxcarbazepine and derivatives thereof
Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
Inventor(s): Bhatt; Padmanabh P. (Rockville, MD), Kidane; Argaw (Montgomery Village, MD), Edwards; Kevin (Lovettsville, VA)
Assignee: Supernus Pharmaceuticals, Inc. (Rockville, MD)
Filing Date:Aug 10, 2011
Application Number:13/137,382
Claims:1. A method of treating seizures, comprising administering to a subject in need thereof a pharmaceutical formulation comprising multiple units, wherein each unit comprises a homogeneous mixture of (a) oxcarbazepine, (b) at least one agent that enhances solubility of oxcarbazepine, and (c) at least one release promoting agent, wherein said release promoting agent comprises a polymer having pH-dependent solubility, and wherein each unit has a release profile for the oxcarbazepine different from other units.

2. The method of claim 1, wherein said agent that enhances solubility of oxcarbazepine is selected from a group comprising surface active agents, complexing agents, cyclodextrins, pH modifying agents, and hydration promoting agents.

3. The method of claim 2, wherein the surface active agents are selected from a group comprising sodium docusate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene oxide (PEO) modified sorbitan monoesters, fatty acid sorbitan esters, and polyethylene oxide-polypropylene oxide-(poly(ethylene oxide)) block copolymers.

4. The method of claim 1, wherein at least one unit of the pharmaceutical formulation comprises a matrix forming polymer selected from a group comprising swellable polymers and gel-forming polymers.

5. The method of claim 4, wherein the matrix forming polymer is selected from the group consisting of cellulosic polymers, alginates, gums, cross-linked polyacrylic acids, carageenan; polyvinyl pyrrolidone; polyethylene oxides; and polyvinyl alcohol.

6. The method of claim 1, wherein the polymer having pH dependent solubility remains intact at pH values of below 4 and dissolves at pH values of more than 4.

7. The method of claim 6, wherein the polymer having pH dependent solubility dissolves at pH values of more than 5.

8. The method of claim 7, wherein the polymer having pH dependent solubility dissolves at pH values of more than 6.

9. The method of claim 1, wherein the polymer having pH dependent solubility comprises cellulose acetate phthalate, cellulose acetate succinate, methylcellulose phthalate, ethylhydroxycellulose phthalate, polyvinylacetate phthalate, polyvinylbutyrate acetate, vinyl acetate-maleic anhydride copolymer, styrene-maleic mono-ester copolymer, or methyl acrylate-methacrylic acid copolymers.

10. The method of claim 1, wherein the amount of the release promoting agent is from 10% to 90% by weight, and the amount of the solubilizing agent is therefore from 1% to 80% by weight of a dosage form.

11. The method of claim 10, wherein the pharmaceutical formulation comprises, by weight of the pharmaceutical formulation, 30% to 70% release promoting agent and 1% to 50% solubilizing agent.

12. The method of claim 1, which exhibits an initial immediate release of oxcarbazepine followed by a modified release of oxcarbazepine.

13. The method of claim 12, wherein said modified release comprises a delayed release, an extended release, or a combination of delayed and extended release, each release characterized by a different release rate profile.

14. The method of claim 1, which comprises multiple units having a modified release profile.

15. The method of claim 14, wherein said modified release profile is selected from a group comprising a delayed release profile, an extended release profile, and a combination of any number of delayed and extended release profiles, each characterized by a different release rate.

16. The method of claim 15, wherein said units are in the form of minipellets, granules, minitablets and layers.

17. The method of claim 1, wherein the formulation is administered to the subject once a day.

18. The method of claim 1, wherein the seizure is an epileptic seizure.

19. The method of claim 1, wherein the epileptic seizure is a partial seizure or a generalized tonic-clonic seizure.

20. The method of claim 1, wherein the patient is a child.

21. The method of claim 1, which exhibits reduced side-effects.

22. A method of treating seizures, comprising administering to a subject in need thereof a pharmaceutical formulation comprising multiple units, wherein each unit comprises a homogeneous mixture of (a) oxcarbazepine, (b) at least one agent that enhances solubility of oxcarbazepine, and (c) at least one release promoting agent, wherein said release promoting agent comprises a polymer having pH-dependent solubility, wherein each unit has a release profile for the oxcarbazepine different from other units, and wherein the amount of oxcarbazepine is effective to produce a steady state blood level of monohydroxy derivative of oxcarbazepine in the range of about 2 .mu.g/ml to about 10 .mu.g/ml.

23. The method of claim 22, wherein C.sub.max levels of monohydroxy derivative of oxcarbazepine (MHD) are in the range of about 6 .mu.g/ml to about 10 .mu.g/ml and C.sub.min levels of MHD are in the range of about 2 .mu.g/ml to about 5 .mu.g/ml.

24. The method of claim 22, wherein the formulation is administered to the subject once a day.

25. A method of treating seizures, comprising administering to a subject in need thereof a pharmaceutical formulation comprising multiple units, wherein each unit consists essentially of a matrix comprising a homogenous mixture of oxcarbazepine, at least one agent that enhances solubility of oxcarbazepine, and at least one release promoting agent, wherein said release promoting agent comprises a polymer having pH-dependent solubility and wherein each unit has a release profile for the oxcarbazepine different from other units.

26. The method of claim 25, wherein the formulation is administered to the subject once a day.
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