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Details for Patent: 8,017,149

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Details for Patent: 8,017,149

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 27, 2008
Application Number:12/230,275
Claims:1. A pharmaceutical formulation for once-a-day administration of oxcarbazepine 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 pharmaceutical formulation 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 pharmaceutical formulation of claim 2 wherein said 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 pharmaceutical formulation of claim 1, wherein at least one unit comprises a matrix forming polymer selected from a group comprising swellable polymers and gel-forming polymers.

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

6. The pharmaceutical formulation of claim 1, 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 pharmaceutical formulation of claim 6, wherein the polymer having pH dependent solubility dissolves at pH values of more than 5.

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

9. The pharmaceutical formulation 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 pharmaceutical formulation 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 can be from 1% to 80% by weight of a dosage form.

11. The pharmaceutical formulation of claim 10, wherein the amount of the release promoting agent is from 30% to 70% by weight, and the amount of the solubilizing agent can be from 1% to 50% by weight of the dosage form.

12. A pharmaceutical formulation for once-a-day administration of oxcarbazepine 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.

13. The pharmaceutical formulation of claim 12, 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.

14. The pharmaceutical formulation of claim 1, which exhibits for an initial immediate release of oxcarbazepine followed by a modified release of oxcarbazepine.

15. The pharmaceutical formulation of claim 14, 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.

16. The pharmaceutical formulation of claim 1, which comprises multiple units having a modified release profile.

17. The pharmaceutical formulation of claim 16, 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.

18. The pharmaceutical formulation of claim 17, wherein said units are in the form of minipellets, minigranules, minitablets and layers.

19. The pharmaceutical formulation of claim 1 in the form of pellets, tablets, granules or capsules.

20. The formulation of claim 1, wherein at least one unit comprises a release modifying coating.

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

22. A pharmaceutical formulation for once-a-day administration of oxcarbazepine 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.
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