Modified release preparations containing oxcarbazepine and derivatives thereof

US 20090004263A1
Filed: 08/27/2008
Published: 01/01/2009
Est. Priority Date: 04/26/2006
Status: Active Grant

First Claim

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1. A pharmaceutical formulation for once-a-day administration of oxcarbazepine comprising an oxcarbazepine, at least one solubility enhancing agent and at least one release promoting agent.

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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.

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23 Claims

1. A pharmaceutical formulation for once-a-day administration of oxcarbazepine comprising an oxcarbazepine, at least one solubility enhancing agent and at least one release promoting agent.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23)
- - 2. The pharmaceutical formulation of claim 1 wherein said solubility enhancing agents are selected from a group comprising surface active agents, complexing agents, molecular entrapping agents, 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 said release promoting agents comprise pH-dependent polymers.
  - 5. The pharmaceutical formulation of claim 1, additionally comprising a matrix forming polymer selected from a group comprising swellable polymers and gel-forming polymers.
  - 6. The pharmaceutical formulation of claim 5 wherein said additional polymer is selected from a group comprising cellulosic polymers, alginates, gums, cross-linked polyacrylic acid derivatives, carageenan;
    - polyvinyl pyrrolidone and its derivatives;
      
      polyethylene oxides; and
      
      polyvinyl alcohol.
  - 7. The pharmaceutical formulation of claim 4, wherein a pH dependent polymer remains intact at pH values of below 4, and dissolves at pH values of more than 4.
  - 8. The pharmaceutical formulation of claim 7, wherein a pH dependent polymer dissolves at pH values of more than 5.
  - 9. The pharmaceutical formulation of claim 7, wherein a pH dependent polymer dissolves at pH values of more than 6.
  - 10. The pharmaceutical formulation of claim 4, wherein said pH dependent polymers are selected from a group comprising cellulose acetate phthalate, cellulose acetate succinate, methylcellulose phthalate, ethylhydroxycellulose phthalate, polyvinylacetate phthalate, polyvinylbutyrate acetate, vinyl acetate-maleic anhydride copolymer, styrene-maleic mono-ester copolymer, and methyl acrylate-methacrylic acid copolymers.
  - 11. The pharmaceutical formulation of claim 1, wherein the amount of the release promoting agent can be 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.
  - 12. The pharmaceutical formulation of claim 11, wherein the amount of the release promoting agent can be 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.
  - 13. The pharmaceutical formulation of claim 1, 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 μ
    - g/ml to about 10 μ
      
      g/ml.
  - 14. The pharmaceutical formulation of claim 13 effective in minimizing fluctuations between C_minand C_maxof monohydroxy derivative of oxcarbazepine.
  - 15. The pharmaceutical formulation of claim 14, wherein C_maxlevels of MHD are in the range of about 6 μ
    - g/ml to about 10 μ
      
      g/ml and C_minlevels of MHD is in the range of about 2 μ
      
      g/ml to about 5 μ
      
      g/ml.
  - 16. The pharmaceutical formulation of claim 1, which provides for variable rates of oxcarbazepine release in gastrointestinal tract.
  - 17. The pharmaceutical formulation of claim 16, which provides for a low rate of release of oxcarbazepine followed by an increased rate.
  - 18. The pharmaceutical formulation of claim 16, which provides for the initial immediate release mode of oxcarbazepine followed by a modified release mode.
  - 19. The pharmaceutical formulation of claim 18, wherein said modified release mode is selected from a group comprising a delayed release mode, an extended release mode, and a combination of any number of delayed and extended release modes, each characterized by a different release rate.
  - 20. The pharmaceutical formulation of claim 16, which combines multiple units with modified release modes in one dosage unit.
  - 21. The pharmaceutical formulation of claim 20, wherein said modified release modes are selected from a group comprising a delayed release mode, an extended release mode, and a combination of any number of delayed and extended release modes, each characterized by a different release rate.
  - 22. The pharmaceutical formulation of claim 21, wherein said units are in the form of (mini)pellets, (mini)granules, (mini)tablets and layers.
  - 23. The pharmaceutical formulation of claim 1 in the form of pellets, tablets, granules or capsules.

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Current Assignee
Supernus Pharmaceuticals Incorporated
Original Assignee
Supernus Pharmaceuticals Incorporated
Inventors
Kidane, Argaw, Edwards, Kevin, Bhatt, Padmanabh P.

Granted Patent

US 7,910,131 B2
Time in Patent Office

Days
Field of Search
US Class Current

424/457
CPC Class Codes

A61K 2800/56   Compounds, absorbed onto or...

A61K 31/55   having seven-membered rings...

A61K 9/0073   Sprays or powders for inhal...

A61K 9/2013   Organic compounds, e.g. pho...

A61K 9/2027   obtained by reactions only ...

A61K 9/2031   obtained otherwise than by ...

A61K 9/205   Polysaccharides, e.g. algin...

A61K 9/2054   Cellulose; Cellulose deriva...

A61P 25/08   Antiepileptics; Anticonvuls...

Modified release preparations containing oxcarbazepine and derivatives thereof

First Claim

2 Assignments

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Abstract

Citations

23 Claims

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Modified release preparations containing oxcarbazepine and derivatives thereof

First Claim

2 Assignments

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Accused Products

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Abstract

Citations

23 Claims

Specification

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Solutions

Use Cases

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