MODIFIED RELEASE FORMULATION AND METHODS OF USE
First Claim
1. A modified release pharmaceutical formulation, comprising:
- about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof;
about 5-30% of a drug delivery matrix comprising hydroxypropylmethylcellulose (HPMC),about 1.0-10% of an anionic surfactant andan enteric polymer,said pharmaceutical formulation producing a sustained plasma concentration of said retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of said retigabine.
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Accused Products
Abstract
A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant, and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. A formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours. A method of treating a disorder characterized by nervous system hyperexcitability includes administering to a subject an effective amount of these pharmaceutical formulations.
40 Citations
26 Claims
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1. A modified release pharmaceutical formulation, comprising:
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about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof; about 5-30% of a drug delivery matrix comprising hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant and an enteric polymer, said pharmaceutical formulation producing a sustained plasma concentration of said retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of said retigabine. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 22, 23, 24, 25, 26)
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17. A formulation comprising about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl) carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof;
- about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment, wherein the plasma concentration vs. time profile is substantially flat over an extended period lasting for about 4 hours to about 36 hours.
- View Dependent Claims (18, 19, 20, 21)
Specification