Immediate release tablet cores of insoluble drugs having sustained-release coating
First Claim
1. A sustained release tablet for oral administration, comprising an immediate release tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml, said tablet core containing a sufficient amount of said therapeutically active agent to render a therapeutic effect, anda film coating formed over said core, said film coating comprising a sufficient amount of a hydrophobic material selected from the group consisting of waxes, shellac, zein, fatty alcohols, hydrogenated vegetable oils, water insoluble celluloses, acrylic polymers and mixtures thereof to provide a sustained release of said therapeutically active agent sufficient to provide a duration of effect from about 8 to about 24 hours when said coated tablet is exposed to aqueous solutions.
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Accused Products
Abstract
A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.
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Citations
25 Claims
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1. A sustained release tablet for oral administration, comprising an immediate release tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml, said tablet core containing a sufficient amount of said therapeutically active agent to render a therapeutic effect, and
a film coating formed over said core, said film coating comprising a sufficient amount of a hydrophobic material selected from the group consisting of waxes, shellac, zein, fatty alcohols, hydrogenated vegetable oils, water insoluble celluloses, acrylic polymers and mixtures thereof to provide a sustained release of said therapeutically active agent sufficient to provide a duration of effect from about 8 to about 24 hours when said coated tablet is exposed to aqueous solutions.
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2. A method of treating, a patient with a dose of a pharmaceutical formulation containing an insoluble therapeutically active agent over an extended period of time, comprising
preparing an immediate release solid tablet core comprising a therapeutically active agent in an amount sufficient to render a therapeutic effect, the therapeutically active agent having a solubility of less than or equal to about 5 mg/ml: coating said tablet core with a hydrophobic material selected from the group consisting of waxes, shellac, zein, fatty alcohols, hydrogenated vegetable oils, water insoluble celluloses, acrylic polymers and mixtures thereof, such that said formulation reproducibly releases said insoluble therapeutically active agent at a dissolution rate between 12.5% and 42.5% (by wt) released after 4 hours and between 55% and 85% (by wt) after 6 hours when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37°
C., and provides a duration of effect from about 8 to about 44 hours.- View Dependent Claims (21)
- 8. A sustained release tablet for oral administration, comprising an immediate release tablet core including from about 300 mg to about 500 mg acetaminophen, and a therapeutically effective amount of an analgesic agent selected from the group consisting of hydromorphone, oxycodone, dihydrocodeine, codeine, dihydromorphine, morphine, buprenorphine, salts of any of the foregoing, and mixtures of any of the foregoing, said immediate release tablet core providing the dissolution of not less than 75% of the acetaminophen in 45 minutes when said tablet core is placed in 900 ml 0.1N hydrochloric acid, said tablet core being coated with a sufficient amount of a hydrophobic material selected from the group consisting of waxes, shellac, zein, fatty alcohols, hydrogenated vegetable oils, water insoluble celluloses, acrylic polymers and mixtures thereof such that said acetaminophen and said analgesic agent are released from the coated tablet over an extended period of time, and provide a duration of effect of from about 12 hours to about 24 hours.
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11. A sustained release tablet for oral administration, comprising an immediate release tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml, said tablet core containing a sufficient amount of said therapeutically active drug to render a therapeutic effect, said tablet core coated with a sustained release film coating comprising a hydrophobic material selected from the group consisting of waxes, shellac, zein, fatty alcohols, hydrogenated vegetable oils, water insoluble celluloses, acrylic polymers and mixtures thereof permitting a dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm in 900 ml aqueous buffer, pH between about 1.6 and about 7.2, at 37°
- C. between 12.5 and 42.5% (by wt) released after 1 hour, between 45 and 56% (by wt) released after 2 hours, between 45 and 75% (by wt) released after 4 hours and between 55 and 85% (by wt) released after 6 hours, and providing a duration of effect of from about 8 to about 24 hours.
- View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19, 20)
Specification