Pulse dosage formulations of methylphenidate and method to prepare same
OwnerGeorge Krsekinventor
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Abstract
Dosage forms comprising pulse release formulations for oral administration of a Methylphenidate drug are provided. The dosage forms provide a substantially immediate dose of methylphenidate upon ingestion, followed by one or more additional doses at predetermined times. By providing such a drug release profile, the dosage forms eliminate the need for a patient to carry an additional dose for ingestion during the day. The dosage forms and methods provided are useful in administering Methylphenidate and pharmaceutically acceptable salts thereof, which generally require one or more doses throughout the day.
Claims25
A dosage form for the oral administration of a methylphenidate drug, comprising a first pulse dosage and a second pulse dosage, wherein:
- said first pulse dosage comprises a first methylphenidate drug portion and a first sealing layer, wherein said first sealing layer is disposed over said first methylphenidate drug portion;
- and
- said second pulse dosage comprises a second methylphenidate drug portion, a second sealing layer disposed over said second methylphenidate drug portion, a polymeric coating layer disposed over said second sealing layer, and a third sealing layer disposed over said polymeric coating layer.
A method to form a pulse release formulation comprising a methylphenidate drug, comprising the steps of:
- providing said methylphenidate drug;
- forming a first mixture comprising said methylphenidate drug, a microcrystalline cellulose, and a polyol;
- adding water to said first mixture to form a second mixture, wherein said second mixture has a bulk viscosity greater than about 10,000 cps;
- extruding said second mixture to form plurality of cylindrically-shaped particles;
- spheronizing said plurality of cylindrically-shaped particles to form a plurality of spheroids;
- drying said spheroids to a moisture content of below about 2 weight percent;
- separating by size said dried spheroids;
- forming a first sealing composition comprising a first hydroxypropylalkylcellulose, a first polyether polyol, and talc;
- applying said first sealing composition to said dried spheroids to form first beads;
- drying said first beads;
- separating said first beads by size to form a first pulse release dosage;
- forming a polymeric coating composition comprising a cellulose acetate polymer and a dialkyl ester of dicarboxylic acid;
- encapsulating said first beads with said polymeric coating composition;
- forming a second sealing composition comprising a second hydroxypropylalkylcellulose and a second polyether polyol;
- applying said second sealing composition over said polymeric coating composition;
- drying said second sealing composition covered, polymeric composition encapsulated first beads to form second beads;
- separating by size said second beads to form second pulse dosage;
- providing a plurality of non-pareil beads;
- blending said first pulse dosage, said second pulse dosage, and said non-pareil beads to form a pulse release formation;
- and
- assaying said pulse release formulation for uniformity.
A method to form a pulse release formulation comprising a methylphenidate drug, comprising the steps of:
- providing said methylphenidate drug;
- forming a first mixture comprising said methylphenidate drug, a microcrystalline cellulose, and a polyol;
- adding water to said first mixture to form a second mixture, wherein said second mixture has a bulk viscosity greater than about 10,000 cps;
- extruding said second mixture to form a plurality of cylindrically-shaped particles;
- spheronizing said plurality of cylindrically-shaped particles to form a plurality of spheroids;
- drying said spheroids to a moisture content of below about 2 weight percent;
- separating by size said dried spheroids;
- forming a first sealing composition comprising a first hydroxypropylalkylcellulose, a first polyether polyol, and talc;
- applying said first sealing composition to said dried spheroids to form first beads;
- drying said first beads;
- separating said first beads by size to form a first pulse release dosage;
- forming a polymeric coating composition comprising a cellulose acetate polymer and a dialkyl ester of a dicarboxylic acid;
- coating said first beads with said polymeric coating composition;
- forming a second sealing composition comprising a second hydroxypropylalkylcellulose and a second polyether polyol;
- applying said second sealing composition over said polymeric composition encapsulated first beads;
- drying said second sealing composition covered, polymeric composition encapsulated first beads to form second beads;
- separating by size said second beads to form a second pulse dosage;
- combining said first pulse dosage, said second pulse dosage, a third polyether polyol, a carbohydrate, and fumed silica to form, a third mixture;
- adding microcrystalline cellulose to said third mixture to form a fourth mixture;
- and
- adding magnesium stearate to said fourth mixture to form said pulse release formation.
Dependencies are inferred from the claim text.