E. R. Squibb Sons, Inc.

Aprecia Pharmaceuticals LLC

Aprecia Pharmaceuticals Company

Tris Pharma, Inc.

Nemichand B Jain

Jules S Jacob

Thomas George West

Donald C Monkhouse

Norman Coyle

Henry Leon Surprenant

Yatindra M Joshi

Edward M Rudnic

Ajit B Thakur

Pierina Chiesa

Mark T DeCrosta

Andrea Nelson

Thomas M Wong

Robert L Jerzewski

George E Reier

Sachin Vasant Chaudhari

Yatinda M Joshi

Linda P Gertie

Robert Abramowitz

Lewis J Gryziewicz

Joseph D Drost

William R Bachman

Shivanand Puthli

Henry L Surprenant

A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of water soluble drug in a porous matrix that disperses in water within a period of less than about 15 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to the drug.

Rapid disperse dosage form

A 12-hour anti-tussive modified release solid tablet or tablet-in-capsule is described which comprises a benzonatate-silicon dioxide adsorbate powder in a hydrophilic matrix to provide a 12-hour modified release profile to the benzonatate, wherein there is substantially no benzonatate release from the tablet or capsule in the buccal cavity and no more than about 1% release of the benzonatate within half an hour as determined in an in vitro dissolution assay.

Benzonatate modified release solid tablets and capsules

A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water within a period of less than about 15 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to levetiracetam.

Rapid disperse dosage form containing levetiracetam

A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water within a period of less than about 10 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to levetiracetam.

A pharmaceutical composition is provided which has excellent stability, when dispersed in water has a pH of at least about 9, and includes a medicament which is sensitive to a low pH environment such as pravastatin, one or more fillers such as lactose and/or microcrystalline cellulose, one or more binders, such as microcrystalline cellulose (dry binder) or polyvinylpyrrolidone (wet binder), one or more disintegrating agents such as croscarmellose sodium, one or more lubricants such as magnesium stearate and one or more basifying agents such as magnesium oxide.

Pravastatin pharmaceuatical compositions having good stability

A formulation comprising captopril within an enteric or delayed release coated pH stable core combined with additional captopril that is available for immediate release following administration.

Captopril formulation providing increased duration of activity

A pharmaceutical compositions is provided which has excellent stability, when dispersed in water has a pH of at least about 9, and includes a medicament which is sensitive to a low pH environment such as pravastatin, one or more fillers such as lactose and/or microcrystalline cellulose, one or more binders, such as mirocrystalline cellulose (dry binder) or polyvinylpyrrolidone (wet binder), one or more disintegrating agents such as croscarmellose sodium, one or more lubricants such as magnesium stearate and one or more basifying agents such as magnesium oxide.

Pharmaceutical compositions having good stability

Shelf stable tablets containing fosinopril sodium are prepared by employing either sodium stearyl fumarate or hydrogenated vegetable oil as the lubricant. The tablets can contain conventional excipients such as fillers, binders, and disintegrants as well as an optional diuretic.

Fosinopril tablet formulations

A pharmaceutical composition is provided which is in the form of a plurality of beadlets, adapted to be filled into pharmaceutical hard shell capsules, or compressed into tablets, which beadlets are formed of a pharmaceutical such as an ACE inhibitor, for example, captopril, a beta-blocker such as nadolol, propranolol or atenolol, a calcium channel blocker such as diltiazem or nifedipine or other pharmaceuticals including combinations thereof, binder such as microcrystalline cellulose, and at least 5% by weight of an acid processing aid, such as citric acid, which imparts plasticity to the wet mass needed for efficient extrusion and spheronization. A method for forming beadlets is also provided which includes the steps of extruding a composition as described above, and subjecting the resulting extrudate to a spheronization step wherein an acid processing aid such as citric acid is employed to improve processing and form improved beadlets.

Pharmaceutical compositions in the form of beadlets and method

A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more primary hydrocolloid gelling agents which is a hydropropylmethyl cellulose having a viscosity of within the range of from about 1,000 to about 6,000 centipoises in 2% solution at 20.degree. C., and a methoxyl content of 28-30%, optionally a secondary hydrocarbon gelling agent, such as hydroxypropyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a pharmaceutical coating composition containing a hydrophobic polymer and a hydrophilic polymer.

Controlled release formulation

In accordance with the present invention, a controlled release formulation is provided from which a drug, selected from the group consisting of angiotensin converting enzyme inhibitors and ascorbic acid, is released at a substantially controlled rate. The controlled release formulation of the invention is comprised of a reactive matrix of from about 5 to about 80 percent by weight of the drug in combination with from about 5 to about 70 percent by weight of poly[(1.fwdarw.4)-2-amino-2-deoxy-.beta.-D-glucose] (also referred to as chitosan herein). Further in accordance with the present invention there is provided a gel-like complex formed of the drug and the chitosan in environments ranging from neutral to acidic.

Controlled release formulation and method

A controlled release pharmaceutical formulation which undergoes slow release of active drug is provided, preferably in the form of a tablet containing medicament, such as captopril, is slowly released over a controlled length of time. The tablet also includes an acrylic acid polymer or copolymer and one or more lubricants and is formed by a dry granulation technique.

A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 10,000 to about 200,000 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a pharmaceutical coating composition containing a hydrophobic polymer and a hydrophilic polymer.

A drug delivery system is provided which is in the form of hydrogel beads employed in a new interpenetrating polymer network which is formed by swelling hydrogel beads with an acrylic swelling agent and reacting the swelling agent with a cross-linking agent. The drug delivery system has superior drug loading capacity and controlled release characteristics.

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Monmouth Junction, NJ, United States of America

Nemichand B Jain