Warner-lambert Company

Michael Ray Harris

Russell U Nesbitt

Gerard C Hokanson

Jay Weiss

Mahdi B Fawzi

Kuchi S Murthy

John E Botzolakis

Frank Waldman

Nouman A Muhammad

Robert G Reisch, Jr

Jane Ellen Daniel

Isaac Ghebre-Sellassie

Robert H Gordon

Henry A Miller, Jr

Nancy L Mills

Wayne Boisvert

Robert Reisch

Dirk Casier

Frank Goodhart

The present invention is directed to ACE inhibitor-containing compositions stabilized by the presence of magnesium oxide. Preferably, the ACE inhibitor, quinapril, is protected from certain forms of degradation when prepared in a pharmaceutical composition consisting essentially of magnesium oxide as the stabilizing agent. The presence of magnesium oxide also lends itself to favorable processing conditions during the manufacture of ACE inhibitor-containing compositions, especially processing by wet granulation.

Stabilization of quinapril using magnesium oxide

Semi-enteric controlled release formulations are comprised of a biological active agent such as an antibiotic that is blended with a water-soluble bulking agent, the mix then coated onto an inert core. The coated active core is further coated with a mixture comprised of an acrylic copolymer, bulking agent and pH dependent food acid. These different coating components possess different solubility characteristics which result in a gradual release of the active in both the stomach and small intestine that provides an increased bioavailability of the active drug.

Sustained release formulations

The present invention pertains to semi-enteric drug delivery systems which comprise (a) an inert core, (b) a first coating layer over the core comprising a medicament, and (c) a second coating layer over the first coating layer comprising a mixture of methacrylic acid copolymer, type C, and povidone present in a ratio by weight of from about 2:1 to about 24:1, respectively.

Semi-enteric drug delivery systems and methods for preparing same

A sustained release oral pharmaceutical composition consists essentially of a recompressed mixture of a water-sensitive pharmaceutical agent, a high molecular weight hydrophilic cellulose polymer, and a lubricant. The mixture is compressed into a unitary mass, comminuted, and recompressed into tablets without the use of solvents.

Sustained release pharmaceutical compositions

According to this invention various hygroscopic malflavored drugs can be proceeded by a unique wet granulation process wherein a slurry of the drug in water is dried in combination with colloidal silicon dioxide and, in a particularly preferred embodiment microcrystalline cellulose with the colloidal silicon dioxide absorbing onto the drug particles.

Drug in combination with flavor masking agent and method for making same

A dosing disc capsule machine has a tamping pin carried in a mounting block for extending into openings in a dosing disc to compact powder in the openings to form a plug. The plug is then transferred into a capsule body by an ejection pin. In accordance with the invention, a load cell is positioned above the tamping pin in the mounting block for measuring the compressive force exerted on the powder by the tamping pin. The load cell occupies the space normally occupied by the overload spring in such dosing disc capsule machines. Thus, modification of the tamping pin is not necessary, and the simple substitution of parts makes it possible to interchange the instrumentation from one machine to another. Further, the modifications are minor and do not affect the normal operation of the machine.

Instrumentation of a dosing-disc capsule machine

Tablet

The oxidation--and color-stability of certain ace inhibitors is optimized when they are formulated with a stabilizer and at least one lubricant and/or excipient.

Drug compositions stabilized against oxidation

Apparatus for measuring the hardness of capsule plugs, granules and pellets, in which a power stand (11) has a base (12) and gear motor (15) for driving a replaceable probe (25) toward a test subject supported on the base. A test subject holder (27) is placed on the base for holding the test subject, and comprises spaced apart first and second support plates (28, 30) fixed relative to one another with a third support plate (29) movable therebetween to define a space variable between zero and a predetermined maximum. Accordingly, a test subject may be held on the support for testing in a selected one of a variety of modes, including crushing, bending and cutting, depending on the spacing of the plates and the probe selected.

Apparatus for measuring capsule plug, granule and pellet hardness

The cyclization and hydrolysis of certain ACE inhibitors is minimized when they are formulated with a stabilizer and at least one lubricant and/or excipient.

Stabilized drug compositions

The cyclization, hydrolysis, and coloration of certain ACE inhibitors is minimized when they are formulated with a metal-containing stabilizer and a saccharide.

Stabilized compositions

The problems of tackiness and long curing times usually associated with the treatment of dosage forms are overcome via the use of a new curing process. That process involves: (1) coating a drug with a sustained release formulation, (2) immediately coating with a water-soluble overcoat, (3) drying, and (4) recovering the coated dosage form.

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Hackettstown, NJ, United States of America

Michael Ray Harris