American Cyanamid Company

Madurai G Ganesan

Nitin V Sheth

Narendra Raghunathji Desai

Joseph J Valorose, Jr

Keith A Ellway

Jerry B Johnson

Kieran G Mooney

Eugene A Carpentier

Edward C Shinal

Wendy Ann Preston

Daniel Joseph Doyon

Prakash S Kulkarni

Gary A Maier

Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures or separate administration units of pH sensitive polymer coated spherical granules adapted to release the minocycline in a medium having a pH of in the range of from about 4.0 to about 7.5 and coated or uncoated quick release granules adapted to release minocycline in a medium having a pH of less than about 3.9 or minocycline powder, pH adapted multi-coated compositions and oral dosage unit form liquids, capsules or tablets containing the above are provided. These systems and formulations provide at least minimum therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day. Methods for the preparation of the systems and formulations are provided as well.

Pulsatile once-a-day delivery systems for minocycline

A controlled release pharmaceutical composition in oral dosage unit form comprising a tablet comprising a therapeutically effective number of active spherical granules comprising an effective amount of active medicament, a pharmaceutically acceptable normally solid diluent adapted to form a diffusable matrix for the active medicament and an optional pharmaceutically acceptable excipient; and a number of compressible spherical granules comprising a mono- or di-saccharide, an optional pharmaceutically acceptable normally solid diluent adapted to form a diffusable matrix, an optional active medicament and/or an optional pharmaceutically acceptable excipient wherein the average compressive yield of the compressible spherical granules is less than the average compressive yield of the active spherical granules is provided. A method for the preparation and for the administration of the above defined composition is provided as well.

Controlled release pharmaceutical compositions from spherical granules

Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures of a minor proportion of slow-release blended polymer coated spherical granules adapted to release part of the minocycline in a medium having a pH of below 3.9 and the rest in the range of from about 4.0 to about 7.5 and a major proportion of coated or uncoated quick-release granules adapted to release minocycline in a medium having a pH of less than about 3.9 and oral dosage unit form capsules containing the above are provided. These systems and formulations provide enhanced therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day, regardless of whether the patient is fed or fasted. Methods for the preparation of the systems and formulations are provided as well.

Complex of 1,4-dihydropyridine with polyoxyethylene-polyoxypropylene copolymer useful in sustained release dosage formulations.

Sustained release delivery system for substituted dihydropyridine

Lipid emulsion form compositions have been formulated and presented to eliminate adverse injection site reactions associated with the intravenous administration of certain sparingly water soluble, hydrophobic, ionizable drugs in mammals and to provide a solubilized drug form for oral, parenteral or intraarticular administration which enhances drug absorption and the therapeutic efficacy of the drug.

Emulsion compositions for administration of sparingly water soluble

This disclosure describes quick breaking, in vivo, intravenous, intramuscular, intraarticular fat emulsion compositions which incorporate the use of benzyl alcohol as a consurfactant and/or a cosolvent in combination with materials such as synthetic surfactants, e.g. sorbitan triisostearate, triglycerol diisostearate or triglycerol pentaoleate; naturally occurring vegetable oils, e.g. sesame oil, and soybean oil; natural lecithins such as egg lecithin or soy lecithin; saturated or unsaturated aliphatic acids, e.g. oleic acid, hexanoic acid and linolenic acid; and other excipients such as glycerine, polyvinylpyrrolidone, Pluronic.RTM. F-68 and di-.alpha.-tocopherol.

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Suffern, NY, United States of America

Madurai G Ganesan