American Cyanamid Company

Joseph J Valorose, Jr

Nitin V Sheth

Jerry B Johnson

Kieran G Mooney

Keith A Ellway

Madurai G Ganesan

Michael K Doelling

Raymond J Biehl

Walter A Strathy

MaduraiGurusamy Ganesan

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

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.

Pharmaceutical compositions comprising spherical granules including thereon or therein a 7- or 9-akylamino-6-deoxy-6-demethyltetracycline or an acid-addition salt thereof blended with at least one excipient are adapted to control the rate of drug release in the stomach and in the intenstine in order not to produce nausea or dizziness upon oral administration during antibacterial therapy.

Novel controlled release formulations of tetracycline compounds

Growing community of inventors

Montgomery, NY, United States of America

Joseph J Valorose, Jr