Pfizer Corporation

Michael C Roy

Kenneth C Waterman

Dwayne Thomas Friesen

William John Curatolo

Avinash G Thombre

Ronald Arthur Beyerinck

Mark B Chidlaw

Mary T Am Ende

Michael B Fergione

Scott W Smith

Sara Kristen Moses

Danni Supplee

Leah A Appel

The present invention is directed to controlled-release (CR) oral pharmaceutical dosage forms of 5,8,14-triazatetracyclo[10.3.1.00]-hexadeca-2(11),3,5,7,9-pentaene, 1, and pharmaceutically acceptable salts thereof, and methods of using them to reduce nicotine addiction or aiding in the cessation or lessening of tobacco use while reducing nausea as an adverse effect. The present invention also relates to an immediate-release (IR) low dosage composition having a stable formulation with uniform drug distribution and potency. 

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A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet. In another embodiment, the dosage form releases less than about 25 wt % of sertraline to the use environment by the second hour after introduction of the dosage form to the use environment, and delivers at least 25 wt % from the eighth to the twenty-fourth hour.

Hydrogel-driven layered drug dosage form

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Groton, CT, United States of America

Michael C Roy