Gastric retentive extended release pharmaceutical compositions

摘要

The present disclosure provides extended release pharmaceutical compositions comprising an opioid and an additional active pharmaceutical ingredient, wherein the composition exhibits gastric retentive properties which are achieved by a combination of a physical property of the composition and release of the opioid, wherein upon administration to a subject, the composition has at least one pharmacokinetic parameter that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.

主权项

1. A pharmaceutical composition, comprising:
an immediate release portion comprising, by total weight of the immediate release portion, about 0.5% to about 2.5% of hydrocodone or a pharmaceutically acceptable salt of hydrocodone, and about 65% to about 85% of acetaminophen; and an extended release portion comprising, by total weight of the extended release portion, about 0.3% to about 1.0% of hydrocodone or a pharmaceutically acceptable salt of hydrocodone and about 15% to about 25% of acetaminophen; wherein the total amount of acetaminophen in the composition is about 200 mg to about 650 mg, and the total amount of hydrocodone or a pharmaceutically acceptable salt of hydrocodone in the composition is about 5 mg to about 15 mg; wherein when the composition is orally administered to a subject in need thereof the composition delivers the hydrocodone or the pharmaceutically acceptable salt thereof and the acetaminophen to the subject's upper gastrointestinal tract for at least about 4 hours to about 12 hours; and wherein either the hydrocodone or the acetaminophen produces a plasma profile characterized by at least one pharmacokinetic parameter selected from the group consisting of Cmax, C1 hr, C2 h, AUC, partial AUC, Tmax, and Tlag that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.