PHARMACEUTICAL COMPOSITIONS FOR EXTENDED RELEASE OF OXYCODONE AND ACETAMINOPHEN RESULTING IN A QUICK ONSET AND PROLONGED PERIOD OF ANALGESIA

摘要

The present disclosure provides extended release pharmaceutical compositions comprising oxycodone and acetaminophen that produce a quick initial onset of analgesia, yet, maintain analgesia for about 12 hours after administration of the composition to a subject in need thereof. The pharmaceutical compositions disclosed herein also reduce the levels of acetaminophen in a subject's blood near the end of the dosing interval because the acetaminophen released by the pharmaceutical composition is being eliminated by a subject's body faster than it is being absorbed.

主权项

1. A pharmaceutical composition comprising:
at least one immediate release portion comprising oxycodone or a pharmaceutically acceptable salt of oxycodone, acetaminophen, or a combination thereof; at least one extended release portion comprising oxycodone or a pharmaceutically acceptable salt of oxycodone, acetaminophen, and an extended release component; wherein the total amount of acetaminophen in the composition is about 325 mg to about 650 mg, and the total amount of oxycodone or salt in the composition is about 7.5 mg to about 15 mg; wherein upon oral administration of the composition to a subject, the composition provides an AUC0-1h for acetaminophen of about 1.25 ng·h/mL/mg to about 3.25 ng·h/mL/mg; a mean AUC for acetaminophen of about 35.0 ng·hr/mL/mg to about 60.0 ng·hr/mL/mg; an AUC0-1h for oxycodone or salt of about 0.1 ng·h/mL/mg to about 0.45 ng·h/mL/mg; and a mean AUC for oxycodone or salt of about 9.0 ng·hr/mL/mg to about 18.5 ng·hr/mL/mg; and wherein the subject attains therapeutic blood levels of both the oxycodone and the acetaminophen within about one hour after administration of the composition and maintains analgesia for at least about 10 hours after administration of the composition.