IMMEDIATE RELEASE DRUG FORMULATION COMBINING OPIOID AND NONOPIOID ANALGESICS WITH ABUSE DETERRENCE AND OVERDOSE PROTECTION

摘要

The present disclosure provides solid immediate release (IR) dosage forms, including particulate and multi-particulate dosage forms, with abuse deterrent and overdose protection characteristics. In certain embodiments, the dosage form is multi¬ particulate, comprising: a first population of particulates comprising a therapeutically effective amount of at least one opioid embedded in a polymer matrix, an optional seal coat, a functional coat layer(s), and an over coat, wherein the functional coat layer(s) comprises a nonionic water-insoluble polymer, and a cationic polymer that dissolves at a pH of less than about 5; a second population of particulates comprising a therapeutically effective amount of acetaminophen (APAP) embedded in a polymer matrix, an optional seal coat, a functional coat layer(s), and an over coat, wherein the functional coat layer(s) comprises a cationic polymer that dissolves at a pH of less than about 5 and an optional nonionic water-insoluble polymer; and a third population of particulates comprising an alkaline agent, and an optional pH-stabilizing agent, wherein the alkaline agent raises the gastric pH when three or more dosage units are ingested, and the pH-stabilizing agent maintains the elevated pH. The dosage forms, including particulate and multi-particulate dosage forms, are designed to accomplish the desired combination of analgesia, abuse deterrence, and overdose protection.