Abuse-resistant controlled-release opioid dosage form

Abstract

Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as an immediate release product as a single dose. The controlled release nature of the tablet prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.

Description

[0001] This application is a divisional of U.S. Ser. No. 10 / 143,111 filed on May 10, 2002 and claims benefit of priority to U.S. Provisional Application No. 60 / 290,439 filed on May 11, 2001.FIELD OF THE INVENTION [0002] The present invention relates to controlled-release analgesic pharmaceutical formulations. More specifically, the invention relates to abuse-deterring controlled-release analgesic tablets. BACKGROUND OF THE RELATED ART [0003] Opioid compounds have long been known both for their powerful analgesic properties, and for their strong potential for abuse. While highly effective at controlling pain, opioids can also be addictive. Abuse of opioids, particularly heroin, but also including morphine, codeine, oxycodone, hydromorphone, oxymorphone, and others, is a problem in modern society. Opioid addicts can obtain drugs from a variety of illicit sources. These street drugs are of questionable quality. Therefore, to potential abusers, prescription pharmaceutical opioids can be...

AI Technical Summary

Benefits of technology

The patent describes a type of opioid tablet that is resistant to abuse and has controlled release properties. The tablet contains a combination of an opioid antagonist and an opioid agonist. The antagonist is present in a controlled-release matrix and is released over time, while the agonist is released quickly in a single dose. This combination of antagonist and agonist helps to block the effects of the opioid and reduce the risk of abuse.

Problems solved by technology

Opioid compounds have long been known both for their powerful analgesic properties, and for their strong potential for abuse.

While highly effective at controlling pain, opioids can also be addictive.

Abuse of opioids, particularly heroin, but also including morphine, codeine, oxycodone, hydromorphone, oxymorphone, and others, is a problem in modern society.

These street drugs are of questionable quality.

To do so, the tablets are crushed and often dissolved.

Naloxone is highly effective when taken parenterally, but poorly effective when taken orally because of its metabolism in the liver and, thus, has a high oral:parenteral potency ratio.

Because antagonists such as naloxone are less effective when taken orally, they have not been used to deter oral abuse and have been limited to deterring parenteral or intranasal abuse.

Prior oral opioid dosage formulations contained relatively low doses of opioid and were not generally targets for oral abuse.

Their immediate release formulations release the opioid all at once, but with low amounts of opioid that would not be sufficient for oral abuse without putting several low dosage units together.

The antagonist is present and released in amounts, over time, that attenuate or reduce the side effects of the opioid agonist, yet in amounts insufficient to block the opioid effect.