New abuse-resistant pharmaceutical composition for the treatment of opioid dependence

Abstract

There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and / or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency / addiction and / or pain.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of U.S. application Ser. No. 13 / 622,151 filed Sep. 18, 2012 which in turn is a utility application of U.S. provisional application Ser. No. 61 / 536,180 filed Sep. 19, 2011.[0002]This invention relates to new pharmaceutical compositions comprising opioids that are useful in the treatment of opioid / opiate dependency and / or pain, which compositions may be abuse-resistant, and may be administered transmucosally and, in particular, sublingually.[0003]Opioids are widely used in medicine as analgesics. Indeed, it is presently accepted that, in the palliation of more severe pain, no more effective therapeutic agents exist.[0004]Opioid agonist analgesics are used to treat moderate to severe, chronic cancer pain, often in combination with non-steroidal anti-inflammatory drugs (NSAIDs), as well as acute pain (e.g. during recovery from surgery and breakthrough pain). Further, their use is increasing in the management...

AI Technical Summary

Benefits of technology

The patent text describes a new pharmaceutical composition that combines the opioid antagonist naloxone with the opioid agonist buprenorphine. This combination is designed to improve the bioavailability of buprenorphine and reduce the risk of diversion and abuse. The composition is presented in a specific formulation that includes microparticles of buprenorphine and naloxone, as well as a disintegrant. The technical effect of this new formulation is to provide a more effective and safer treatment for opioid addiction.

Problems solved by technology

Indeed, it is presently accepted that, in the palliation of more severe pain, no more effective therapeutic agents exist.

A perennial problem with potent opioid agonists however is one of abuse by drug addicts.

Drug addiction is a worldwide problem of which opioid dependence, notably of heroin, is a major component.

Opioid dependence is a major health problem and long-term heroin use is connected to a substantially increased risk of premature death from drug overdoses, violence and suicide.

Furthermore, sharing of needles among addicts contribute to the spreading of potentially fatal blood infections such as HIV, and hepatitis C. In addition, opioid dependence often leads to difficulties with social relations, inability to manage a normal job and increased criminality to finance addiction, with severe implications for the opioid dependent person and his / her family.

With most commercially-available pharmaceutical formulations, this can be done relatively easily, which renders them unsafe or “abusable”.

Naloxone in particular has a poor bioavailability when administered transmucosally but is rendered fully bioavailable when administered by injection.

Nonetheless, when administered parenterally, naloxone's functional blockade of buprenorphine's action is also only partial and is short-lived in its nature.

Further, Suboxone has also been reported to have several other significant limitations.

Moreover, the taste is not well tolerated by all patients and the tablet has an unpleasant gritty mouthfeel.

A film-based product has recently been developed to counteract these problems, but the film formulation also does not dissolve particularly quickly.

Opioid agonist effects of buprenorphine are less than the maximal effects of other, “full” opioid agonists, such as morphine, and are limited by a “ceiling” effect.

It will be evident to the skilled person that “premature” hydration will dramatically decrease the performance of a tablet formulation in use and may result in premature dissolution of active ingredients.

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