Protection against intentional and unintentional dose-dumping

Dose-dumping is the rapid release of the active ingredient from an extended release product into the blood stream. It can result in increased toxicity and side effects, as well as, in reduced efficacy due to the loss of the extended release PK profile.

Intentional dose-dumping or tampering occurs when people tamper with medications by crushing or chewing the tablets or dissolving them in alcohol or water. The drugs are then ingested orally, snorted or injected. OraGuard resists all of these tampering measures.

Unintentional dose-dumping or accidental dose-dumping can occur if a patient consumes alcohol while taking a medication. Although unintentional, the effect can be the same as with tampering. OraGuard also protects against accidental dose-dumping.

Effective and adaptable

OraGuard technology provides an extended release profile and protection against intentional and unintentional dose-dumping caused by the following:

  • Crushing and ingestion, injection or snorting
  • Chewing
  • Aqueous extraction for IV dosing
  • Alcohol extraction

The technology was evaluated in three phase 1 studies, and the manufacturing processes have been successfully scaled up to commercial equipment.

OraGuard technology uses compendial excipients and is adaptable to a wide variety of molecules. Dosing is up to 250 mg in tablet form with extended release profile.

CIMA OraGuard™ abuse-deterrent and alcohol-resistant technology

CIMA has developed a abuse-deterrent and alcohol-resistant extended release formulation platform that is applicable to opioids as well as other drugs. As the graphs demonstrate, the formulation design is focused on maximizing the following:

  • Resistance against mechanical crushing (a typical abuser’s approach for I.V. injection, snorting or oral ingestion)
  • Resistance against small volume extraction with aqueous or organic solvent
  • Protection against unintentional dose-dumping with alcohol

As part of product optimization, the developed prototypes are subjected to a battery of tests designed to simulate several extraction techniques used by abusers.

OxyContin and Palladone are registered trademarks of Purdue Pharma L.P.

Overview

Protection against intentional and unintentional dose-dumping

Dose-dumping is the rapid release of the active ingredient from an extended release product into the blood stream. It can result in increased toxicity and side effects, as well as, in reduced efficacy due to the loss of the extended release PK profile.

Intentional dose-dumping or tampering occurs when people tamper with medications by crushing or chewing the tablets or dissolving them in alcohol or water. The drugs are then ingested orally, snorted or injected. OraGuard resists all of these tampering measures.

Unintentional dose-dumping or accidental dose-dumping can occur if a patient consumes alcohol while taking a medication. Although unintentional, the effect can be the same as with tampering. OraGuard also protects against accidental dose-dumping.

Technical Notes

Effective and adaptable

OraGuard technology provides an extended release profile and protection against intentional and unintentional dose-dumping caused by the following:

  • Crushing and ingestion, injection or snorting
  • Chewing
  • Aqueous extraction for IV dosing
  • Alcohol extraction

The technology was evaluated in three phase 1 studies, and the manufacturing processes have been successfully scaled up to commercial equipment.

OraGuard technology uses compendial excipients and is adaptable to a wide variety of molecules. Dosing is up to 250 mg in tablet form with extended release profile.

Case Study

CIMA OraGuard™ abuse-deterrent and alcohol-resistant technology

CIMA has developed a abuse-deterrent and alcohol-resistant extended release formulation platform that is applicable to opioids as well as other drugs. As the graphs demonstrate, the formulation design is focused on maximizing the following:

  • Resistance against mechanical crushing (a typical abuser’s approach for I.V. injection, snorting or oral ingestion)
  • Resistance against small volume extraction with aqueous or organic solvent
  • Protection against unintentional dose-dumping with alcohol

As part of product optimization, the developed prototypes are subjected to a battery of tests designed to simulate several extraction techniques used by abusers.

OxyContin and Palladone are registered trademarks of Purdue Pharma L.P.