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US 7,842,309 B2Granted
Tamper-resistant oral opioid agonist formulations
AssigneePurdue Pharma L.P.
InventorsBenjamin Oshlack, Curtis Wright, J. David Haddox
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Abstract
Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.
Claims22
An opioid antagonist composition having a structure comprising
- an inert core,
- a first layer,
- a second layer, and
- a third layer, the first layer being between the inert core and under the second layer, the second layer being between the first layer and the third layer, wherein
- the opioid antagonist is in the first layer and is sequestered by (i) a first hydrophobic material and additional excipients in the second layer and (ii) a second hydrophobic material and additional excipients in the third layer, such that the amount of the antagonist released from the opioid antagonist composition at 2 hours is undetectable by High Performance Liquid Chromatography, based on the in-vitro dissolution of the intact opioid antagonist composition, and such that, upon inclusion into a solid oral dosage form containing an opioid agonist, an amount of the opioid antagonist released from the solid oral dosage form which has been orally administered intact is insufficient to produce an antagonistic effect of the opioid antagonist in a human patient, and an amount of the opioid antagonist released from the solid oral dosage which has been tampered with and administered orally, intranasally, parenterally or sublingually will substantially block an effect of the opioid agonist,
- the second or the third layer is insoluble in a gastrointestinal system of a human, and
- the opioid antagonist composition is free from an opioid agonist.
4 more elements
An opioid antagonist composition having a structure comprising
- an inert core,
- a first layer,
- a second layer, and
- a third layer, the first layer being between the inert core and the second layer, the second layer being between the first layer and the third layer, wherein
- the opioid antagonist is in the first layer, consists of naltrexone or a pharmaceutically acceptable salt thereof, and is sequestered by (i) a first hydrophobic material and additional excipients in the second layer and (ii) a second hydrophobic material and additional excipients in the third layer, such that the amount of the antagonist released from the opioid antagonist composition at 2 hours is undetectable by High Performance Liquid Chromatography, based on the in-vitro dissolution of the intact opioid antagonist composition, and such that, upon inclusion into a solid oral dosage form containing an opioid agonist, an amount of the opioid antagonist released from the solid oral dosage form which has been orally administered intact is insufficient to produce an antagonistic effect of the opioid antagonist in a human patient, and an amount of the opioid antagonist released from the solid oral dosage which has been tampered with and administered orally, intranasally, parenterally or sublingually will substantially block an effect of the opioid agonist,
- the second or the third layer is insoluble in a gastrointestinal system of a human, and
- the opioid antagonist composition is free from an opioid agonist.
4 more elements
Dependencies are inferred from the claim text.