02-10-2014 дата публикации
Номер: US20140296276A1
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, such that the ratio of the mean Cmax of the antagonist after single dose oral administration of the dosage form after tampering to the mean Cmax of antagonist after single dose oral administration of an intact dosage form is at least 1.5:1. 1159-. (canceled)160. An oral dosage form consisting ofan opioid agonist selected from the group consisting of morphine, hydromorphone, hydrocodone, oxycodone, codeine, meperidine, methadone, oxymorphone, and pharmaceutically acceptable salts thereof,an opioid antagonist selected from the group consisting of naltrexone, naloxone and pharmaceutically acceptable salts thereof,one or more hydrophobic materials, andadditional pharmaceutically acceptable excipients, whereinall of the opioid antagonist in the dosage form is sequestered with the one or more hydrophobic materials such that the ratio of the mean Cmax of the opioid antagonist after single dose oral administration of the dosage form after tampering by means of crushing, shearing, grinding, chewing, dissolution in a solvent, heating or any combination thereof to the mean Cmax of the opioid antagonist after single dose oral administration of the dosage form intact is at least 1.5:1.161. The dosage form of claim 160 , wherein said ratio is at least 3:1.162. The dosage form of claim 160 , wherein said ratio is at least 4.5:1.163. The dosage form of claim 160 , wherein said ratio is at least 4.5:1.164. The dosage form of claim 160 , wherein said ratio is at least 8:1.165. The dosage form of claim 164 , wherein said ratio is at least 10:1.166. The dosage form of claim 160 , wherein the opioid agonist is selected from the group consisting of morphine claim 160 , hydromorphone claim 160 , hydrocodone claim 160 , oxycodone claim 160 , oxymorphone claim 160 , pharmaceutically ...
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