Compounds and compositions for prevention of overdose of oxycodone
First Claim
Patent Images
1. A method of making an ingredient for an oral dosage form of an oxycodone composition comprising:
- covalently bonding at the 6′
position and the 14′
position of said oxycodone a single amino acid or an oligopeptide of 12 or fewer amino acids.
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Abstract
The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to an opioid such as oxycodone in a manner that substantially decreases the potential of the opioid to cause overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction.
112 Citations
87 Claims
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1. A method of making an ingredient for an oral dosage form of an oxycodone composition comprising:
covalently bonding at the 6′
position and the 14′
position of said oxycodone a single amino acid or an oligopeptide of 12 or fewer amino acids.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 12, 13, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
- 10. The method of 1, wherein each oligopeptide is Glu-Tyr-Val.
- 11. The method of 1, wherein each oligopeptide is Ile-Tyr-Val.
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30. A method for altering short term bioavailability of oxycodone in an oral dosage form composition comprising:
covalently bonding at the 6′
position and the 14′
position of said oxycodone a single amino acid or an oligopeptide of 12 or fewer amino acids such that the short term bioavailability of oxycodone is altered.- View Dependent Claims (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58)
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59. A method for treating pain comprising delivering an oral dosage form of oxycodone, wherein said oxycodone is covalently bound to a single amino acid or an oligopeptide of 12 or fewer amino acids at the 6′
- position and the 14′
position of said oxycodone. - View Dependent Claims (60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87)
- position and the 14′
Specification