초록 ▼

The present invention decreases the potential for abuse of opioids, particularly hydrocodone, by covalent modification. The invention provides methods of delivering hydrocodone as conjugates that release the hydrocodone following oral administration while being resistant to abuse by circuitous route

The present invention decreases the potential for abuse of opioids, particularly hydrocodone, by covalent modification. The invention provides methods of delivering hydrocodone as conjugates that release the hydrocodone following oral administration while being resistant to abuse by circuitous routes such as intravenous ("shooting") injection and intranasal administration ("snorting"). Further, hydrocodone compositions of the invention are resistant to oral abuse as well, since release of the hydrocodone at suprapharmacological doses reaches saturation.

대표청구항 ▼

The invention claimed is: 1. A compound comprising hydrocodone, or a pharmaceutically acceptable salt thereof, covalently attached at the 6' position to the C-terminus of a peptide wherein said peptide is Glu-Glu-Phe-Phe-Ile [SEQ ID NO: 5], Glu-Glu-Phe-Phe-Phe [SEQ ID NO: 3], Asp-Asp-Ile, Tyr-Tyr-P

The invention claimed is: 1. A compound comprising hydrocodone, or a pharmaceutically acceptable salt thereof, covalently attached at the 6' position to the C-terminus of a peptide wherein said peptide is Glu-Glu-Phe-Phe-Ile [SEQ ID NO: 5], Glu-Glu-Phe-Phe-Phe [SEQ ID NO: 3], Asp-Asp-Ile, Tyr-Tyr-Phe-Phe-Ile [SEQ ID NO: 4], or Tyr-Tyr-Ile. 2. A compound comprising hydrocodone, or a pharmaceutically acceptable salt thereof, covalently attached at the 6' position to the C-terminus of Tyr-Tyr-Phe-Phe-Ile [SEQ ID NO: 4]. 3. A composition comprising hydrocodone, or a pharmaceutically acceptable salt thereof, covalently attached at the 6' position to the C-terminus of Tyr-Tyr-Phe-Phe-Ile [SEQ ID NO: 4] and at least one pharmaceutically acceptable excipient. 4. A composition consisting essentially of hydrocodone, or a pharmaceutically acceptable salt thereof, covalently attached at the 6' position to the C-terminus of Tyr-Tyr-Phe-Phe-Ile [SEQ ID NO: 4] and at least one pharmaceutically acceptable excipient. 5. The composition of claim 3 or 4 wherein said composition is in tablet, capsule, oral solution, or oral suspension dosage form. 6. A method of treating acute or chronic pain comprising administering to a patient the composition of claim 3 or 4. 7. A method of treating acute or chronic pain comprising administering to a patient the compound of claim 1 or 2. 8. The method of claim 7 wherein said compound is formulated into a tablet, a capsule, an oral solution, or an oral suspension. 9. The composition of claim 5 wherein said composition is in tablet or capsule dosage form. 10. The method of claim 8 wherein said compound is in tablet form. 11. The method of claim 8 wherein said compound is in capsule form.