The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular u
The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
대표청구항▼
The invention claimed is: 1. A composition comprising from 25 to 75 mg of L-lysine-d-amphetamine or a salt thereof and having an amphetamine base amount of from 7.37 to 22.1 mg of said amphetamine, said L-lysine-d-amphetamine or a salt thereof providing at least five properties selected from the gr
The invention claimed is: 1. A composition comprising from 25 to 75 mg of L-lysine-d-amphetamine or a salt thereof and having an amphetamine base amount of from 7.37 to 22.1 mg of said amphetamine, said L-lysine-d-amphetamine or a salt thereof providing at least five properties selected from the group consisting of a mean AUC0-12 h (ng h/mL) from 205.4±42.5 to 611.5±104.5, a mean AUClast (ng h/mL) from 396.7±84.8 to 1237.0±194.0, a mean AUCinf (ng h/mL) from 415.0±80.1 to 1259.5±191.3, a mean Cmax (ng/mL) from 25.0±5.6 to 74.0±12.9, a mean Tmax (hours) from 3.1±0.876 to 3.9±1.0, and a mean T1/2 (hours) from 9.68±1.43 to 10.3±1.7 of amphetamine when orally administered to a human subject. 2. A composition as defined in claim 1, wherein said L-lysine-d-amphetamine is in the form of a salt. 3. A composition as defined in claim 2, wherein said salt is a mesylate salt. 4. A composition as defined in claim 3, wherein said salt is a dimesylate salt. 5. A composition as defined in claim 2, wherein said salt is a hydrochloride salt. 6. A composition as defined in claim 1, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension. 7. A composition as defined in claim 6, wherein said dosage form further comprises a pharmacological substance selected from the group consisting of amphetamines, antidepressants, anxiolytics, non-steroidal anti-inflammatory drugs, or any combination of any of the foregoing. 8. A composition comprising 25 mg of L-lysine-d-amphetamine or a salt thereof and having an amphetamine base amount of 7.37 mg of said amphetamine, said L-lysine-d-amphetamine or a salt thereof providing at least five properties selected from the group consisting of a mean AUC0-12 h (ng h/mL) of 205.4±42.5, a mean AUClast (ng h/mL) of 396.7±84.8, a mean AUCinf (ng h/mL) of 415.0±80.1, a mean Cmax (ng/mL) of 25.0±5.6, a mean Tmax (hours) of 3.1±0.876, and a mean T1/2 (hours) of 9.68±1.43 of amphetamine when orally administered to a human subject. 9. A composition as defined in claim 8, wherein said L-lysine-d-amphetamine is in the form of a salt. 10. A composition as defined in claim 9, wherein said salt is a mesylate salt. 11. A composition as defined in claim 10, wherein said salt is a dimesylate salt. 12. A composition as defined in claim 9, wherein said salt is a hydrochloride salt. 13. A composition as defined in claim 8, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension. 14. A composition as defined in claim 13, wherein said dosage form further comprises a pharmacological substance selected from the group consisting of amphetamines, antidepressants, anxiolytics, Non-steroidal anti-inflammatory drugs, or any combination of any of the foregoing. 15. A composition comprising 75 mg of L-lysine-d-amphetamine or a salt thereof and having an amphetamine base amount of 22.1 mg of said amphetamine, said L-lysine-d-amphetamine or a salt thereof providing at least five properties selected from the group consisting of a mean AUC0-12 h (ng h/mL) of 611.5±104.5, a mean AUClast (ng h/mL) of 1237.0±194.0, a mean AUCinf (ng h/mL) of 1259.5±191.3, a mean Cmax (ng/mL) of 74.0±12.9, a mean Tmax (hours) of 3.9±1.0, and a mean T1/2 (hours) of 10.3±1.7 of amphetamine when orally administered to a human subject. 16. A composition as defined in claim 15, wherein said L-lysine-d-amphetamine is in the form of a salt. 17. A composition as defined in claim 16, wherein said salt is a mesylate salt. 18. A composition as defined in claim 17, wherein said salt is a dimesylate salt. 19. A composition as defined in claim 16, wherein said salt is a hydrochloride salt. 20. A composition as defined in claim 15, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension. 21. A composition as defined in claim 20, wherein said dosage form further comprises a pharmacological substance selected from the group consisting of amphetamines, antidepressants, anxiolytics, non-steroidal anti-inflammatory drugs, or any combination of any of the foregoing. 22. A method, in a subject in need thereof, of treating attention deficit hyperactivity disorder, said method comprising administering to said subject a composition as defined in any of claims 1, 8, and 15.
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