Abuse-resistant amphetamine prodrugs
DC CAFCFirst Claim
1. A method, in a subject in need thereof, of providing an amphetamine in a steady-state serum release curve without spiking blood serum concentrations, said method comprising administering to said subject L-lysine-d-amphetamine or a salt thereof, whereby said L-lysine-d-amphetamine or a salt thereof maintains a steady-state serum release curve which provides therapeutically effective bioavailability of said amphetamine, but without spiking blood serum concentrations of said amphetamine when compared to the administration to said subject of the same amount of said amphetamine in the form of D-amphetamine.
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Abstract
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.
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Citations
64 Claims
- 1. A method, in a subject in need thereof, of providing an amphetamine in a steady-state serum release curve without spiking blood serum concentrations, said method comprising administering to said subject L-lysine-d-amphetamine or a salt thereof, whereby said L-lysine-d-amphetamine or a salt thereof maintains a steady-state serum release curve which provides therapeutically effective bioavailability of said amphetamine, but without spiking blood serum concentrations of said amphetamine when compared to the administration to said subject of the same amount of said amphetamine in the form of D-amphetamine.
- 17. A method, in a subject in need thereof, of providing an amphetamine in a steady-state serum release curve without increased blood serum concentrations, said method comprising administering to said subject L-lysine-d-amphetamine or a salt thereof, whereby said L-lysine-d-amphetamine or a salt thereof maintains a steady-state serum release curve which provides therapeutically effective bioavailability of said amphetamine, but without increased blood serum concentrations of said amphetamine when compared to the administration to said subject of the same amount of said amphetamine in the form of D-amphetamine.
- 33. A method, in a subject in need thereof, of providing an amphetamine in a steady-state serum release curve with reduced spiking blood serum concentrations, said method comprising administering to said subject L-lysine-d-amphetamine or a salt thereof, whereby said L-lysine-d-amphetamine or a salt thereof maintains a steady-state serum release curve which provides therapeutically effective bioavailability of said amphetamine, but reduces spiking blood serum concentrations of said amphetamine when compared to the administration to said subject of the same amount of said amphetamine in the form of D-amphetamine.
- 49. A method, in a subject in need thereof, of providing an amphetamine in a steady-state serum release curve with a reduced increased blood serum concentration, said method comprising administering to said subject L-lysine-d-amphetamine or a salt thereof, whereby said L-lysine-d-amphetamine or a salt thereof maintains a steady-state serum release curve which provides therapeutically effective bioavailability of said amphetamine, but with a reduced increased blood serum concentration of said amphetamine when compared to the administration to said subject of the same amount of said amphetamine in the form of D-amphetamine.
Specification