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 pharmaceutical composition comprising: a. about 10 mg to about 250 mg of L-lysine-d-amphetamine or a pharmaceutically acceptable salt thereof; b. about 40% to about 90% by weight percent of microcrystalline cellulose; c. about 1% to about 10% by weight percent of cros
The invention claimed is: 1. A pharmaceutical composition comprising: a. about 10 mg to about 250 mg of L-lysine-d-amphetamine or a pharmaceutically acceptable salt thereof; b. about 40% to about 90% by weight percent of microcrystalline cellulose; c. about 1% to about 10% by weight percent of croscarmellose sodium; and d. less than about 5% by weight percent of magnesium stearate. 2. The pharmaceutical composition of claim 1, consisting essentially of: a. about 30 mg L-lysine-d-amphetamine dimesylate; b. about 151 mg microcrystalline cellulose; c. about 4.69 mg croscarmellose sodium; d. about 1.88 mg magnesium stearate. 3. The pharmaceutical composition of claim 1, consisting essentially of: a. about 50 mg L-lysine-d-amphetamine dimesylate; b. about 70 mg microcrystalline cellulose; c. about 3.12 mg croscarmellose sodium; d. about 1.88 mg magnesium stearate. 4. The pharmaceutical composition of claim 1, consisting essentially of: a. about 70 mg L-lysine-d-amphetamine dimesylate; b. about 98 mg microcrystalline cellulose; c. about 4.37 mg croscarmellose sodium; d. about 2.63 mg magnesium stearate. 5. The pharmaceutical composition of claim 1, wherein the Cmax of released amphetamine is within about 80% to about 120% of a value selected wherein said value is 53.2±9.62 ng/mL, 93.3±18.2 ng/mL, or 134±26.1 ng/mL. 6. The pharmaceutical composition of claim 1, wherein the Tmax of released amphetamine is within about 80% to about 120% of a value selected wherein said value is 3.41±1.09 hours 3.58±1.18 hours, or 3.46±1.34 hours. 7. The pharmaceutical composition of claim 1, wherein the area under the curve (AUC) of released amphetamine is within about 80% to about 120% of a value selected wherein said value is 845±117 ngh/mL 1510±242 ngh/mL, or 2157±383 ngh/mL. 8. The pharmaceutical composition of claim 1, 2, 3, or 4, wherein the oral bioavailability of amphetamine released from the prodrug following administration is at least about 60% of the area under the curve (AUC) of that following administration of an equivalent amount of unbound d-amphetamine. 9. The pharmaceutical composition of claim 1, 2, 3, or 4, wherein the oral bioavailability of amphetamine released from the prodrug following administration is at least about 95% of the area under the curve (AUC) of that following administration of an equivalent amount of unbound d-amphetamine. 10. The pharmaceutical composition of claim 1, 2, 3, or 4, wherein the parenteral bioavailability of amphetamine released from the prodrug following administration is less than about 50% of the area under the curve (AUC) of that following administration of an equivalent amount of unbound d-amphetamine. 11. The pharmaceutical composition of claim 1, 2, 3, or 4, wherein the parenteral bioavailability of amphetamine released from the prodrug following administration is less than about 1% of the area under the curve (AUC) of that following administration of an equivalent amount of unbound d-amphetamine.
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