.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 7,723,305

« Back to Dashboard

Claims for Patent: 7,723,305

Title:Abuse-resistant amphetamine prodrugs
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.
Inventor(s): Mickle; Travis (Coralville, IA), Krishnan; Suma (Belvedere, CA), Bishop; Barney (Annandale, VA), Lauderback; Christopher (Blacksburg, VA), Moncrief; James Scott (Christiansburg, VA), Oberlender; Robert (Blacksburg, VA), Piccariello; Thomas (Blacksburg, VA), Paul; Bernhard J. (Lexington, MA), Verbicky; Christopher A. (Broadalbin, NY)
Assignee: Shire LLC (Florence, KY)
Application Number:12/202,003
Patent Claims: 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 two properties selected from the group consisting of a mean AUC.sub.0-12 h (ng h/mL) from 205.4.+-.42.5 to 611.5.+-.104.5, a mean AUC.sub.last (ng h/mL) from 396.7.+-.84.8 to 1237.0.+-.194.0, a mean AUC.sub.inf (ng h/mL) from 415.0.+-.80.1 to 1259.5.+-.191.3, a mean C.sub.max (ng/mL) from 25.0.+-.5.6 to 74.0.+-.12.9, a mean T.sub.max (hours) from 3.1.+-.0.876 to 3.9.+-.1.0, and a mean T.sub.1/2 (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 two properties selected from the group consisting of a mean AUC.sub.0-12 h (ng h/mL) of 205.4.+-.42.5, a mean AUC.sub.last (ng h/mL) of 396.7.+-.84.8, a mean AUC.sub.inf (ng h/mL) of 415.0.+-.80.1, a mean C.sub.max (ng/mL) of 25.0.+-.5.6, a mean T.sub.max (hours) of 3.1.+-.0.876, and a mean T.sub.1/2 (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 10, 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 two properties selected from the group consisting of a mean AUC.sub.0-12 h (ng h/mL) of 611.5.+-.104.5, a mean AUC.sub.last (ng h/mL) of 1237.0.+-.194.0, a mean AUC.sub.inf (ng h/mL) of 1259.5.+-.191.3, a mean C.sub.max (ng/mL) of 74.0.+-.12.9, a mean T.sub.max (hours) of 3.9.+-.1.0, and a mean T.sub.1/2 (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 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 two properties selected from the group consisting of a mean AUC.sub.last (ng h/mL) from 11.32.+-.3.74 to 58.1.+-.30.2, a mean AUC.sub.inf (ng h/mL) from 13.5.+-.3.40 to 59.5.+-.29.9, a mean C.sub.max (ng/mL) from 11.56.+-.3.8 to 53.6.+-.34.1, a mean T.sub.max (hours) of 1.05.+-.0.16, and a mean T.sub.1/2 (hours) from 0.419.+-.0.077 to 0.534.+-.0.211 of intact L-lysine-d-amphetamine or a salt thereof when orally administered to a human subject.

23. A composition as defined in claim 22, wherein said L-lysine-d-amphetamine is in the form of a salt.

24. A composition as defined in claim 23, wherein said salt is a mesylate salt.

25. A composition as defined in claim 24, wherein said salt is a dimesylate salt.

26. A composition as defined in claim 23, wherein said salt is a hydrochloride salt.

27. A composition as defined in claim 22, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension.

28. A composition as defined in claim 27, 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.

29. 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 two properties selected from the group consisting of a mean AUC.sub.last (ng h/mL) of 11.32.+-.3.74, a mean AUC.sub.inf (ng h/mL) of 13.5.+-.3.40, a mean C.sub.max (ng/mL) of 11.56.+-.3.8, a mean T.sub.max (hours) of 1.05.+-.0.16, and a mean T.sub.1/2 (hours) of 0.419.+-.0.077 of intact L-lysine-d-amphetamine or a salt thereof when orally administered to a human subject.

30. A composition as defined in claim 29, wherein said L-lysine-d-amphetamine is in the form of a salt.

31. A composition as defined in claim 30, wherein said salt is a mesylate salt.

32. A composition as defined in claim 31, wherein said salt is a dimesylate salt.

33. A composition as defined in claim 30, wherein said salt is a hydrochloride salt.

34. A composition as defined in claim 29, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension.

35. A composition as defined in claim 34, 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.

36. 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 two properties selected from the group consisting of a mean AUC.sub.last (ng h/mL) of 58.1.+-.30.2, a mean AUC.sub.inf (ng h/mL) of 59.5.+-.29.9, a mean C.sub.max (ng/mL) of 53.6.+-.34.1, a mean T.sub.max (hours) of 1.05.+-.0.16, and a mean T.sub.1/2 (hours) of 0.534.+-.0.211 of intact L-lysine-d-amphetamine or a salt thereof when orally administered to a human subject.

37. A composition as defined in claim 36, wherein said L-lysine-d-amphetamine is in the form of a salt.

38. A composition as defined in claim 37, wherein said salt is a mesylate salt.

39. A composition as defined in claim 38, wherein said salt is a dimesylate salt.

40. A composition as defined in claim 37, wherein said salt is a hydrochloride salt.

41. A composition as defined in claim 36, wherein said composition is in a dosage form selected from the group consisting of a tablet, capsule, caplet, oral solution, and oral suspension.

42. A composition as defined in claim 41, 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.

43. 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, 15, 22, 29, and 36.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc