.

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

Details for Patent: 7,169,752

« Back to Dashboard

Details for Patent: 7,169,752

Title:Compounds and compositions for prevention of overdose of oxycodone
Abstract: The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to an opioid such as oxycodone in a manner that substantially decreases the potential of the opioid to cause overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction.
Inventor(s): Mickle; Travis (Charlottesville, VA), Krishnan; Suma (Blacksburg, VA), Moncrief; James Scott (Christiansburg, VA), Lauderback; Christopher (Blacksburg, VA), Bera; Sanjib (Blacksburg, VA), Guenther; Sven (Blacksburg, VA), Hirschelman; Wendy (Blacksburg, VA)
Assignee: New River Pharmaceuticals Inc. (Radford, VA)
Filing Date:Sep 30, 2004
Application Number:10/955,006
Claims:1. A method of making an ingredient for an oral dosage form of an oxycodone composition comprising: covalently bonding at the 6' position and the 14' position of said oxycodone a single amino acid or an oligopeptide of 12 or fewer amino acids.

2. The method of claim 1 wherein the oligopeptide is a dipeptide.

3. The method of claim 1 wherein the oligopeptide is a tripeptide.

4. The method of claim 1 wherein the oligopeptide is a tetrapeptide.

5. The method of claim 1 wherein the oligopeptide is a pentapeptide.

6. The method of claim 1 wherein the oligopeptide is a hexapeptide.

7. The method of claim 1 wherein said oligopeptide consists essentially of naturally occurring amino acids.

8. The method of claim 1 wherein said oligopeptide consists of naturally occurring amino acids.

9. The method of claim 1, wherein each oligopeptide is Glu-Pro-Val.

10. The method of 1, wherein each oligopeptide is Glu-Tyr-Val.

11. The method of 1, wherein each oligopeptide is Ile-Tyr-Val.

12. The method of claims 1 wherein said oligopeptide is Phe-Phe-Lys-Phe-Phe [SEQ ID NO: 5]Tyr-Tyr-Lys-Tyr-Tyr [SEQ ID NO: 4], or Glu-Glu-Phe-Phe-Ile [SEQ ID NO: 1].

13. The method of claim 9, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

14. The method of claim 10, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

15. The method of claim 11, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

16. The method of claim 3, wherein the at least one tripeptide is Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Glu-Glu-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Leu, Glu-Pro-Val, Lys-Lys-Leu, Pro-Pro-Vat, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Leu-Val, Phe-Phe-Leu, or Tyr-Pro-Val.

17. The method of claim 3, wherein each tripeptide is one of Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Glu-Glu-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Leu, Glu-Pro-Val, Lys-Lys-Leu, Pro-Pro-Val, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Leu-Val, Phe-Phe-Leu, Tyr-Pro-Val.

18. The method of claim 1, wherein each oligopeptide is Glu-Asp-Val.

19. The method of claim 1, wherein each oligopeptide is Ser-Gly-Val.

20. The method of claim 16, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

21. The method of claim 17, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

22. The method of claim 18, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

23. The method of claim 19, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

24. The method of any of claims 1, 9, or 19, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.

25. The method of any of claims 1, 9, or 19, wherein the pharmacological activity of oxycodone is substantially decreased when the composition is used in a manner inconsistent with the manufacturer's instructions as compared to unbound oxycodone.

26. The method of any of claims 1, 9, or 19, wherein said oxycodone is released into a patient's bloodstream at levels that give rise to a reduced or delayed C.sub.max spike for oxycodone and provides a therapeutically effective bioavailability curve.

27. The method of any of claims 1, 9, or 19, wherein the bioavailability of the covalently modified oxycodone is diminished and delayed when delivered by routes other than oral administration as compared to unbound oxycodone.

28. The method of any of claims 1, 9, or 19, wherein the method provides a therapeutically effective bioavailability curve when delivered orally and in accordance with a manufacturer's instructions.

29. The method of any of claims 1, 9, or 19, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.

30. A method for altering short term bioavailability of oxycodone in an oral dosage form composition comprising: covalently bonding at the 6' position and the 14' position of said oxycodone a single amino acid or an oligopeptide of 12 or fewer amino acids such that the short term bioavailability of oxycodone is altered.

31. The method of claim 30, wherein the oligopeptide is a dipeptide.

32. The method of claim 30, wherein the oligopeptide is a tripeptide.

33. The method of claim 30, wherein the oligopeptide is a tetrapeptide.

34. The method of claim 30, wherein the oligopeptide is a pentapeptide.

35. The method of claim 30, wherein the oligopeptide is a hexapeptide.

36. The method of claim 30, wherein said oligopeptide consists essentially of naturally occurring amino acids.

37. The method of claim 30, wherein said oligopeptide consists of naturally occurring amino acids.

38. The method of claim 30, wherein each oligopeptide is Glu-Pro-Val.

39. The method of claim 30, wherein each oligopeptide is Glu-Tyr-Val.

40. The method of claim 30, wherein each oligopeptide is Ile-Tyr-Val.

41. The method of claims 30, wherein said oligopeptide is Phe-Phe-Lys-Phe-Phe [SEQ D NO: 5] Tyr-Tyr-Lys-Tyr-Tyr [SEQ ID NO: 4], or Glu-Glu-Phe-Phe-Ile [SEQ ID NO: 1].

42. The method of claim 38, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

43. The method of claim 39, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

44. The method of claim 40, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

45. The method of claim 32, wherein the at least one tripeptide is Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Glu-Glu-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Leu, Glu-Pro-Val, Lys-Lys-Leu, Pro-Pro-Val, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Leu-Val, Phe-Phe-Leu, or Tyr-Pro-Val.

46. The method of claim 32, wherein each tripeptide is one of Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Glu-Glu-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Leu, Glu-Pro-Val, Lys-Lys-Leu, Pro-Pro-Val, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Leu-Val, Phe-Phe-Leu, Tyr-Pro-Val.

47. The method of claim 30, wherein each oligopeptide is Glu-Asp-Val.

48. The method of claim 30, wherein each oligopeptide is Ser-Gly-Val.

49. The method of claim 45, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

50. The method of claim 46, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

51. The method of claim 47, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

52. The method of claim 48, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

53. The method of any of claims 30, 38, or 48, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.

54. The method of any of claims 30, 38, or 48, wherein the pharmacological activity of oxycodone is substantially decreased when the composition is used in a manner inconsistent with the manufacturer's instructions as compared to unbound oxycodone.

55. The method of any of claims 30, 38, or 48, wherein said oxycodone is released into a patient's bloodstream at levels that give rise to a reduced or delayed C.sub.max spike for oxycodone and provides a therapeutically effective bioavailability curve.

56. The method of any of claims 30, 38, or 48, wherein the bioavailability of the covalently modified oxycodone is diminished and delayed when delivered by routes other than oral administration as compared to unbound oxycodone.

57. The method of any of claims 30, 38, or 48, wherein the method provides a therapeutically effective bioavailability curve when delivered orally and in accordance with a manufacturer's instructions.

58. The method of any of claims 30, 38, or 48, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.

59. A method for treating pain comprising delivering an oral dosage form of oxycodone, wherein said oxycodone is covalently bound to a single amino acid or an oligopeptide of 12 or fewer amino acids at the 6' position and the 14' position of said oxycodone.

60. The method of claim 59, wherein the oligopeptide is a dipeptide.

61. The method of claim 59, wherein the oligopeptide is a tripeptide.

62. The method of claim 59, wherein the oligopeptide is a tetrapeptide.

63. The method of claim 59, wherein the oligopeptide is a pentapeptide.

64. The method of claim 59, wherein the oligopeptide is a hexapeptide.

65. The method of claim 59, wherein said oligopeptide consists essentially of naturally occurring amino acids.

66. The method of claim 59, wherein said oligopeptide consists of naturally occurring amino acids.

67. The method of claim 59, wherein each oligopeptide is Glu-Pro-Val.

68. The method of claim 59, wherein each oligopeptide is Glu-Tyr-Val.

69. The method of claim 59, wherein each oligopeptide is Ile-Tyr-Val.

70. The method of claims 59, wherein said oligopeptide is Phe-Phe-Lys-Phe-Phe [SEQ ID NO: 5] Tyr-Tyr-Lys-Tyr-Tyr [SEQ ID NO: 4], or Glu-Glu-Phe-Phe-Ile [SEQ ID NO: 1].

71. The method of claim 67, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

72. The method of claim 68, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

73. The method of claim 69, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

74. The method of claim 59, wherein the at least one tripeptide is Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Glu-Glu-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Leu, Glu-Pro-Val, Lys-Lys-Leu, Pro-Pro-Val, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Leu-Val, Phe-Phe-Leu, or Tyr-Pro-Val.

75. The method of claim 59, wherein each tripeptide is one of Asp-Asp-Ile, Gly-Tyr-Ile, Phe-Phe-Val, Tyr-Tyr-Ile, Asp-Asp-Val, Gly-Tyr-Leu, Phe-Val-Val, Tyr-Tyr-Phe, Glu-Asp-Val, Gly-Tyr-Val, Pro-Glu-Val, Tyr-Tyr-Val, Gln-Gln-Val, Ile-Tyr-Val, Pro-Pro-Ile, Val-Glu-Gly, Glu-Leu-Val, Leu-Tyr-Val, Pro-Pro-Len, Gln-Pro-Val, Lys-Lys-Leu, Pro-Pro-Val, Glu-Tyr-Val, Lys-Lys-Val, Ser-Gly-Val, Gly-Glu-Val, Lys-Ser-Val, Ser-Thr-Val, Gly-Gly-Ile, Phe-Phe-Ile, Thr-Thr-Val, Gly-Len-Val, Phe-Phe-Len, Tyr-Pro-Val.

76. The method of claim 59, wherein each oligopeptide is Glu-Asp-Val.

77. The method of claim 59, wherein each oligopeptide is Ser-Gly-Val.

78. The method of claim 74, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

79. The method of claim 75, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

80. The method of claim 76, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

81. The method of claim 77, wherein said oral dosage form is a tablet, a capsule, an oral solution, or an oral suspension.

82. The method of any of claims 59, 67, or 77, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.

83. The method of any of claims 59, 67, or 77, wherein the pharmacological activity of oxycodone is substantially decreased when the composition is used in a manner inconsistent with the manufacturer's instructions as compared to unbound oxycodone.

84. The method of any of claims 59, 67, or 77, wherein said oxycodone is released into a patient's bloodstream at levels that give rise to a reduced or delayed C.sub.max spike for oxycodone and provides a therapeutically effective bioavailability curve.

85. The method of any of claims 59, 67, or 77, wherein the bioavailability of the covalently modified oxycodone is diminished and delayed when delivered by routes other than oral administration as compared to unbound oxycodone.

86. The method of any of claims 59, 67, or 77, wherein the method provides a therapeutically effective bioavailability curve when delivered orally and in accordance with a manufacturer's instructions.

87. The method of any of claims 59, 67, or 77, wherein the method prevents spiking or increased blood serum concentrations when delivered at doses exceeding those within the therapeutic range of said oxycodone.
« Back to Dashboard

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

How are People Using DrugPatentWatch?

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