Active agent delivery systems and methods for protecting and administering active agents

• US 20070232529A1
• Filed: 08/23/2004
• Published: 10/04/2007
• Est. Priority Date: 08/22/2000
• Status: Active Grant

• Current Assignee: Takeda Pharmaceutical Company Limited
• Original Assignee: New River Pharmaceuticals Inc. (Shire plc)
• Inventors: Piccariello, Thomas, Krishnan, Suma, Mickle, Travis, Lauderback, Christopher, Kirk, Randal, Moncrief, James
• Granted Patent: US 7,427,600 B2
• Time in Patent Office: Days
• US Class Current: 514/190
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 47/55 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• CPC Class Codes: A61K 47/62 the modifying agent being a protein, peptide or polyamino acid
• CPC Class Codes: A61K 47/64 Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent peptidic linkers A61K47/65

Abstract

The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

Claims

1-56. -56. (canceled)

57. A composition comprising:

an anti-inflammatory agent covalently attached to a carrier peptide wherein said carrier peptide comprises fewer than 50 amino acids; and

wherein said composition is in oral dosage form.

58. The composition of claim 57, wherein the anti-inflammatory agent is misoprostol, fluticasone, azathioprine, cyclosporine, acetaminophen, allopurinal, betamethasone, cefoxitin, celecoxib, diclofenac, etodolac, etoposide, ibuprofen, ketorolac, mesalamine, methylprednisolone, nabumetone, naproxen, oxaprozin, prednisone, rofecoxib, acetylsalicylic acid, tepoxalin, or valdecoxib.

59. The composition of claim 58, wherein said carrier peptide is a single amino acid.

60. The composition of claim 58, wherein said carrier peptide comprises dipetide.

61. The composition of claim 60, wherein said dipeptide further comprises at least one of glutamine, glutamic acid, aspartic acid, serine, lysine, cysteine, threonine, tyrosine, asparagine, or arginine.

62. The composition of claim 58, wherein said carrier peptide is a tripeptide.

63. The composition of claim 62, wherein said tripeptide further comprises at least one of glutamine, aspartic acid, glutamic acid, serine, lysine, cysteine, threonine, tyrosine, asparagine, or arginine.

64. The composition of claim 58, wherein said carrier peptide has a length between four and eight amino acids.

65. The composition of claim 58, wherein said carrier peptide has a length between four and 15 amino acids.

66. The composition of claim 58, wherein said carrier peptide has a length between nine and 50 amino acids.

67. The composition of claim 58, wherein said carrier peptide is -Ser-Ser, -PolySer, -Lys, -Glu-Glu, Asp-Asp, Asp-Asp-Asp, Asp-Asp-Glu, Asp-Asp-Ser, Asp-Asp-Lys, Asp-Asp-Cys, Ala-Glu, Ala-Ser, Ala-Asp, Ala-Asn, Ala-Thr, Ala-Arg, Ala-Cys, Ala-Gln, Ala-Tyr, LeuGlu, Leu-Ser, Leu-Asp, Leu-Asn, Leu-Thr, Leu-Arg, Leu-Cys, Leu-Gln, Leu-Tyr, PheGlu, Phe-Ser, Phe-Asp, Phe-Asn, Phe-Thr, Phe-Arg, Phe-Cys, Phe-Gln, Phe-Tyr, Val-Glu, Val-Ser, Val-Asp, Val-Asn, Val-Thr, Val-Arg, Val-Cys, Val-Gln, or Val-Tyr.

68. The composition of claim 58, wherein said carrier peptide is a homopolymer of naturally occurring amino acids or a heteropolymer of naturally occurring amino acids.

69. The composition of claim 58, wherein said carrier peptide is a homopolymer of naturally occurring amino acids.

70. The composition of claim 58, wherein said carrier peptide is a homopolymer of synthetic amino acids.

71. The composition of claim 58, wherein said carrier peptide is a heteropolymer of naturally occurring amino acids.

72. The composition of claim 58, wherein said carrier peptide is a heteropolymer of synthetic amino acids.

73. The composition of claim 58, wherein said carrier peptide is a heteropolymer comprising one or more naturally occurring amino acids and one or more synthetic amino acids.

76. A method of treating a disease or disorder comprising administering the composition of claim 58.

74. A composition comprising:

a carrier peptide with a length between three and nine amino acids; and

an anti-inflammatory agent covalently bound to said carrier peptide.

75. A composition comprising a carrier peptide that comprises an anti-inflammatory agent covalently attached to said carrier peptide;

wherein said carrier peptide is a single amino acid with the proviso that the amino acid is not alanine, glutamine, tyrosine, or methionine.