Transepithelial delivery of peptides with incretin hormone activities
First Claim
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1. A topical preparation for the treatment of diabetes comprising:
- a conjugate comprising a peptide with incretin hormone activity covalently attached to a transepithelial carrier; and
a skin contact base,wherein the conjugate has a concentration in the skin contact base from 0.001% to 70%,wherein the peptide with incretin hormone activity is SEQ ID NO;
6 or SEQ ID NO;
33 optionally having a cysteine amino acid residue attached to the N-terminus or the C-terminus of the peptide with incretin activity, or having a cysteine amino acid residue which replaces one of the serine amino acid residues in the peptide with incretin activity, andwherein the transepithelial carrier comprises SEQ ID NO;
32.
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Abstract
Compositions and methods are disclosed for the treatment of diabetes and related diseases using peptides with incretin hormone activity. Preferably, the peptide with incretin hormone activity is GLP-1, exendin or an analog of GLP-1 or exendin. The peptides with incretin hormone activity are administered transepithelially using a transepithelial carrier peptide. The transepithelial peptide contains sufficient amino, guanidine or amidino groups to stimulate transepithelial delivery. In some embodiments, the transepithelial carrier and the peptide with incretin hormone activity are embedded in a pressure sensitive adhesive layer of a plaster or patch.
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Citations
29 Claims
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1. A topical preparation for the treatment of diabetes comprising:
- a conjugate comprising a peptide with incretin hormone activity covalently attached to a transepithelial carrier; and
a skin contact base, wherein the conjugate has a concentration in the skin contact base from 0.001% to 70%, wherein the peptide with incretin hormone activity is SEQ ID NO;
6 or SEQ ID NO;
33 optionally having a cysteine amino acid residue attached to the N-terminus or the C-terminus of the peptide with incretin activity, or having a cysteine amino acid residue which replaces one of the serine amino acid residues in the peptide with incretin activity, andwherein the transepithelial carrier comprises SEQ ID NO;
32. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
- a conjugate comprising a peptide with incretin hormone activity covalently attached to a transepithelial carrier; and
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19. A topical preparation for the treatment of diabetes comprising:
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a peptide comprising SEQ ID NO;
45; anda skin contact base, wherein the peptide has a concentration in the skin contact base from 0.001% to 70%. - View Dependent Claims (20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
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Specification