| 摘要 |
Disclosed herein is a prodrug for use in the treatment of physiological conditions comprising a carrier moiety selected from the consisting essentially of cinnamoyl, benzoyl, phenylacetyl, 3,4-methylenedioxycinnamoyl and 3,4,5-trimethoxycinnamoyl, wherein the carrier moiety is chemically linked to a therapeutic pseudo-polypeptide of the formula aan, where aa is a chemically modified amino acid, or a chemical or structural variation thereof, where n is an integer from 2 to 40, and wherein the pseudo-polypeptide is poorly absorbed orally. In an alternative variation, the prodrug of the present invention further comprises a non-therapeutic linker species linking the pseudo-polypeptide to the carrier moiety. Preferably, the linker species is an amino acid. Thus, the prodrug of the present invention can be viewed as a three-component entity: the first, therapeutically active component is the pseudo-polypeptide; the second is the linker species, possibly an additional, non-therapeutic amino acid; and the third is the carrier moiety. Also disclosed are methods for the enhancement of the bioavailability of orally administered polypeptide substances.
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