Fatty Acid Acylated D-Amino Acids for Oral Peptide Delivery

摘要

The present invention relates to fatty acid acylated amino acids (FA-Daa's) acting as permeation enhancers for oral delivery of therapeutic macromolecules such as peptides and pharmaceutical compositions comprising such FA-Daa's.

主权项

1. A pharmaceutical composition comprising
a. At least one FA-Daa or a salt thereof represented by the general formula A-Xy, wherein A is a non-polar uncharged or acidic amino acid and Xy is a fatty acid moiety attached by acylation to A's alpha amino group and y represents the number of carbon atoms in said fatty acid moiety, wherein y is 10, 12, 14, 16 or 18 when said amino acid is a non-polar uncharged amino acid and y is 16 or 18 when said amino acid is an acidic, wherein the stereo configuration of the chiral carbon atom in the amino acid moiety is D and b. a hydrophilic peptide or protein.