COMPOSITIONS AND METHODS FOR ENHANCED PHARMACOLOGICAL ACTIVITY THROUGH ORAL AND PARENTERAL ADMINISTRATION OF COMPOSITIONS COMPRISING POLYPEPTIDE DRUG SUBSTANCES AND OTHER POORLY ABSORBED ACTIVE INGREDIENTS

摘要

Disclosed herein are novel pharmaceutical agents and compositions, as well as novel methods, to enhance the absorption of j polypeptide drug substances that normally display little if any absorbability if administered orally. Also disclosed are novel compositions and methods to significantly enhance the bioavailability and pharmacological efficacy of polypeptide drug substances whether administered orally or parenterally. In preferred embodiments, the cerrier selected from a group comprising cinnamoyl, benzoyl, phenylacetyl, 3,4-methylenedioxycinnamoyl, 3,4,5-trimethoxycinnamoyl, t-butoxycarbonyl, benzyloxycarbonyl, pivaloyl, N-9-fluorenylmethoxycarbonyt, and fumaroyl. ISUBn/SUB another preferred embodiment a polypeptide moiety Xn, where n = 1 - 3,is added at one end of the polypeptide drug substance, and where a terminal amino acid of the polypeptide moiety is selected from the group consisting of Pro, Met and Arg, and a protecting moiety is added the opposite end of the polypeptide drug substance.