ORALLY ADMINISTERED BIOLOGICALLY ACTIVE PEPTIDES AND PROTEINS.

摘要

An enterally effective, biologically active peptide or protein composition, comprising a sandwich complex comprising a hydrophobic core complex of a biologically active peptide or protein with an alkyl or alkenyl sulfate having 6-24 carbon atoms and 0-3 double bonds which form an electrostatic complex with a soft quaternary ammonium ion of the formula NR1R2R3R4 wherein R1 represents a C1-C12-alkyl group; R2 and R3 independently represent hydrogen or a C1-C12-alkyl group; and R4 represents hydrogen or a radical of the formula IMAGE where R5 is hydrogen, C1-C5 n-alkyl group and R6 is a linear alkyl or alkenyl group having 6-22 carbon atoms and 0-3 double bonds; or R1 and R2 together represent a divalent radical of the formula -CH2CH2CH2CH2-, -CH2CH2CH2CH2CH2-, -CH=CH-N=CH-, or -CH2CH2OCH2CH2- and R3 and R4 have the meanings previously defined; with the proviso that R1, R2 or R3 may optionally be substituted with a hydroxyl group or an alkoxyl group of the formula -OR4 where R4 is an alkyl group having 1-4 carbon atoms; that when R1 and R2 together represent a divalent radical, the radical may be substituted by methyl, hydroxyl, R1, or -OR4; and that when R2 is hydrogen, R1 is not methyl.