Sustained-release leuprorelin preparation

摘要

A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3' is a heterocyclic group; R5 represents a group of the formula -(CH2)n-R5' wherein n is 2 or 3, and R5' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula -(CH2)n-R6' wherein n is 2 or 3, and R6' is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time without an initial burst.