| 摘要 |
PURPOSE: To readily obtain a sustained release pharmaceutical preparation, capable of stationarily releasing a biologically active peptide having a luteinizing hormone releasing hormone antagonism, excellent in storage stability and suppressed in histamine-isolating action in high yield. CONSTITUTION: An inner water phase comprising a liquid containing a biologically active peptide of the formula (X is H or tetrahydrofurylcarboxamide; Q is H or methyl; A is nicotinoyl or N,N'-diethylamidino; B is isopropyl or N,N'- diethylamidino) or its salt is added to oil phase comprising a solution containing a biodegradable polymer having a free carboxyl at the ends and the water phase is emulsified to afford a W/O type emulsion. Then, the emulsion is added to an outer water phase to give a W/O/W type emulsion and a solvent in the oil phase is usually removed to provide the objective pharmaceutical preparation. A lactic acid-glycolic acid copolymer having (90/10) to (50/50) composition ratio (mol.%) of lactic acid/glycol and 8000-15000 weight-average molecular weight is preferably used as the biodegradable polymer. |
