The disclosure provides a pharmaceutical composition of KOR receptor agonist. Specifically, the disclosure provides the pharmaceutical composition of KOR receptor agonist contains 4-amino-N-[N2-[N-[N-[N-((R)-2-phenylpropyl)glycyl]-D-phenylalanyl]-D-leucyl]-D-lysyl]piperidine-4-carboxylic acid or its pharmaceutical salts and acetate buffers. The pharmaceutical composition of the disclosure shows good stability after several months of storage.本披露涉及一種KOR受體激動劑醫藥組成物。具體而言,本披露涉及的KOR受體激動劑醫藥組成物其包含4-胺基-N-[N2-[N-[N-[N-((R)-2-苯基丙基)甘胺醯基]-D-苯丙胺醯基]-D-亮胺醯基]-D-賴胺醯基]哌啶-4-羧酸或其可藥用鹽,和醋酸鹽緩衝液。本披露之醫藥組成物在儲存數月之後展現了良好的穩定性。