This invention provides an injectable formulation to be administered intramuscularly or subcutaneously that is used for the prevention or treatment of polycystic kidney disease, and that can maintain a therapeutically effective blood concentration of tolvaptan for a long period of time; and a process for producing the same. More specifically, this invention relates to an injectable depot formulation comprising (1) a particle containing optically active tolvaptan as an active ingredient and (2) a pharmaceutically acceptable carrier for injection, and a process for producing the same.本發明係提供一種以肌肉或皮下給藥之可注射的配方,其用於多囊性腎病之預防或治療,及其可長時間維持托伐普坦(tolvaptan)之治療有效之血中濃度;以及其製造方法。更具體地,本發明係有關一種包含(1)作為活性成分之含有光學活性托伐普坦之顆粒,及(2)用於注射之藥學上可接受載劑之可注射的補給配方,以及其製造方法。