The present invention relates to a pharmaceutical composition comprising at least one liposome, a trapping agent and a sedative drug with a high drug to lipid ratio and a high encapsulation efficiency. Also provided are the methods to sedate or treat pain in a subject in need thereof by administering the pharmaceutical composition disclosed herein.本發明關於一種具有高藥物脂質比及高包埋效率的藥物組合物,所述藥物組合物包含至少一微脂體、捕獲劑及鎮靜藥物。本發明亦提供藉由施予本文所揭露的藥物組合物給需要的個體以鎮靜或治療其疼痛的方法。