The present invention provides a method to prepare drug-loaded emulsion which can decrease the degradation of drug during the preparation. The present method includes such steps as followings: First, prepare non-self emulsifying oil-in-water emulsion containing no drugs. Second, add therapeutic drug into the oil-in-water emulsion and make the drug across the membrane into the inner oil phase of the emulsion by adjusting the pH value. The present preparation process is simple, avoiding the use of organic solvents and applicable to mass production.本發明提供製備載藥乳劑的方法,可減少藥物在製備過程中的降解。該方法包括如下步驟:a.製備不含藥物組分的非自乳化O/W型空白乳劑;b.將治療有效量的藥物加入空白O/W型乳劑中,經由調節pH值,使藥物跨膜分佈到乳劑內相中製備載藥乳劑。本方法過程簡單,避免使用有機溶劑,適合大規模工業化生產。