脂肪乳作为难溶性药物的载体受到广泛的关注。乌苯美司作为一种水难溶性药物,市场上没有可供注射用剂型。本文利用SolEmuls技术制备注射用乌苯美司脂肪乳,采用单因素设计优化处方,得到的乌苯美司脂肪乳高压灭菌前后均比较稳定。制备的乌苯美司脂肪乳平均粒径在200nm左右,zeta电位为-44mV,体外释放行为符合双相动力学方程:100-Q=75.27e~(0.369t)+15.94e~(-0.0324t),R_α=0.9863,R_β=0.9878。药代动力学实验表明乌苯美司脂肪乳和静注乌苯美司混悬液药代动力学参数只有t_(1/2)有显著性差异。实验结果表明,对于水难溶性药物乌苯美司来说,静脉注射用脂肪乳可以作为一种安全有效的给药方式。 Fat emulsion as a poorly soluble drug carrier has received widespread attention. Ubenimex, a water-insoluble drug, is not available on the market for injection. In this paper, the use of SolEmuls technology for the preparation of ubenimexe emulsion for injection, the use of single factor design and optimization of prescription, ubiquinone fat emulsion obtained before and after sterilization were relatively stable. The average particle size of ubenimex fat emulsion was about 200nm and the zeta potential was -44mV. The in vitro release behavior was in accordance with the biphasic kinetic equation: 100-Q = 75.27e ~ (0.369t) + 15.94e ~ (-0.0324t ), R α = 0.9863, R β = 0.9878. Pharmacokinetic experiments showed that the pharmacokinetic parameters of ubenimex fat emulsion and intravenous ubenimex suspension were only significantly different from t 1/2. The experimental results show that, for the water-insoluble drug ubenimex, intravenous fat emulsion can be used as a safe and effective mode of administration.