硫酸头孢喹肟脂质体的制备工艺

Preparation of Cefquinome Sulfate Liposome

采用固体分散技术结合泡腾技术制备硫酸头孢喹肟脂质体,考察了减压旋转蒸发温度、氯仿用量、大豆卵磷脂/胆固醇质量比、吐温-80用量、药/脂质量比、柠檬酸与NaHCO3用量对脂质体外观形态和包封率的影响.通过正交实验优化制备条件,并探讨了脂质体的形成机制.结果表明,制备硫酸头孢喹肟脂质体的优化条件为:大豆卵磷脂/胆固醇/吐温-80/柠檬酸/NaHCO3的质量比为37:18:5:33:7,药/脂质量比1:10.该条件下所制脂质体外观形态良好,粒径分布均匀,平均粒径为(203±5)nm,平均包封率为55.17%±0.44%,平均载药量为5.04%±0.02%.

Cefquinome sulfate liposome was prepared by solid dispersion and effervescent techniques. The effects of decompression rotary evaporator temperature, volume of chloroform, mass ratios of soybean phosphatidylcholine （SPC） to cholesterol （CH）, drug to lipid and citric acid to NaHCO3, and mass of Tween-80 on its visual form and entrapment efficiency were studied. Orthogonal design was adopted to optimize the formulation, and the formation mechanism of liposomes discussed. The optimized formulation parameters included the mass ratio of SPC/CH/tween-80/citric acid/NaHCO3 at 37：18：5：33：7, and drug/lipid 1：10. The received liposome prepared under the optimized conditions had a good appearance form and uniform size distribution of particles with the mean size of （203±5） nm, entrapment efficiency 55.17%±0.44%, and drug loading rate 5.04%±0.02%, respectively.