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目的制备载诺帝(去甲二氢愈创木酸)脂质微泡并测定其包封率、载药量及观察其体内超声显像效果。方法采用机械振荡法制备载诺帝脂质微泡,测定其粒径大小、分布和Zeta电位、包封率、载药量;超声造影观察其在兔肝内的显像效果。结果载药脂质微泡的浓度为(2.53±0.52)×10~9个/ml,粒径为(2.61±0.32)μm,Zeta电位为+(17.52±2.04)mV;脂质微泡诺帝的包封率(27.1±2.01)%,载药量为(10.9±0.90)%;微泡经外周静脉注射后,兔肝可见良好、持续的增强显像效果。结论采用机械振荡法可以成功制备携带诺帝的脂质微泡,微泡可以通过肺血管床,符合静脉注射要求,在家兔体内获得了良好的显像效果。
OBJECTIVE To prepare the lipid microtubules loaded with nocodimic acid (nordihydroguaiaretic acid) and determine its entrapment efficiency, drug loading and observe the effect of ultrasound imaging in vivo. Methods Loaded Nordrhein liposomes were prepared by mechanical vibration method. The size, distribution, Zeta potential, entrapment efficiency and drug loading were measured. The imaging results were observed by contrast-enhanced ultrasound. Results The concentration of lipid microbubbles was (2.53 ± 0.52) × 10 ~ 9 / ml, the particle size was (2.61 ± 0.32) μm and the Zeta potential was + (17.52 ± 2.04) mV. (27.1 ± 2.01)% and the drug loading was (10.9 ± 0.90)%. After the microvesicles were injected through the peripheral vein, the rabbit liver showed a good and sustained enhanced imaging effect. Conclusions Lipid microbubbles carrying Nordisk can be successfully prepared by mechanical vibration method. Microbubbles can pass through the pulmonary vascular bed and meet the requirements of intravenous injection. Good imaging results are achieved in rabbits.