【摘要】 采用逆相蒸发法结合冷冻干燥法制备重酒石酸长春瑞滨(1)脂质体,考察其理化性质和在大鼠体内的药动学。透射电镜观察表明,1脂质体的粒子形态呈球形。制品平均粒径为(221.5±19)nm,包封率为(86.7±1.0)%,24 h累积释放率为83.4%。大鼠尾静脉注射1溶液或1脂质体溶液后,所得主要药动学参数t1/2?分别为(0.09±0.03)和(0.32±0.10)h,t1/2?分别为(1.45±0.21)和(4.00±0.25)h;AUC0→t分别为(2.44±0.12)和(37.75±0.98)mg·h·L-1,AUC0→∞分别为(2.71±0.52)和(38.16±0.98)mg·h·L-1。更多还原

【Abstract】 Vinorelbine bitartrate(1) liposomes were prepared by reverse-phase evaporation combined with freeze-drying method. The properties and pharmacokinetics of the product were investigated. The results of transmission electron microscopy(TEM) showed that the product was almost spherical. The mean diameter and entrapment effi ciency of 1 liposomes were(221.5±19)nm and(86.7±1.0)%. The cumulative release at 24 h of 1 from the liposomes was about 83.4%. The pharmacokinetic behaviors of 1 solution and its liposomes in rats after intravenous administration were evaluated. The main pharmacokinetic parameters were as follows: t1/2?(0.09±0.03) and(0.32±0.10)h, t1/2?(1.45±0.21)and(4.00±0.25)h, AUC0→t(2.44±0.12) and(37.75±0.98)mg·h·L-1, AUC0→∞(2.71±0.52) and(38.16±0.98)mg·h·L-1.更多还原