卡巴他赛脂质体的制备及其大鼠药动学

发布时间：2018-10-30 07:38

【摘要】：选用氢化大豆磷脂(HSPC)、胆固醇、二硬脂酰磷脂酰甘油(DSPG)为辅料,采用薄膜分散-高压均质法制备卡巴他赛脂质体。以透射电镜观察其形态、动态光散射法测定粒径分布及ζ电位、葡聚糖凝胶柱色谱法测定包封率;采用透析法测定脂质体在体外的释放行为、并测定脂质体在大鼠体内的药动学行为。结果显示,所制得的样品外观和形态较佳、平均粒径为(68.04±1.73)nm、多分散系数为0.213±0.015、ζ电位为(-57.7±1.2)mV、包封率为(86.7±1.5)%。卡巴他赛脂质体在0.05%Tween-80水溶液中的48 h累积释放率为74%,释放速率比注射液(20 h累积释放率为80%)缓慢。卡巴他赛注射液及其脂质体在大鼠体内的AUC_0→∞为(696.89±0.16)和(4 210.07±0.19)ng·ml~(-1)·h,t_(1/2)为(5.85±0.32)和(7.28±0.40)h,提示脂质体有延缓药物释放的作用。
[Abstract]:Carbatin liposomes were prepared by thin-film dispersion and high pressure homogenization with hydrogenated soybean phospholipid (HSPC), cholesterol and distearyl phosphatidylglycerol (DSPG) as auxiliary materials. The morphology was observed by transmission electron microscope, particle size distribution and 味 potential were measured by dynamic light scattering method, encapsulation efficiency was determined by dextran gel column chromatography. The release behavior of liposomes in vitro and the pharmacokinetic behaviors of liposomes in rats were determined by dialysis. The results showed that the average particle size was (68.04 卤1.73) nm, polydispersity coefficient (0.213 卤0.015), Zeta potential was (-57.7 卤1.2) mV, entrapment efficiency was (86.7 卤1.5)%. The cumulative release rate of carbatasai liposome in 0.05%Tween-80 aqueous solution at 48 h was 74%, which was slower than that of injection (20 h cumulative release rate was 80%). The AUC_0 鈭，

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