【摘要】：選用氫化大豆磷脂(HSPC)、膽固醇、二硬脂酰磷脂酰甘油(DSPG)為輔料,采用薄膜分散-高壓均質(zhì)法制備卡巴他賽脂質(zhì)體。以透射電鏡觀察其形態(tài)、動態(tài)光散射法測定粒徑分布及ζ電位、葡聚糖凝膠柱色譜法測定包封率;采用透析法測定脂質(zhì)體在體外的釋放行為、并測定脂質(zhì)體在大鼠體內(nèi)的藥動學行為。結(jié)果顯示,所制得的樣品外觀和形態(tài)較佳、平均粒徑為(68.04±1.73)nm、多分散系數(shù)為0.213±0.015、ζ電位為(-57.7±1.2)mV、包封率為(86.7±1.5)%�？ò退愔|(zhì)體在0.05%Tween-80水溶液中的48 h累積釋放率為74%,釋放速率比注射液(20 h累積釋放率為80%)緩慢�？ò退愖⑸湟杭捌渲|(zhì)體在大鼠體內(nèi)的AUC_0→∞為(696.89±0.16)和(4 210.07±0.19)ng·ml~(-1)·h,t_(1/2)為(5.85±0.32)和(7.28±0.40)h,提示脂質(zhì)體有延緩藥物釋放的作用。
[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 鹵1.73) nm, polydispersity coefficient (0.213 鹵0.015), Zeta potential was (-57.7 鹵1.2) mV, entrapment efficiency was (86.7 鹵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，

本文編號：2299368