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采用蔗糖八硫酸酯三乙胺梯度法制备聚乙二醇2000-二硬脂酰磷脂酰乙醇胺(PEG2000-DSPE)摩尔比分别为6%、3%和1%的酒石酸长春瑞滨(1)脂质体。考察了3种处方脂质体的药物粒径、ζ电位、包封率、体外释放度和稳定性。以1注射液为对照,比较3种脂质体对裸鼠SW620移植瘤的生长抑制作用。结果表明,3种处方脂质体的体外特性基本一致,且4℃条件下放置6个月,各样品的主要质量指标均未发生显著变化。药效学研究结果表明,PEG2000-DSPE含量由高至低的各脂质体组抑瘤率分别为52.8%、72.1%和61.8%,而1注射液组抑瘤率仅47%。
The sucrose octasulfate triethylamine gradient method was used to prepare vinorelbine tartrate (1) with polyethylene glycol 2000-distearoylphosphatidylethanolamine (PEG2000-DSPE) molar ratio of 6%, 3% and 1% Plastids. The drug particle size, zeta potential, entrapment efficiency, in vitro release and stability of three kinds of prescription liposomes were investigated. 1 injection as a control, the three liposomes on nude mice SW620 tumor growth inhibition. The results showed that the in vitro characteristics of the three kinds of prescription liposomes were basically the same, and placed at 4 ℃ for 6 months, the main quality indicators of each sample did not change significantly. The results of pharmacodynamic studies showed that the antitumor rates of liposomes with PEG2000-DSPE contents ranging from high to low were 52.8%, 72.1% and 61.8%, respectively, while the inhibition rate of the 1 injection group was only 47%.