抗癌新药3′,5′-环胞苷二棕榈酸酯脂质体的研究  

STUDIES ON A NEW ANTITUMOR PHARMACEUTICAL 3′,5′-DIPALMITOYL CYCLOCYTIDINE LIPOSOME

作  者:王继波[1] 侯新朴[2] 赵辉[1] 

机构地区:[1]青岛医学院化学教研室 [2]北京医科大学药学院物化教研室

出  处:《青岛医学院学报》1990年第2期91-9,共1页Acta Academiae Medicinae Qingdao Universitatis

摘  要:将3′,5′-环胞苷二棕榈酸酯包封于脂质体中.药效学研究表明,药物的脂质体剂型对腹水型肝癌细胞的抑制率比游离药物以及阿糖胞苷脂质体的抑制率高1倍以上.化学动力学实验显示,在pH为6.9时,脂质体中药物的分解反应速度比游离药物慢得多,其有效期比游离药物长3倍以上.用荧光法研究药物分子在脂双层上的状态,探讨了药物包封于脂质体中抗癌活性及化学稳定性提高的原因.We made a study of 3' ,5' -Dipalmitoyl Cyclocytidine (DP CyC-C) encapsulated in liposome composed of phosphatidyl choline(PC). Pharmacodynamatical results Showed that the efficiency of liposomal DP CyC-C in inhibiting ascites cancer liver cells was over twice as high as that of the unencapsulated drug and liposomal Ara-C. Chemical kinetic experiment showed that with pH=6.9, the decomposition rate of DP CyC-C in liposome was much lower than when it is in free state. The shelflife of liposomal doses of DP CyC-C was over four times as long as that of unencapsulated ones. The molecular state of the drug in lipid bilayer was studied and the mechanism which resulted in the increase in antitumor activity and chemical stability was analysed.

关 键 词:抗癌药 环胞苷 二棕榈酸酯 

分 类 号:R979.19[医药卫生—药品]

 

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