阿昔洛韦药质体的制备和性质  

Preparation and Properties of Acyclovir Pharmacosomes

作　　者：金义光[1] 艾萍[2] 李淼[2] 侯新朴[1] 

机构地区：[1]北京大学药学院物理药学研究室,北京100083 [2]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《中国医药工业杂志》2005年第10期617-621,共5页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金资助项目(30371700)

摘　　要：合成了琥珀酰阿昔洛韦单硬脂酸甘油酯,用四氢呋喃注入法得到药质体。透射电镜观察和激光散射检测表明药质体是纳米粒度的囊泡,呈负电;差示扫描量热法测得其凝胶-液晶相变温度为50℃。离心和加热对药质体稳定性影响较小,可用加热法灭菌。冷冻和冻干会破坏药质体结构。两亲性的药质体单体分子可插入家兔红细胞膜,并引起溶血,但全血中的血浆蛋白可吸附药质体或干扰其与红细胞的作用,减少溶血反应。Acyclovir succinyl glyceryl monostearate was synthesized and utilized as pharmacosomes by tetrahydrofuran injection method. The negative charged pharmacosomes were nanometer vesicles based on the analysis of transmission electron microscope and laser scattering method. The gel-liquid crystalline phase transition temperature was 50℃ by differential scanning calorimetry. The effects of centrifugation and heating on the stability of pharmacosomes were weak, and stassanization was suitable for pharmacosomes. Freezing and lyophilization disrupted pharmacosomal structure. The amphiphilic pharmacosomes would insert into rabbit erythrocyte membranes and led to hemolysis. Plasma proteins in blood absorbed pharmacosomes or interfered the interaction with erythrocytes to reduce hemolytic reaction.

关 键 词：阿昔洛韦 药质体 两亲性 自组装 囊泡 红细胞 

分 类 号：R944.9[医药卫生—药剂学] R978.7[医药卫生—药学]