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目的:合成具有肝靶向意义的2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷,并考察其肝脏靶向性能。方法:以半乳糖为起始物,经乙酰化、澳代、缩合、置换,加醇后得目的化合物。小鼠尾静脉注射给药后,HPLC测定药物在小鼠肝脏及血液中的浓度。结果:目标化合物经IR和MS进行了结构确证。白蛋白微球表面偶联2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷,肝靶向效率增大约1.5倍。结论:所制半乳糖白蛋白微球趋肝性能增强。
OBJECTIVE: To synthesize 2-imino-2-methoxyethyl-1-thio-β-D-galactopyranoside with liver targeting and to investigate its liver targeting properties. Methods: galactose as starting material, acetylation, O generation, condensation, replacement, add alcohol to obtain the desired compound. After the mice were injected through the tail vein, the concentrations of the drugs in the liver and blood of the mice were determined by HPLC. Results: The target compounds were confirmed by IR and MS. Coupling 2-imino-2-methoxyethyl-1-thio-β-D-galactopyranoside on the surface of albumin microspheres increased the efficiency of liver targeting by about 1.5 times. Conclusion: The galactose-loaded microspheres have enhanced liver function.