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半乳糖化白蛋白汉防己甲素纳米粒的合成
引用本文:余潜,;王卓缨,;肖大伟. 半乳糖化白蛋白汉防己甲素纳米粒的合成[J]. 上海中医药杂志, 2009, 43(6): 80-82
作者姓名:余潜,  王卓缨,  肖大伟
作者单位:南京医科大学附属南京第一医院临床药理实验室,江苏,南京,210006;南京陕科大学第二临床医学院心内科,江苏,南京,210029
基金项目:江苏省南京市科技局项目(2006ZD0164)
摘    要:目的制备半乳糖化白蛋白汉防己甲素纳米粒(Galn-BSA-Tet-NPs),并考察合成半乳糖化白蛋白的最佳条件。方法以乳糖和牛血清白蛋白为原料,采用还原胺化法制备半乳糖化白蛋白(Gain-BSA)。采用苯酚-硫酸比色法测定糖化比率,以糖化比率作为指标考察反应的pH、时间、催化物剂量的多个水平,从中选出最优化组合。并采用去溶剂化法制备半乳糖化白蛋白汉防己甲素纳米粒(Galn-BSA-Tet-NPs)。结果制备半乳糖化白蛋白的最佳条件是磷酸缓冲液的pH值为7.4,反应时间为80h,氰基硼氢化钠的催化量为0.8mmol/L;成功合成了半乳糖化白蛋白汉防己甲素纳米粒(Gain-BSA-Tet-NPs)。结论汉防己甲素可以采用去溶剂化法制备成半乳糖化白蛋白纳米粒,此方法可提高汉防己甲素在水相中的浓度,并靶向肝细胞,从而增强汉防己甲素的抗肝纤维化药效。

关 键 词:汉防己甲素  肝靶向  半乳糖基牛血清白蛋白  苯酚-硫酸比色法

Systhesis of Galactosyl-BSA in Nanoparticles Containing Tetrandrine
Affiliation:YU Qian, WANG Zhuo-ying, XIAO Da-wei(1. The First Hospital Affiliated to Nanjing Medical University;2. The Second Hospital Affiliated to Nanjing Medieal University)
Abstract:Objective To prepare Galactosyl-BSA in nanoparticles containing Tetrandfine and study its optimum synthesis conditions. Methods Galactose and BSA ( bovine serum albumin) were incorporated into Galn-BSA by reductive amination method. The phenol-sulfuric calorimetric method was applied to analyze the molar ratio of the galactose to BSA by evaluating pH, time and the dose of the catalist. Galactosyl-BSA in nanoparticles containing Tetrandrine were prepared by desolvation-chemical crosslinking method. Results The optimum condition for preparing Galn-BSA was phosphate buffer of pH 7.4, 0.8 mmol/L sodium cyanoboro- hydride within 80 hours. Conclusion Galn-BSA-Tet-NPs can be prepared to increase the concentration of Tel in water.
Keywords:Tetrandrine  hepatic targeting  Galactosyl-BSA  phenol-sulfuric colorimetry
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