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目的探索通过聚乙二醇修饰技术以改善麦冬多糖MDG-1的药动学性质。方法以氨基聚乙二醇单甲醚作为修饰剂,研究聚乙二醇修饰MDG-1的合成反应条件,用高效凝胶色谱法测定修饰物的表观相对分子质量与接枝率,并考察其药动学性质。结果确定了优化的合成条件,制得多种用不同相对分子质量聚乙二醇修饰的具有不同接枝率的MDG-1聚乙二醇修饰物,其生物半衰期较原药有明显的延长,延长程度与修饰剂的相对分子质量和修饰物的接枝率有关。结论聚乙二醇修饰技术是一个具有进一步研究前景的改善MDG-1药动学性质的方法。
OBJECTIVE: To explore the pharmacokinetics of MDG-1 through the modification of polyethylene glycol. Methods Amino polyethylene glycol monomethyl ether was used as a modifier to study the synthesis conditions of polyethylene glycol modified MDG-1. The apparent relative molecular mass and grafting degree of modified MDG-1 were determined by high performance gel permeation chromatography Its pharmacokinetic properties. Results The optimized synthesis conditions were determined, and a number of modified MDG-1 PEG modified with different molecular weight polyethylene glycol were obtained. The biological half-life of MDG-1 was significantly longer than that of the original drug. The degree of extension is related to the relative molecular mass of the modifier and the graft rate of the modifier. Conclusion Polyethylene glycol modification is a promising method to improve the pharmacokinetics of MDG-1.