聚乙二醇化修饰对蛋白多肽药物药代动力学的影响

聚乙二醇（PEG）化修饰在生物制药领域被认为是改变蛋白多肽类药物生物、理化性质的最佳方法之一。众多研究表明，PEG化后的蛋白多肽在生物体内的药代动力学行为有了很大改变，主要表现在：吸收相半衰期及消除相半衰期延长．血药峰浓度提高，达峰时间滞后，表观分布容积变小，免疫反应性减弱，血浆清除减慢。这些变化极大地改善了蛋白多肽药物在机体内清除快、免疫原性高、有效血药浓度持续时间短、需频繁给药等缺点。聚乙二醇化修饰为生物制药领域开辟了新的天地。

The Effects of Pegylation on the Pharmacokinetics of Polypeptide

Pegylation was assumed to be one of the optimal approaches changing the biological activity, the physical and chemical characterization of polypeptide in biological medication field. Studies indicate that the pharmacokinetic properties of polyethylene glycol-modified polypeptide have been improved greatly, which mainly shows a longer absorption and elimination half-life time, a greater Cmax(peak concentration), a delayed Tpeak(peak time), a restricted Vd(apparent volume of distribution), a depressed immune response, and a decreased Cl(plasma clearance). These changes of polypeptide have exceedingly improved their disadvantages such as accelerated clearance in human beings, intense immunogenicity, a short sustained periods of effective concentration, frequent administrations, et al. Pegylation has broken a new ground for biological medication.