摘要
Hirudin 是在自然发现的大多数抗凝剂药，但是它的短浆液半衰期显著地禁止它的临床的申请。hirudin 的 PEGylation，最有希望的抗凝剂药，在这篇论文被执行。为 PEGylated hirudin 的最佳的反应条件被调查。PEGylation 反应什么时候在 10h 以后在 4 ° C 下面被进行，在在最适 PH 的硼酸盐缓冲区 8.5 与到 hirudin 的木钉的摩尔比率 250:1，更高的修正程度被完成。最后， PEGylated hirudin 的 bioactrvity 在 vitro 被测量。与未修改的 hirudin 相比， 26% 反凝血酵素活动被保留。
Hirudin is the most anticoagulant drug found in nature, but its short serum half-life significantly inhibits its clinical anpplication. The PEGvlation of hirudin, the most promising anticoagulant drug, was performed in this paper. The optimal reaction conditions for PEG ylated hirudin were investigated, wh.en the PEGylation react, on.wasconducted under 4℃ after 10h, in the borate buffer at pH 8.5 .with the molar ratio 230 ： 1 of PEG to hirudin, a higher modification extent was achieved. Finally, the bioactivity of PEGylated hirudin was measured in vitro.Compared with unmodified hirudin, 26% of anti-thrombin activity was retained.
