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目的为得到生长激素释放肽-2(growth hormone releasing peptide-2,GHRP-2)的聚乙二醇(mPEG)修饰产物并考察其稳定性。方法采用mPEG-NHS活性酯,在不同的溶剂条件下,用不同的投料比对GHRP-2进行修饰;HPLC检测反应结果;Sephadex 75凝胶层析法进行分离纯化。结果确定以无水二甲基甲酰胺为溶剂,m(PEG-NHS)∶m(GHRP-2)=1∶1为最佳条件,原料基本消失,主要得到单修饰的GHRP-2。所得产物在pH7.4、pH8.4、pH9.4缓冲液中50 d时的释药率分别为2.1%、7.2%、20.5%。结论无水条件更有利于mPEG-NHS活性酯对GHRP-2的修饰,产物在体外弱碱性条件下较稳定。
The aim was to obtain the polyethylene glycol (mPEG) modified product of growth hormone releasing peptide-2 (GHRP-2) and investigate its stability. Methods mPEG-NHS active ester was used to modify GHRP-2 with different feed ratios under different solvent conditions. The reaction results were detected by HPLC and Sephadex 75 gel chromatography. As a result, it was confirmed that the optimal condition was m (PEG-NHS): m (GHRP-2) = 1: 1 in anhydrous dimethylformamide. The drug release rate of the obtained product at pH7.4, pH8.4, pH9.4 buffer for 50 d were 2.1%, 7.2% and 20.5% respectively. Conclusion Anhydrous conditions are more conducive to mPEG-NHS active ester modified GHRP-2, the product is relatively stable in vitro weakly alkaline conditions.