PHEG-美他沙酮前药的合成及药控释放研究

Synthesis of PHEG-Met Conjugates and the control drug release behaviors

目的研究聚([2-羟乙基)-L-谷酰胺]-美他沙酮前药的合成方法。方法以L-谷氨酸为起始原料合成聚([2-羟乙基)-L-谷酰胺],然后再与美他沙酮连接。结果合成了聚([2-羟乙基)-L-谷酰胺]-美他沙酮,并对产物进行了红外、差示扫描量热分析鉴定和表征。美他沙酮在前药中的质量分数大于16%。合成的前药具有控制释放的功能。结论该合成方法简单,条件温和,具有很好的应用前景。

Aim To report a method for synthesis of poly [ （2-hydroxyethyl） -L-glutamine ] -metaxalone （ PHEG- Met） macromolecule prodrug. Methods Poly [ （2-hydroxyethyl）-L-glutamine ] was prepared by L-glutamic acid, metaxalone was covalently linked to poly [ （2-hydroxyethyl）-L-glutamine ] via a chloroacetyl chloride spacer. Re- suits PHEG-Met was synthesized. The products are characterized by IR and DSC. The content of metaxalone in the prodrug is 16.2%. Conclusion The prodrug preparation method is simple and with mild conditions, high yields, which owns good prospect of application.