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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
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摘要 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.
出处 《西北大学学报(自然科学版)》 CAS CSCD 北大核心 2011年第6期998-1000,共3页 Journal of Northwest University(Natural Science Edition)
基金 陕西省自然科学基金资助项目(2011JM2114) 陕西省教育厅自然科学基金资助项目(09JK791)
关键词 聚[(2-羟乙基)-L-谷酰胺] 前药 美他沙酮 Poly [ (2-hydroxyethy) -L-glutamine ] prodrug metaxalone
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