可控降解抗感染材料的合成和表征  

Synthesis and characterization of antimicrobial material controlled degradation

作　　者：李春艳[1] 出端艳[1] 单丽[1] 温志国[2] 黄剑华[2] 董声雄[2] 丁马太[3] 

机构地区：[1]福建医科大学药学院,福建福州350108 [2]福州大学化学化工学院,福建福州350108 [3]厦门大学材料学院,福建厦门361005

出　　处：《功能材料》2010年第4期730-733,736,共5页Journal of Functional Materials

基　　金：福建省科技厅国际合作处重点资助项目(2006I0019);福建省科技厅资助省属高校资助项目(2008F50502)

摘　　要：在聚己内酯(PCL)与六亚甲基二异氰酸酯(HDI)缩合体系中加入抗菌药物环丙沙星(CF),制备CF嵌入聚氨酯(PU)主链的聚氨酯前药CFPU。用UV、FTIR、H-NMR表征其结构;GPC法测定分子量;UV法测定载药率;摸索影响其分子量和载药率的主要因素;并用琼脂稀释法测定其胆固醇酯酶(CE)降解液对金黄色葡萄球菌的抗菌活性。结果表明,确已成功制得目标产物;PCL浓度和HDI加料方式分别对其平均分子量和载药率有较大影响;而其CE降解液对金黄色葡萄球菌具有抗菌活性。因此,当其用作医用内植物的涂层材料时,能被炎症组织所分泌的CE可控降解为这种具抗菌活性的降解液,从而可发挥抗感染作用。Polyurethane prodrug（CFPU）,was synthesized via polyurethane condensation reaction,with polycarprolactone（PCL） as soft-segment,1,6-hexane diisocyanate（HDI） as hard-segment and an antibiotics drug,ciprofloxacin（CF）.The structure of CFPU was characterized by UV,FTIR,H-NMR,the molecular weight was determined through the method of GPC,the drug-loading rate was determined by UV.The influence factors of molecular weight and drug-loading rate were studied.The antibacterial activity of prodrug degradation solution to staphylococcus aureus,degraded by cholesterol esterase （CE）,was determined by agar dilution.The result suggested that polymer prodrug had been successfully synthesized by incorporating ciprofloxacin into polyurethane.The concentration of PCL has great effect on the average molecular weight of CFPU,while the feeding way of HDI has great effect on the drug-loading rate.CFPU degradation solution has shown an ability to kill Staphylococcus aureus.CFPU coated within the medical material implants,it can be controlled degraded by CE,which produced by inflammation,can reach the effect of anti-infection.

关 键 词：环丙沙星 聚氨酯 高分子前药 可控降解 抗感染 

分 类 号：R914.5[医药卫生—药物化学] R978.5[医药卫生—药学]