高分子微球偶联固定卡托普利药物分子的研究  

Study on the Covalent Immobilization of Captopril onto Polymer Microspheres

作　　者：张妙[1,2] 方仕江[1] 金志敏[2] 

机构地区：[1]浙江大学化学工程国家重点实验室,聚合与聚合物工程研究所,杭州310027 [2]浙江工业大学药学院,杭州310014

出　　处：《高分子通报》2012年第8期85-91,共7页Polymer Bulletin

基　　金：国家自然科学资金资助项目(20676113);浙江大学化学工程国家重点实验室经费资助

摘　　要：采用无皂乳液聚合法制得聚苯乙烯-甲基丙烯酸缩水甘油酯(PSG)乳液微球,然后在微球表面嫁接空间臂分子1,6-己二胺,得到表面含氨基的PSGN微球,接着借助EDC/NHS催化作用将药物分子卡托普利化学偶联到PSGN微球表面,制成固定卡托普利的亲和PSG微球。实验着重考察了PSGN微球偶联固定卡托普利反应过程中催化剂比例和用量、pH值、反应温度和时间等的影响规律。结果表明,在25℃,pH为4.0,m(NHS)∶m(EDC)=1∶2,EDC的浓度为4mg/mL的条件下,卡托普利偶联到微球表面的效果较好。The poly （styrene-co-glyeidyl methacrylate） （PSG） latex microspheres were prepared by soap-free emulsion polymerization. The resulted PSG microspheres were further modified with 1,6- hexanediamine as a space arm to get the amino-modified PSGN microsphere. Captopril was coupled onto the surface of PSGN microspheres by the activation with N ethylcarbodiimide hydrochloride （EDC） and polymer microspheres immobilized captopril N-Hydroxysuccinimide （ 3-dimethylaminopropyl ）（NHS）, so that the affinity was finally obtained. The effects of the ratio and concentration of catalysts, pH, temperature and time on the coupling reaction between the PSGN mierospheres and captopril were examined. It was shown that the effect of immobilization was much better under the condition of 25℃, pH=4.0, m（NHS）：m（EDC）=1： 2, m（EDC）=4mg/mL.

关 键 词：无皂乳液聚合 亲和微球 卡托普利 苯乙烯 甲基丙烯酸缩水甘油酯 

分 类 号：R917[医药卫生—药物分析学] TQ460.1[医药卫生—药学]