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以吲哚美辛(1)为原料先经酯化反应和Knoevenagel缩合,再与可溶性淀粉连接,合成了侧链含有阿魏酸的高分子载体药物(4),该化合物未见文献报道.用比浊法和放免法测定了(4)体外对兔血小板聚集以及对TXB2,6KetoPGF1α含量的影响.化合物(4)240μmol·L-1对AA诱导的兔血小板聚集的抑制率为396%,对TXB2释放的抑制率为287%.与吲哚美辛(1)或阿魏酸比较,阿魏酸衍生物高分子载体药物(4)显示有抑制兔体外血小板聚集和抑制TXB2,6KetoPGF1α释放的作用,呈现明显的药物协同作用.
The indomethacin (1) was used as the raw material to esterify and Knoevenagel, and then linked with soluble starch to synthesize a polymer carrier drug containing side-chain ferulic acid (4). This compound has not been reported in the literature. With turbidimetry and radioimmunoassay (4) in vitro rabbit platelet aggregation and TXB2,6 Keto PGF1α content. Compound (4) 240μmol·L-1 on AA-induced rabbit platelet aggregation inhibition rate was 39 6%, TXB2 release inhibition rate of 28 7%. Compared with indomethacin (1) or ferulic acid, ferulic acid derivative polymer carrier drug (4) showed inhibition of rabbit platelet aggregation in vitro and inhibition of TXB2, 6 Keto PGF1α release of the role of showing obvious drug Synergy.