大豆磷脂酰聚乙二醇单甲醚2000的制备及性能研究
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摘要
以大豆磷脂为原料,先制备成为反应活性较高的大豆磷脂酸钠,将其与活化的聚乙二醇单甲醚即聚乙二醇单甲醚2000对甲苯磺酸酯(mPEG_(2000)-OTs)反应制备了大豆磷脂酰聚乙二醇单甲醚2000(SP-mPEG_(2000))。实验得到最优的制备工艺为:以65mg NaH处理大豆磷脂得到大豆磷脂酸钠,m(大豆磷脂酸钠):m(mPEG_(2000)-OTs)=0.45:1,反应时间为4h,反应温度为90℃,在最佳合成条件下转化率为71.2%,产物为淡黄色固体。产物结构经~1H-NMR和IR表征,表明已成功制备得到SP-mPEG_(2000)。该法的优点是反应条件温和,同时能够将大豆磷脂中的各种组分均进行充分利用,在前人基础上提高利用率。SP-mPEG_(2000)水溶液临界胶束浓度为0.5 g.L~(-1),此时表面张力(γ_(CMC))为42 mN·m~(-1)。通过SP-mPEG_(2000)对正己烷和水形成的乳状液的稳定性表征,表明产物的动力学稳定性优于大豆粉末磷脂。
With soybean phospholipid as raw material,first,it was prepared into sodium soy phospholipids of high reactive activity and then reacted with activated monomethoxypolyethylene glycol,namely,monomethoxypolyethylene glycol 2000 tosylate(mPEG_(2000)-OTs) and soybean phosphatidyl methoxy polyethylene glycol 2000 esters(SP-mPEG_(2000) were synthesized.Optimal experiments of preparation were as follows:soybean phospholipid was treated with 65 mg NaH to obtain sodium soy phospholipids,m(sodium soy phospholipids):m(mPEG2000-OTs) = 0.45:1,reaction time was 4 h and the reaction temperature was 90 ℃,under optimal conditions the conversion was 71.2%,and the product as a pale yellow solid.The product structure was characterized by ~1H-NMR and IR,which indicating the successful preparation of SP-mPEG_(2000).The critical micelle concentration of SP-mPEG_(2000) is 0.5 g·L~(-1) by surface tension(γ_(CMC)) is 42 mN·m~(-1),The kinetic stability of SP-mPEG_(2000) was characterized by emulsifying power of n-hexane and water,which indicated that kinetic stability of the product is superior to soy lecithin powder.
引文
[1]Greenwald R B.PEG drugs:an overview.Journal of Controlled Release Official Journal of the Controlled Release Society,2001,74(1-3):159.
    [2]陈庆春,邓慧宇,马燕明.聚乙二醇在新材料制备中的作用及其机理.日用化学工业,2002,32(5):35.

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