高取代度羧甲基茯苓多糖(CMP)的制备及其注射剂的研制

Preparation of Carboxymethylpachymaran(CMP) with High Degree of Substitution and Its Injection

为研究高取代度羧甲基茯苓多糖(CMP)及其注射剂的制备工艺条件,以中药茯苓粉为原料,正交试验优化其羧甲基反应的工艺条件,并对所制备的多糖注射剂进行性能鉴定和药理学试验。结果表明:所获得的羧甲基茯苓多糖取代度高、纯度高,具有羧甲基反应特征,最优反应工艺条件为氯乙酸:氢氧化钠=1.15:1,反应温度75℃,反应时间3 h,此最优组合下羧甲基取代度(DS)值为1.21。所制备的多糖注射剂性状稳定、无毒、无热原性和无刺激性,安全可靠。羧甲基茯苓多糖具有直接抑制或杀死肿瘤细胞、增强巨噬细胞吞噬、调节机体免疫功能的药理作用。高取代度羧甲基茯苓多糖及其注射剂的研制可为丰富茯苓多糖的产品类型、拓宽应用范围及市场投入提供前期的理论基础。

To study the process conditions of carboxymethylpachymaran（CMP） with high degree of substitutionand its injection, using Poria cocos powder as raw material, the carboxymethyl reaction process conditions ofCMP were optimized by orthogonal experiments. And CMP injection was prepared and tested by performancetesting and pharmacology experiment. The results indicated that the obtained CMP had high degree ofsubstitution, high purity and had carboxymethyl reaction characteristics. The optimal process condition for thecarboxymethyl group substitution of pachyman was chloroacetic acid： sodium hydroxide=1.15：1, the reactiontemperature 75℃, the reaction time 3 h. Under this optimal condition, the degree of carboxymethyl groupsubstitution（DS） was 1.21. The CMP injection was stable, non-toxic, non-pyrogenic and non-irritating, so itwas safe and reliable. The CMP could directly inhibit or kill tumor cells, enhance the phagocytosis ofmacrophages, regulate the immune function of the body. Preparation of CMP and its injection could help toenrich the product type of the polysaccharide, broaden the application scope and provide the early stagetheoretical basis for the market investment.