【作者】 吴虹；

【导师】 魏伟；

【作者基本信息】 安徽医科大学 ， 药理学， 2003， 硕士

【摘要】 为了探讨木瓜中抗炎镇痛有效部位——木瓜苷（GCS）的最佳制备工艺并制订其质量标准，本文以抗炎镇痛作用为指标，对木瓜中三种提取物进行了药效学初步筛选，并以正交试验对其提取条件进行了优化研究；研究了大孔吸附树脂分离、纯化GCS的工艺条件和参数，并制订了GCS的质量标准。 在药效及提取工艺条件优化试验中，比较研究了木瓜总提物（TECS）、GCS和非木瓜苷（NGCS）的抗炎镇痛作用。采用二甲苯引起的小鼠耳肿胀模型，观察木瓜中三种提取物的抗炎作用；采用热板法测定小鼠的痛阈，观察三种提取物的镇痛作用。以临床常用的具有抗炎镇痛作用的中药制剂——雷公藤多苷（GTW）为阳性对照药，GCS(60，120，240mg·kg^-1)ig给药，对小鼠耳肿胀均有明显抑制作用，且抑制作用呈剂量相关趋势；NGCS(200，400mg·kg^-1)无抑制作用。GCS(120，240mg·kg^-1)ig给药，可以明显升高小鼠的痛阈，且镇痛作用呈剂量相关趋势。结果表明GCS具有抗炎、镇痛作用，确定了GCS为木瓜抗炎镇痛的有效部位。并通过正交设计，采用L₉（3⁴）表对GCS提取条件进行优化，以芸香苷对照品标示的OCS含量为质控指标，优选出GCS提取的最佳条件，即以80％乙醇为提取溶剂，用8倍量体积，回流1h，提取3次。 在大孔吸附树脂分离纯化试验中，通过对D₁₀₁型大孔树脂分离、纯化GCS工艺条件和参数的研究，探索其工艺流程，建立质量控制体系，从而确立了分离、纯化GCS的可行方法。 以正交试验优选的GCS提取条件提取的样品水溶液上大孔树脂柱（R1.5×H16cm，干重4.2±0.02g），吸附1h后，先用100ml蒸馏水洗脱去除水溶性杂质，然后用100ml 20％乙醇洗脱，再用50％乙醇100ml洗脱出GCS。 利用化学鉴别法和薄层层析法进行鉴别，用比色法测定了GCS含量，平均回收率为99.80％，RSD为1.82％。本方法简便易行，重现性较好，可作为GCS的质控方安徽医科大学硕士学位论文二_<sub>法。 本实验确定了木瓜中抗炎镇痛的有效部位—GCS，以及优化的提取条件。采用大孔吸附树脂分离、纯化工艺，得到纯度大于500/0的GCS，所确立的质量标准可以有效地控制GCS的质量，为GCS及制剂的开发研究奠定了基础，也可为GCS工业生产提供一定的理论参考。更多还原

【Abstract】 In order to research the optimum technics of producing glycosides of chaenomeles speciosa(GCS)-the effective anti-inflammatory and analgesic component of chaenomeles speciosa, and to establish the quality standard, the pharmacodynamics experiments of three extracts from chaenomeles speciosa were studied as the parameter of anti-inflammatory and analgesic effect. Meanwhile,different conditions for extracting GCS were analyzed through the orthogonal design experiments with analysis of variance.The technical conditions and parameters of GCS’s illustration and purification with macroporus adsorptive resin were investigated. The quality standards of GCS were established.To compare the anti-inflammatory and analgesic effects of the total extracts of chaenomeles speciosa (TECS), GCS and non-glycosides of chenomeles speciosa (NGCS),the ear swelling in mice with xylene was used. The anti-inflammatory effects of three extracts from chaenomeles speciosa were observed, hot-plate test was used to assess pain threshold in mice, and observed the analgesic effects of three extracts from chaenomeles speciosa. GCS 60,120,240mg kg-1 ig significantly inhibited the acute imflammation induced by xylene,and demonstrated the dose-related inhibitory effect, NGCS 200,400mg . kg-1 had no inhibitory effect. When GCS 120,240mg . kg-1 administered intragastrically , the pain threshold was risen remarkably in mice,and the analgesic effect was dependent on the dosage. GCS had the effect of anti-inflammation and analgesia. GCS is the effective component of anti-inflammation and analgesia from chaenomeles speciosa.The optimum preparation process of GCS was investigated by the orthogonal design as the GCS content index, which was determined by colormetric method. The optimum alcohol-extracting factors were 8 times of 80% alcohol, refluxing and extracting for Ih, for 3 times.The technical parameters of GCS’s purification with macroporous adsorptive resin were investigated, and the quality control system was established. This technique was a good method to purify GCS.The water solution of the optimum alcohol-extracts was absorbed for Ih with a column of macroporous resin(l.5cm 16cm) and the resin was washed with 100ml of distilled water,then washed with 100ml of 20% alcohol, at last the GCS was eluted from macroporous resin with 100ml of 50% alcohol.The Chemical indentification and TCL of GCS were carried out. GCS was determined by colormetric method. The average recovery was 99.80%,and RSD was 1.82%. This method was simple, feasible and could be repeated. The method could be used to control the quality.The whole of the studies got the best technics of producing GCS, which purity exceeded 50%, and established the quality control standard. It will be the foundation for deeper development and research on GCS and the preparation,and supply the theoretical reference for GCS industrial production.更多还原