苦豆子总生物碱冻干粉针的制备及其抑瘤作用考察  

Preparation of total alkaloids from Sophora alopecuroides freeze-dried powders and investigation of its antitumor effects

作　　者：闫家福[1,2] 仝燕[1] 蒲纯[3] 王锦玉[1] 

机构地区：[1]中国中医科学院中药研究所,北京100700 [2]中国专利信息中心,北京100088 [3]卫计委北京医院,北京100005

出　　处：《中国中药杂志》2014年第7期1234-1237,共4页China Journal of Chinese Materia Medica

基　　金：国家"重大新药创制"科技重大专项(2009ZX09301-005)

摘　　要：目的： 考察苦豆子总生物碱注射用冻干粉针的成型工艺并观察其对小鼠肝癌H22移植性肿瘤的抑瘤作用。方法：以颜色、澄明度、水溶性及成形性为指标，通过单因素试验筛选充填剂的种类和用量，确定苦豆子总生物碱注射用冻干粉针的最佳处方；选取药液质量浓度及pH为考察因素，采用单因素试验优选苦豆子总生物碱注射用冻干粉针的制备工艺，测定最低共熔点并绘制冷冻干燥曲线。通过在小鼠右腋皮下无菌接种小鼠肝癌H22腹水瘤瘤株，观察苦豆子总生物碱注射用冻干粉针对该移植性肿瘤的抑瘤作用。结果：选取80 g·L-1甘露醇为填充剂，冻干前药液中苦豆子总生物碱质量浓度为25 g·L-1，pH 6.5~7.5时，冻干效果最好，复溶速度快。苦豆子总碱注射用冻干粉针高（120 mg·kg-1）、中（60 mg·kg-1）剂量组对小鼠肝癌H22移植性肿瘤的平均抑瘤率分别为56.08%，35.49%。结论：苦豆子总生物碱冻干粉针制备工艺合理且重复性好，质量稳定，对小鼠肝癌H22移植性肿瘤具有明显的抑瘤作用并呈明显量效关系。Objective： To investigate molding technology of total alkaloids from Sophora alopecuroides freeze-dried powders and observe its inhibition effects on liver transplantation tumor in mice. Method： With color, clarity, water-soluble and formability as indexes, single factor tests were adopted to screen type and amount of filler, the concentration of total alkaloids in drug liquid, pH in order to determine optimum prescription of total alkaloids from S. alopecuroides freeze-dried powders, the lowest melting point was determined and freeze drying curve was drafted. Mice hepatoma H22 ascites tumor strain was sterile inoculated in right axillary subcutaneous of mice, and antitumor effect of total alkaloids from S. alopecuroides freeze-dried powders on liver transplantation tumor H22 in mice. Result： When selected 80 g·L-1 as mannitol as filler, the concentration of total alkaloids in drug liquid was 25 g·L-1 and pH 6.5-7.5, freeze-dried effect was optimum with fast reconstitute speed. Average inhibition rate of the big （120 mg·kg-1） and medium （60 mg·kg-1） dose group of total alkaloids from S. alopecuroides freeze-dried powders on liver transplantation tumor H22 in mice were 56.08% and 35.49%, respectively. Conclusion： Preparation technology was reasonable, reproducible and stable, total alkaloids from S. alopecuroides freeze-dried powders had significant antitumor effect and showed a dose-effect relationship.

关 键 词：苦豆子总生物碱冻干粉针剂 制备工艺 肝癌 抑瘤率 

分 类 号：R735.7[医药卫生—肿瘤] TQ461[医药卫生—临床医学]