【作者】 王慧君；

【导师】 赵长山；

【作者基本信息】 东北农业大学 ， 农药学， 2010， 硕士

【摘要】 米尔贝(Milbemycins)是从Streptomyce hygroscopicus subsp.的发酵产物中提取的一类十六元大环内酯混合物。三共(Sankyo)株式会社在1973年用未试验棉红蜘蛛进行新的杀虫抗生素筛选时,发现该发酵产物对多种害虫有独特的效果。当前,米尔贝已在日本、欧美等多个国家登记,并且作为安全、对环境友好的杀虫杀螨剂被美国环保局推荐使用。米尔贝被认为是目前最有前途的广谱、高效、新型、无交叉抗性的生物杀虫剂。鉴于我国尚未有米尔贝类杀虫杀螨剂的登记注册,农业害虫防治又需要像米尔贝这种高效、低毒、安全、环保的药剂。本研究旨在将米尔贝加工成适宜其理化性质、相对其他剂型药效高的乳油制剂,并优化筛选了乳油配方中的有机溶剂及乳化剂的种类与含量,解决了传统乳油由于有机溶剂的大量使用而造成的环境污染问题,最终得到的乳油制剂对环境友好,能保证米尔贝原药的高效生物活性的发挥。配方中乳化剂的筛选方法为系列HLB值试验筛选法。光稳定剂筛选首先考察了光对米尔贝的影响,然后选用不同的稳定剂,测定光稳定剂对米尔贝分解的抑制作用,进行多重比较,最终确定配方中最优稳定剂。乳油小样加工按照试验室制备方法,将原药溶于一定量溶剂,加入合适的乳化剂,再加入稳定剂溶液。室内生物测定采用的是叶片残毒法,室外盆栽试验以喷雾植株茎叶为施药方法,考察药后的死亡率,校正死亡率及防效。试验结果表明:经过对各种辅助剂的筛选,最后得出的5%米尔贝乳油配方为:有效成分米尔贝的含量为5%,乳化剂NP10和EL90分别占6.8%和1.2%,抗氧化剂1010含量为1%,溶解光稳定剂的乙酸乙酯含量为2%,溶剂油200#补足至100%。按照国家标准对按上述配方工艺制得的乳油制剂进行质量检测,乳油制剂的各指标测定结果均符合国家乳油标准:有效成分含量符合制剂要求,制剂的物理化学稳定性较好,外观均相油体,无可见悬浮物或沉淀,含水量≤0.5%,挥发率≤30%,冷热贮稳定性合格。室内生物测定试验结果表明5%米尔贝乳油对红蜘蛛和菜蚜有较好的防效,其LC50分别为0.7002mg?L-1和0.9822 mg?L-1。与同类药剂1.8%阿维菌素乳油相比,防治红蜘蛛的效果较优,防治菜蚜的效果稍差,用5%米尔贝乳油的50 000倍液防治红蜘蛛的防效,与用1.8%阿维菌素乳油10 000倍液的防效相当,即米尔贝对红蜘蛛的活性显著高于阿维菌素。更多还原

【Abstract】 Milbemycins are a class of 16 yuan macrolide compounds. Extracting from the fermentation products of Streptomyce hygroscopicus subsp. Sankyo Co., Ltd. Screening the new insecticidal antibiotic with not test new cotton spider in 1973, they found that the fermentation product has a unique effect on a variety of pests. Currently, Milbemycin has registered in Japan, Europe and the United States and other countries, and as safety, environmentally friendly insecticide acricide was recommended by the U.S. Environmental Protection Agency. Milbemycin is considered the most promising broad-spectrum, highly efficient, new pattern and no cross resistance biological pesticides. In view of that milbemycin insecticide acricide is not registered in China, yet agricultural pest control needs the pesticide just as Milbemycin, efficient, low toxicity, safety, environmental. This study aims to be processed the milbemycin into EC, which is high efficacy relatives to other formulaitons and suitable for its physical and chemical properties, screened of organic solvent and emulsifier types and content for the EC formulation, solved the environmental pollution problems that caused by largely to use organic solvents. The resulting EC can guarantee for environmental friendly and efficient bioactive of the original drug to play.Screening for the emulsifier adopted HLB value of test screening. Light stabilizer selecting firstly investigated the influence of light on the Milbemycin decomposition, and secondly chose different stabilizer, measured the inhibition of decomposition, after multiple comparison, at last determine the optimal stabilizer. EC sample processing methods in accordance with the preparation method in the laboratory, the original drug dissolved in a small amount of solvent, adding a suitable emulsifier, and then stabilizer. Bioassay using the leaf residue method for the outdoor pot experiment with spray application method to study mortality, mortality and control effect correction.The results showed that:After the screening of various auxiliary agents, finally reached 5% milbemycin EC formula: Milbemycin active ingredient content of 5%, emulsifier NP10 and EL90 accounted for 6.8% and 1.2%, light stabilizer 1010 1%, the content of ethyl acetate dissolving light stabilizer is 2%, solvent oil 200# make up to 100%.According to national standards by the EC formulation product is a preparation for quality inspection, EC is the result of various index measures the EC are in line with the national standards: physical and chemical stability is good preparation, the appearance of homogeneous oil bodies, no visible suspended solids or precipitation, water content less than 0.5%, volatile rate of less than 30%, hot and cold storage stability of the pass.Bioassay results showed that 5% milbemycin EC control effect on red spider is better than cabbage aphid, the LC50 were 0.7002mg?L-1, 0.9822 mg?L-1. Compared to 1.8% Abamectin EC, control red spider well, the effect of cabbage aphid is little worse. 5% milbemycin EC 50 000 times control red spider, and equal to 1.8% Avermectin EC 10 000 dilution of the control effect. That is say, Milbemycin on the red spider was significantly higher than abamectin.更多还原