功夫菊酯固体分散体的制备及性能分析  

Preparation and properties of cyhalothrin solid dispersions

作　　者：卢瑞 莫宇星 曹莉慧 杨华[2] 

机构地区：[1]广西田园生化股份有限公司,南宁530007 [2]广西大学化学化工学院,南宁530005

出　　处：《南方农业学报》2016年第2期234-240,共7页Journal of Southern Agriculture

基　　金：广西科学研究与技术开发计划项目(桂科攻1598007-28)

摘　　要：【目的】制备功夫菊酯不同载体固体分散体,并研究其对功夫菊酯的增溶效果及溶出特性,为开发功夫菊酯新剂型提供参考。【方法】选择聚乙二醇6000(PEG-6000)、聚乙二醇20000(PEG-20000)和聚乙烯吡咯烷酮K30(PVP-K30)作为载体,采用溶剂—熔融法和溶剂法制备功夫菊酯固体分散体;采用紫外可见分光光度法测定功夫菊酯固体分散体的溶解度及溶出度。利用紫外光谱和红外光谱、扫描电镜等表征手段对固体分散体的结构特征进行分析,并在玉米上采用内吸法测定功夫菊酯固体分散体对玉米螟的生物活性。【结果】固体分散体中功夫菊酯的溶解度比功夫菊酯原药及相同质量比物理混合物的溶解度有明显提高,其中以PVP-K30的增溶效果最好,功夫菊酯的溶解度由0.0050 mg/L增加到28.1776 mg/L。物相分析结果表明,药物以非晶型高度分散在载体中。毒力测定结果表明,固体分散体的杀虫活性超过2.5%功夫菊酯微乳液,表现出一定的杀虫效果。【结论】以PEG-6000、PEG-20000和PVP-K30为载体制备的功夫菊酯固体分散体能明显提高功夫菊酯的溶解度,进而提高杀虫效果,可在农业生产中推广应用。【Objective】The present experiment was conducted to prepare cyhalothrin solid dispersions, and investigate their solubilization effect on cyhalothrin and their dissolution characteristics of cyhalothrin. 【Method 】With polyethylene glycol 6000（PEG-6000）, polyethylene glycol 20000（PEG-20000） and polyvinylpyrrolidone K30（PVP-K30） as carriers,the cyhalothrin solid dispersions were prepared by using solvent-melting and solvent methods, respectively. The UV spectrometry methods were used to determinate solubility and dissolution rate of cyhalothrin solid dispersions. And UV spectrum, FTIR and SEM methods were used to characterize structures of solid dispersions. Finally, the absorption method was used to determinate biological activity of solid dispersions against corn borer. 【Result】The solubility of cyhalothrin in solid dispersions was significantly increased, compared with those of cyhalothrin and physical mixture of cyhalothrin and carrier with same mass ratio, particularly, PVP-K30 had best solubilization effect on cyhalothrin, thus the solubility of cyhalothrin was increased from 0.0050 mg/L to 28.1776 mg/L. Furthermore, the results of phase analysis indicated that cyhalothrin was highly dispersed in carriers as amorphous state. The results of toxicity test showed that the solid dispersions had some insecticidal effect, and their insecticidal activity was higher than 2.5% cyhalothrin microemulsion. 【Conclusion】The solubility of cyhalothrin can be greatly improved by cyhalothrin solid dispersions with PEG-6000, PEG-20000 and PVP-K30 as its carriers. Furthermore, these cyhalothrin solid dispersions have more insecticidal effect, and should be applied in actual agricultural production.

关 键 词：功夫菊酯 固体分散体 聚乙二醇 聚乙烯吡咯烷酮 溶解度 

分 类 号：S482.3[农业科学—农药学]