曹莉慧 王立升 杨华

摘要：制备阿维菌素不同载体固体分散体，并研究其对阿维菌素的增溶情况及溶出特性。 选择聚乙二醇（PEG 6000、PEG 20000）、聚乙烯吡咯烷酮 K30（PVP）作为载体，用熔融法和溶剂法制备了阿维菌素固体分散体；采用紫外可见分光光度法测定阿维菌素固体分散体的溶解度以及缓释溶出度。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研究。结果表明，固体分散体中阿维菌素的溶解度比阿维菌素及相同质量比的物理混合物的溶解度有明显提高，其中PVP-K30的增溶效果最好；固体分散体表现出了良好的缓释效果。物相分析结果表明，药物以非晶型高度分散在载体中。以PEG 6000、PEG 20000、PVP-K30为载体制备的阿维菌素固体分散体能显著提高阿维菌素的溶解度，且缓释效果良好，具有实际应用价值。

关键词：阿维菌素； 固体分散体； 缓释； 聚乙二醇； 聚乙烯吡咯烷酮； 溶解度

中图分类号：S482；TQ45 文献标识码：A 文章编号：0439-8114（2016）05-1163-05

DOI：10.14088/j.cnki.issn0439-8114.2016.05.019

The Preparation and Properties of Avermectin Release Solid Dispersion

CAO Li-hui，WANG Li-sheng，YANG Hua

（College of Chemistry and Chemical Engineering， Guangxi University， Nanning 530004，China）

Abstract： The solid dispersions of avermectin was prepared， and the enhancement of solubility and their dissolution characteristics of avermectin were measured. The solid dispersions were obtained by using the melted and dissolved methods with PEG6000， PEG20000， PVP-K30 as carriers respectively， the UV spectrometry method for determination of solubility and controlled release of avermectin was established. The structure of solid dispersions was characterized by UV spectrum， FTIR， SEM. The results showed that the solubility of avermectin in solid dispersions had significantly increased than avermectin and the same quality of physical mixture， among them PVP-K30 with the best solubilization effect； These solid dispersions had better sustained release effect. The results from the phase analysis indicated that avermectin existed in carriers as amorphous state. The solubility of avermectin could be greatly improved by the solid dispersions with PEG6000， PEG20000， PVP-K30 as its carriers， and solid dispersions exhibited excellent sustained release characteristics with the actual applied value.

Key words： solid dispersion； sustained release； polyethylene glycol； polyvinylpyrrolidone； solubility

阿維菌素（Avermectin）是一种高效生物杀虫、杀螨、杀线虫剂，防治谱十分广泛，常用于防治农业害虫和牲畜寄生虫。因其具有高效、低毒、结构新颖等优点，在中国的害虫防治体系中占有重要地位，被农业部推荐为无公害农药[1]。阿维菌素对昆虫和螨类具有触杀和胃毒作用，只有微弱的熏蒸作用，并且无杀卵、无内吸作用。因此如何提高阿维菌素的内吸性成为近年来研究的热点问题[2，3]。针对无内吸性原药，通过物理或是化学方法，以增加药物水溶性进而提高内吸性，达到增加药效的目的。……