Sustained-release microsphere formulation containing an agrochemical by polyurethane polymerization during an agitation granulation process.
Sustained-release microsphere formulation containing an agrochemical by polyurethane polymerization during an agitation granulation process.
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DOI：
10.1016/j.ijpharm.2016.05.061
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发表时间：
2016-07
影响因子：
5.8
通讯作者：
T. Terada;M. Tagami;T. Ohtsubo;Y. Iwao;Shuji Noguchi;S. Itai
中科院分区：
文献类型：
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作者：
T. Terada;M. Tagami;T. Ohtsubo;Y. Iwao;Shuji Noguchi;S. Itai
在高速混合装置中，以多元醇和异氰酸酯为原料，通过凝聚过程合成聚氨酯（PU），研究了一种无溶剂微胶囊化新方法。以新烟碱类杀虫剂噻虫胺（Clothianidin， CTD）作为模型化合物，对多种害虫均有较好的防治效果。包覆PU （CTD微球）的微胶囊样品中位直径<75 μm，具有缓释性能。采用同步加速器x射线计算机断层扫描测量对CTD微球进行了分析。多芯CTD和其他固体赋形剂分散在PU中。CTD释放后，虽然微球中出现了空洞，但微球的球形保持稳定，结构没有发生变化。实验释放数据与基于球形整体分散体药物释放的Baker-Lonsdale模型高度一致，与计算机断层扫描测量结果一致。
In this report, a new solventless microencapsulation method by synthesizing polyurethane (PU) from polyol and isocyanate during an agglomeration process in a high-speed mixing apparatus was developed. Clothianidin (CTD), which is a neonicotinoid insecticide and highly effective against a wide variety of insect pests, was used as the model compound. The microencapsulated samples covered with PU (CTD microspheres) had a median diameter of <75 μm and sustained-release properties. The CTD microspheres were analyzed by synchrotron X-ray computed tomography measurements. Multiple cores of CTD and other solid excipient were dispersed in PU. Although voids appeared in the CTD microspheres after CTD release, the spherical shape of the microspheres remained stable and no change in its framework was observed. The experimental release data were highly consistent with the Baker–Lonsdale model derived from drug release of spherical monolithic dispersions and consistent with the computed tomography measurements.