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    • 3. 发明授权
    • Oil dispersions of nAChR binding neonicotinoids
    • nAChR结合新烟碱类的油分散体
    • US08293733B2
    • 2012-10-23
    • US13254785
    • 2010-03-04
    • Victor Casaña GinerMiguel Gimeno SierraBárbara Gimeno Sierra
    • Victor Casaña GinerMiguel Gimeno SierraBárbara Gimeno Sierra
    • A61K31/535A61K31/435A61K31/44A61K31/34A61K31/426A01N43/08A01N43/78
    • A01N51/00A01N43/40A01N43/78A01N47/40A01N25/04A01N25/30A01N47/34A01N53/00A01N2300/00
    • Selective insect neonicotinoids is a class of pesticide active ingredients that share some characteristics in their chemical structures and bind to the nAChR acetylcholine receptors. Formulation of such compounds in oil suspension or oil dispersion is challenging due to their electrostatic interactions of the heteroatoms in oily media, that lead to irreversible flocculation or diminished homogeneicity and bleeding of such oil dispersions. Imidacloprid, Thiamethoxam, Thiachloprid, Nitenpyram, Acetamiprid, Clothianidin and Dinetofuran and derivatives thereof with nAChR binding ability are successfully formulated in oil suspension with the use of certain copolymeric anionic fatty-acid based dispersants, sorbitan derivatives, ionic surfactants, other non-ionic surfactants and inorganic polyvalent cationic salt dispersed in the oil. The formulations this way produced show excellent storage stability properties regarding physiochemical parameters, including stability of the neonicotinoid active ingredient, reduced bleeding, and complete redispersibility. Further, they show excellent biological efficacy due to the reduced and homogeneous particle size below 2 μm when diluted—emulsified—in water.
    • 选择性昆虫新烟碱类是一类农药活性成分,在其化学结构中具有一些特征,并与nAChR乙酰胆碱受体结合。 这种化合物在油悬浮液或油分散体中的配制是具有挑战性的,因为它们在油性介质中的杂原子的静电相互作用,导致不可逆的絮凝或这种油分散体的均匀性下降和渗色。 使用某些共聚阴离子脂肪酸基分散剂,脱水山梨糖醇衍生物,离子表面活性剂,其他非离子表面活性剂,成功配制了具有nAChR结合能力的吡虫啉,噻虫嗪,噻虫啉,Nitenpyram,Acetamiprid,Clothianidin和Dinetofuran及其衍生物 和分散在油中的无机多价阳离子盐。 通过这种方式制备的制剂显示了关于生理化学参数的优异的储存稳定性,包括新烟碱活性成分的稳定性,降低的出血和完全的再分散性。 此外,当稀释乳化在水中时,由于减小且均匀的粒径小于2μm,它们显示出优异的生物学效力。