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    • 6. 发明申请
    • IMPROVEMENTS RELATING TO NANODISPERSE COMPOSITIONS
    • 关于纳米复合材料的改进
    • WO2010020518A2
    • 2010-02-25
    • PCT/EP2009/059546
    • 2009-07-24
    • UNILEVER PLCUNILEVER N.V.ANGUS, DorisDUNCALF, David JohnFOSTER, Alison JayneRANNARD, Steven PaulWANG, Dong
    • ANGUS, DorisDUNCALF, David JohnFOSTER, Alison JayneRANNARD, Steven PaulWANG, Dong
    • A61K9/1694A61K9/1623A61K9/1635B01J2/04
    • A process for the production of a soluble composition comprising a water- insoluble active which comprises either the steps of: a) providing a liquid mixture comprising: i) a dissolved water-insoluble active, ii) a dissolved water-soluble carrier, iii) a solvent for each of the active and the carrier, and b) spray-granulating the mixture to remove the, or each, solvent and obtain a substantially solvent-free nano-dispersion of the water-insoluble active in the carrier said water-insoluble active being in nano-particles having a size range of 999-20 nm; or, the steps of: a) providing a substantially solvent-free powder comprising a water-insoluble active dispersed in a water soluble carrier, said water-insoluble active being in nano-particles having a size range of 999-20 nm, and, b) spray-granulating the powder to obtain larger and denser particles. The invention also relates to solvent-free, granular products with a particle size in the range 20 microns to 10mm and a bulk-density of greater than 0.4g/cm3 comprising a water-soluble carrier material, the carrier material having dispersed therein a water-insoluble active, wherein on addition of water the carrier dissolves to form an aqueous dispersion of the active with a peak (z-average) particle size of below 800nm, preferably below 500nm and more preferably below 200nm. The invention also relates to an analogous "reverse" process in which the active is water soluble and the carrier is oil soluble.
    • 一种用于生产包含水不溶性活性物质的可溶性组合物的方法,其包括以下步骤:a)提供液体混合物,其包含:i)溶解的水不溶性活性物质,ii)溶解的水溶性载体,iii) 用于活性物质和载体中的每一种的溶剂,以及b)将混合物喷雾造粒以除去溶剂或每种溶剂,并获得载体中不溶于水的活性物质的基本上无溶剂的纳米分散体,所述水不溶性 活性纳米颗粒的尺寸范围为999〜20nm; 或者步骤:a)提供基本上无溶剂的粉末,其包含分散在水溶性载体中的不溶于水的活性物质,所述水不溶性活性物质的尺寸范围为999-20nm, b)将粉末喷雾造粒以获得更大和更致密的颗粒。 本发明还涉及粒径在20微米至10mm范围内的无溶剂颗粒状产品,其中堆积密度大于0.4g / cm3,包括水溶性载体材料,载体材料中分散有水 其中在加入水时,载体溶解以形成具有低于800nm,优选低于500nm,更优选低于200nm的峰(z-平均)粒度的活性物质的水分散体。 本发明还涉及类似的“反向”方法,其中活性物质是水溶性的并且载体是油溶性的。