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    • 3. 发明申请
    • IMPROVEMENTS RELATING TO ANTI-PARASITIC COMPOSITIONS
    • 有关抗菌成分的改进
    • WO2008006713A2
    • 2008-01-17
    • PCT/EP2007056561
    • 2007-06-29
    • UNILEVER PLCUNILEVER NVDUNCALF DAVID JOHNESSA ASHA HASSANFOSTER ALISON JAYNELONG JAMESRANNARD STEVEN PAULWANG DONG
    • DUNCALF DAVID JOHNESSA ASHA HASSANFOSTER ALISON JAYNELONG JAMESRANNARD STEVEN PAULWANG DONG
    • A61K9/16A23L27/00A61K31/496
    • A61K9/1617A01N25/04A61K9/10A61K9/1635A61K9/1641A61K9/1652A61K9/19A61K31/167A01N43/54A01N53/00A01N31/16A01N37/18
    • The present invention relates to nanodisperse antiparasitcs and provides a composition comprising at least one water insoluble anti-parasitic drug and a water-soluble carrier material, wherein the water-insoluble anti-parasitic drug (preferably an Artemisinin-type drug or a quinine type drug) is dispersed through the carrier material in nano-disperse form having a peak diameter of the nano-disperse form below 1000nm. The invention further provides an aqueous dispersion of a water insoluble anti-parasitic drug and a water-soluble carrier material, wherein the anti-parasitic drug is in nano-disperse form having a peak diameter of the nano- disperse form below 1000nm, the invention further subsists in a process for preparing an anti-parasitic composition comprising a water insoluble anti-parasitc agent and a water-soluble carrier, which comprises the steps of either: a) providing an emulsion comprising a solution of the anti-parasitic agent in a water-immiscible solvent for the same, and an aqueous solution of the carrier, or providing a mixture comprising at least one non-aqueous solvent optional water a water-soluble carrier material soluble in the mixture and a water-insoluble anti- parasitic agent soluble in the mixture, and, b) drying the emulsion (preferably by spray drying) to remove water and the water-immiscible solvent to obtain a substantially solvent-free nano-dispersion of the anti-parasitic agent in the carrier.
    • 本发明涉及纳米分散抗寄生虫剂,并提供包含至少一种水不溶性抗寄生虫药物和水溶性载体材料的组合物,其中所述水不溶性抗寄生虫药物(优选青蒿素型药物或奎宁型药物 )以纳米分散形式的峰值直径低于1000nm的纳米分散形式分散在载体材料中。 本发明还提供了水不溶性抗寄生虫药物和水溶性载体材料的水性分散体,其中抗寄生虫药物为纳米分散形式,其纳米分散体形式的峰值直径低于1000nm,本发明 进一步存在于制备包含水不溶性抗寄生虫剂和水溶性载体的抗寄生物组合物的方法中,其包括以下步骤:a)提供包含抗寄生虫剂溶液的乳液 或与提供包含至少一种非水溶剂任选的水的混合物,可溶于该混合物的水溶性载体材料和可溶于水的不溶性抗寄生剂溶液 在混合物中,并且b)干燥乳液(优选通过喷雾干燥)以除去水和与水不混溶的溶剂,以获得基本上无溶剂的抗吸附剂的纳米分散体 tic代理在承运人。
    • 8. 发明申请
    • IMPROVEMENTS RELATING TO NANODISPERSE COMPOSITIONS
    • 有关纳米分散组合物的改进
    • WO2010020518A3
    • 2010-10-14
    • PCT/EP2009059546
    • 2009-07-24
    • UNILEVER PLCUNILEVER NVANGUS DORISDUNCALF DAVID JOHNFOSTER ALISON JAYNERANNARD STEVEN PAULWANG DONG
    • ANGUS DORISDUNCALF DAVID JOHNFOSTER ALISON JAYNERANNARD STEVEN PAULWANG DONG
    • A61K9/16A61K31/00
    • 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.
    • 一种生产包含水不溶性活性物质的可溶性组合物的方法,该方法包括以下步骤:a)提供液体混合物,该液体混合物包含: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,和b)喷雾造粒混合物以除去所述溶剂或每种溶剂,并获得所述水不溶性活性物质在所述载体中的基本上无溶剂的纳米分散体,所述水不溶性物质 活性纳米颗粒的尺寸范围为999-20nm; 或以下步骤: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水不溶性活性物质,所述水不溶性活性物质为纳米颗粒,其尺寸范围为999-20nm, b)将粉末喷雾造粒以获得更大和更致密的颗粒。 本发明还涉及包含水溶性载体材料的无溶剂颗粒产品,其颗粒尺寸为20微米至10毫米,堆密度大于0.4克/厘米3,所述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并且更优选低于200nm的峰(z-平均)粒径的活性物质的含水分散体。 本发明还涉及一种类似的“反向”方法,其中活性成分是水溶性的而载体是油溶性的。