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1. 发明申请

WO2008006712A3 PREPARATION OF NANODISPERSIONS 审中-公开
标题翻译：纳米尺度的制备
公开(公告)号：WO2008006712A3
公开(公告)日：2009-02-26
申请号：PCT/EP2007056560
申请日：2007-06-29
申请人： UNILEVER PLC , UNILEVER NV , ANGUS DORIS , DUNCALF DAVID JOHN , ELPHICK ANDREW JAMES , FOSTER ALISON JAYNE , LONG JAMES , RANNARD STEVEN PAUL , WANG DONG
发明人： ANGUS DORIS , DUNCALF DAVID JOHN , ELPHICK ANDREW JAMES , FOSTER ALISON JAYNE , LONG JAMES , RANNARD STEVEN PAUL , WANG DONG
IPC分类号： A61K9/16 , A01N31/16 , A01N37/50 , A01N43/653 , A01N53/00 , A23L27/00
CPC分类号： A61K9/1617 , A01N25/04 , A61K9/10 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/19 , A61K31/167 , A01N43/54 , A01N53/00 , A01N31/16 , A01N37/18
摘要： The invention provides process for making contra-soluble nano-dispersions of at most sparingly-soluble materials in a soluble carrier material comprising the steps of: (i) providing a single phase mixture of: a) a solvent or a mixture of miscible solvents, b) at least one carrier material soluble in solvent (a), said carrier material being also contra-soluble to payload material (c) and solid at ambient temperature, c) at least one a payload material which is soluble in solvent (a), and, (ii) drying the mixture to remove solvent (a) and thereby obtain the carrier material (b) in solid form with payload (c) dispersed therein as nanoparticles.
摘要翻译：本发明提供了在可溶性载体材料中制备至多微溶性材料的可溶性纳米分散体的方法，其包括以下步骤：（i）提供单相混合物：a）溶剂或可混溶溶剂的混合物， b）可溶于溶剂（a）的至少一种载体材料，所述载体材料在环境温度下也可溶于有效载荷材料（c）和固体，c）至少一种可溶于溶剂（a）的有效载荷材料，，和（ii）干燥混合物以除去溶剂（a），从而获得固体形式的载体材料（b），其中有效载荷（c）作为纳米颗粒分散在其中。

2. 发明申请

WO2010023066A3 IMPROVEMENTS RELATING TO PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：与药物组合物有关的改进
公开(公告)号：WO2010023066A3
公开(公告)日：2010-08-05
申请号：PCT/EP2009060007
申请日：2009-08-03
申请人： UNILEVER PLC , UNILEVER NV , ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , RANNARD STEVEN PAUL , WANG DONG
发明人： ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , RANNARD STEVEN PAUL , WANG DONG
IPC分类号： A61K9/16
CPC分类号： A61K9/1694 , A61K9/1652 , A61K9/5161
摘要： The present invention provides a substantially solvent-free nano-dispersion of an active in a carrier, wherein the carrier comprises an enteric carrier soluble at intestinal pH, but insoluble at stomach pH, and wherein the enteric carrier comprises at least 50% by weight of the nano-dispersion; and processes for the preparation of a substantially solvent-free nano-dispersion of an active in a carrier.
摘要翻译：本发明提供了基本上无溶剂的载体中活性剂的纳米分散体，其中所述载体包含可溶于肠pH的肠溶载体，但在胃pH下不溶，并且其中所述肠载体包含至少50重量％的纳米分散体; 以及用于制备载体中的活性物质的基本上无溶剂的纳米分散体的方法。

3. 发明申请

WO2010020518A3 IMPROVEMENTS RELATING TO NANODISPERSE COMPOSITIONS 审中-公开
标题翻译：有关纳米分散组合物的改进
公开(公告)号：WO2010020518A3
公开(公告)日：2010-10-14
申请号：PCT/EP2009059546
申请日：2009-07-24
申请人： UNILEVER PLC , UNILEVER NV , ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , RANNARD STEVEN PAUL , WANG DONG
发明人： ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , RANNARD STEVEN PAUL , WANG DONG
IPC分类号： A61K9/16 , A61K31/00
CPC分类号： A61K9/1694 , A61K9/1623 , A61K9/1635 , B01J2/04
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2011141721A2 COMPOSITIONS 审中-公开
标题翻译：组合物
公开(公告)号：WO2011141721A2
公开(公告)日：2011-11-17
申请号：PCT/GB2011000747
申请日：2011-05-13
申请人： IOTA NANOSOLUTIONS LTD , ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , COOPER ANDREW IAN , RANNARD STEVEN PAUL , WANG DONG , ZHANG HAIFEI
发明人： ANGUS DORIS , DUNCALF DAVID JOHN , FOSTER ALISON JAYNE , COOPER ANDREW IAN , RANNARD STEVEN PAUL , WANG DONG , ZHANG HAIFEI
IPC分类号： A61K9/00
CPC分类号： A61K9/006 , A61K9/0056 , A61K9/10 , A61K9/19 , A61K9/7007
摘要： A method for the preparation of a composition comprising a water-soluble porous matrix having a water-insoluble active ingredient dispersed throughout the matrix in the form of nano-particles having a z-average particle size of up to 1000 nm, which process comprises the steps of: (i) providing a preformed porous, water-soluble matrix; (ii) treating the matrix with a solution of the water-insoluble active ingredient in a solvent, wherein the solvent is a non-aqueous solvent in which the matrix is insoluble, whereby the solution permeates through the pores of the matrix; and (iii) removing the solvent by evaporation, thereby leaving the water-insoluble active ingredient in nano- disperse form throughout the matrix. Also disclosed is an identical method using a water-insoluble porous matrix and a water-soluble active ingredient.
摘要翻译：一种制备包含水溶性多孔基质的组合物的方法，所述多孔基质具有分散在整个基质中的水不溶性活性成分，其形式为z-平均粒度高达1000nm的纳米粒子，该方法包括步骤：（i）提供预制的多孔，水溶性基质; （ii）用水不溶性活性成分在溶剂中处理该基质，其中溶剂是基质不溶于其中的非水溶剂，由此溶液渗透通过基质的孔; 和（iii）通过蒸发除去溶剂，从而使整个基质中纳米分散形式的水不溶性活性成分留下。还公开了使用水不溶性多孔基质和水溶性活性成分的相同方法。

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