公开(公告)号：US20060198893A1

公开(公告)日：2006-09-07

申请号：US10543545

申请日：2004-02-02

申请人： Lennart Lindfors

发明人： Lennart Lindfors

IPC分类号： A61K31/454 ,  A61K31/4015 ,  A61K31/401 ,  A61K9/14

CPC分类号： C07D207/416 ,  A61K9/145

摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a pyrrole carboxamide compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions prepared by the process, solid particles prepared by the process and use of such particles.

摘要翻译： 一种在水性介质中制备固体颗粒的稳定分散体的方法，包括将（a）包含基本上不溶于水的物质（其是式I的吡咯甲酰胺化合物），水混溶性有机溶剂和 抑制剂与（b）包含水和任选的稳定剂的水相，从而沉淀包含抑制剂和基本上不溶于水的物质的固体颗粒; 并任选地除去水混溶性有机溶剂; 其中所述抑制剂是如说明书中定义的非聚合疏水性有机化合物。 还要求的是通过该方法制备的稳定分散体，通过该方法制备的固体颗粒和使用这种颗粒。

公开(公告)号：US06673365B1

公开(公告)日：2004-01-06

申请号：US08894615

申请日：1997-08-22

申请人： Jan-Erik Löfroth ,  Lennart Lindfors ,  Anna-Lena Ungell

发明人： Jan-Erik Löfroth ,  Lennart Lindfors ,  Anna-Lena Ungell

IPC分类号： A61K948

CPC分类号： A61K9/4858 ,  A61K9/1274 ,  A61K38/55 ,  Y10S514/946

摘要： A new pharmaceutical formulation comprising the thrombin inhibitor HOOC—CH2—(R)-Cgl-Aze-Pab in combination with medium chain glycerides, a process for the preparation of such a pharmaceutical formulation, the use of a such formulation in the treatment of thromboembolism as well as a method of treating a patient in need of such a treatment by using said formulation.

摘要翻译： 一种新的药物制剂，其包含与中链甘油酯组合的凝血酶抑制剂HOOC-CH2-（R）-Cgl-Aze-Pab，制备这种药物制剂的方法，使用这种制剂治疗血栓栓塞 以及通过使用所述制剂治疗需要这样治疗的患者的方法。

公开(公告)号：US20060134146A1

公开(公告)日：2006-06-22

申请号：US10543264

申请日：2004-02-02

申请人： Lennart Lindfors

发明人： Lennart Lindfors

IPC分类号： A61K31/4965 ,  A61K9/00

CPC分类号： A61K9/146 ,  A61K9/0019 ,  A61K9/5138 ,  A61K31/4965 ,  A61K31/497 ,  A61K47/14

摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a pyrazine compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions prepared by the process, solid particles prepared by the process and use of such particles.

摘要翻译： 一种在水性介质中制备固体颗粒的稳定分散体的方法，包括将（a）包含基本上不溶于水的物质（其是式I的吡嗪化合物），水混溶性有机溶剂和抑制剂 （b）包含水和任选的稳定剂的水相，从而沉淀包含抑制剂和基本上不溶于水的物质的固体颗粒; 并任选地除去水混溶性有机溶剂; 其中所述抑制剂是如说明书中定义的非聚合疏水性有机化合物。 还要求的是通过该方法制备的稳定分散体，通过该方法制备的固体颗粒和使用这种颗粒。

公开(公告)号：US07780989B2

公开(公告)日：2010-08-24

申请号：US10521617

申请日：2003-07-14

申请人： Tommy Urban Skantze ,  Per Lennart Lindfors ,  Sara Forssen

发明人： Tommy Urban Skantze ,  Per Lennart Lindfors ,  Sara Forssen

IPC分类号： A61K9/14

CPC分类号： A61K9/145 ,  A61K9/146 ,  A61K9/5138

摘要： A process for the preparation of a dispersion of crystalline nanoparticles in an aqueous medium is disclosed. Specifically, a first solution comprising a substantially water-insoluble substance in a water-miscible organic solvent is rapid mixed with an aqueous phase comprising water, and optionally a stabilizer, to form a dispersion of amorphous particles. The dispersion of amorphous particles is then sonicated for a sufficient period to form crystalline nanoparticles of the substantially water-insoluble substance. The process provides nanocrystals with a mean hydrodynamic diameter of less than 1 micron, particularly less than 300 nm, and is particularly useful for the preparation of nanocrystalline dispersions of pharmaceutical substances.

摘要翻译： 公开了一种在水性介质中制备结晶纳米颗粒的分散体的方法。 具体地说，将包含水可混溶的有机溶剂中基本上不溶于水的物质的第一溶液与包含水和任选的稳定剂的水相快速混合以形成无定形颗粒的分散体。 然后将无定形颗粒的分散体超声处理足够的时间以形成基本上不溶于水的物质的结晶纳米颗粒。 该方法提供的纳米晶体具有小于1微米，特别是小于300nm的平均流体动力学直径，并且特别可用于制备药物物质的纳米晶体分散体。

公开(公告)号：US20100068287A1

公开(公告)日：2010-03-18

申请号：US12524882

申请日：2008-02-08

申请人： Lennart Lindfors ,  Urban Skantze

发明人： Lennart Lindfors ,  Urban Skantze

IPC分类号： A61K9/14

CPC分类号： A61K9/10 ,  A61K9/14 ,  A61K9/1617 ,  A61K9/1688 ,  A61K47/20

摘要： The invention relates to a process for the preparation of a stable dispersion of particles, particularly sub-micron particles in an aqueous medium and to a stable dispersion of particles in a liquid medium. The sub-micron dispersion provided exhibit reduced or substantially no particle growth during storage and reduced crystallisation rate of the substantially water insoluble active compound.

摘要翻译： 本发明涉及一种在水性介质中制备颗粒，特别是亚微米颗粒的稳定分散体和颗粒在液体介质中的稳定分散体的方法。 所提供的亚微米分散体在储存期间显示出降低的或基本上没有颗粒生长，并且基本上不溶于水的活性化合物的结晶速率降低。

公开(公告)号：US20080214611A1

公开(公告)日：2008-09-04

申请号：US12028074

申请日：2008-02-08

申请人： Lennart LINDFORS ,  Urban Skantze

发明人： Lennart LINDFORS ,  Urban Skantze

IPC分类号： A61K31/4545 ,  A61K31/415 ,  A61K31/454

CPC分类号： A61K9/1075 ,  A61K9/14 ,  A61K31/445 ,  A61K47/14 ,  A61K47/24 ,  A61K47/32 ,  C07D231/14 ,  C07D233/90 ,  C07D471/04

摘要： The invention relates to a process for the preparation of a stable dispersion of amorphous particles of a CB1 modulator of sub-micron size in an aqueous medium.

摘要翻译： 本发明涉及在水性介质中制备亚微米尺寸的CB1调节剂的无定形颗粒的稳定分散体的方法。

公开(公告)号：US07473693B2

公开(公告)日：2009-01-06

申请号：US10543264

申请日：2004-02-02

申请人： Lennart Lindfors

发明人： Lennart Lindfors

IPC分类号： A61K31/495 ,  C07D253/06 ,  C07D401/00

CPC分类号： A61K9/146 ,  A61K9/0019 ,  A61K9/5138 ,  A61K31/4965 ,  A61K31/497 ,  A61K47/14

摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a pyrazine compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabilizer, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions prepared by the process, solid particles prepared by the process and use of such particles.

摘要翻译： 一种在水性介质中制备固体颗粒的稳定分散体的方法，包括将（a）包含基本上不溶于水的物质（其是式I的吡嗪化合物），水混溶性有机溶剂和抑制剂 （b）包含水和任选的稳定剂的水相，从而沉淀包含抑制剂和基本上不溶于水的物质的固体颗粒; 并任选地除去水混溶性有机溶剂; 其中所述抑制剂是如说明书中定义的非聚合疏水性有机化合物。 还要求的是通过该方法制备的稳定分散体，通过该方法制备的固体颗粒和使用这种颗粒。

公开(公告)号：US20080193534A1

公开(公告)日：2008-08-14

申请号：US12063438

申请日：2006-08-09

申请人： Lennart Lindfors ,  Urban Skantze

发明人： Lennart Lindfors ,  Urban Skantze

IPC分类号： A61K9/107

CPC分类号： A61K9/10 ,  A61K31/16 ,  A61K31/216 ,  A61K31/4422

摘要： The present invention relates to a process for the preparation of a stable dispersion of particles, particularly sub-micron particles in an aqueous medium and to a stable dispersion of particles in a liquid medium. The process provided comprises the following steps: 1) combining a) an emulsion comprising a continuous aqueous phase; an inhibitor; a stabiliser; with b) the substantially water-insoluble substance; and 2) increasing the temperature to vicinity of the melting temperature of the substantially water-insoluble substance. The sub-micron dispersion provided exhibit reduced or substantially no particle growth during storage and reduced crystallisation rate of the substantially water insoluble active compound.

摘要翻译： 本发明涉及一种在水性介质中制备颗粒，特别是亚微米颗粒的稳定分散体以及颗粒在液体介质中的稳定分散体的方法。 提供的方法包括以下步骤：1）组合a）包含连续水相的乳液; 抑制剂 稳定剂 与b）基本上不溶于水的物质; 和2）将温度升高到基本上不溶于水的物质的熔融温度附近。 所提供的亚微米分散体在储存期间显示出降低的或基本上没有颗粒生长，并且基本上不溶于水的活性化合物的结晶速率降低。

公开(公告)号：US20060141043A1

公开(公告)日：2006-06-29

申请号：US10543265

申请日：2004-02-02

申请人： Lennart Lindfors

发明人： Lennart Lindfors

IPC分类号： A61K31/426 ,  A61K9/14

CPC分类号： C07D417/04 ,  A61K9/145 ,  C07D277/56

摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a thiazole compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions prepared by the process, solid particles prepared by the process and use of such particles.

摘要翻译： 一种在水性介质中制备固体颗粒的稳定分散体的方法，包括将（a）包含基本上不溶于水的物质（其是式I的噻唑化合物），水混溶性有机溶剂和抑制剂 （b）包含水和任选的稳定剂的水相，从而沉淀包含抑制剂和基本上不溶于水的物质的固体颗粒; 并任选地除去水混溶性有机溶剂; 其中所述抑制剂是如说明书中定义的非聚合疏水性有机化合物。 还要求的是通过该方法制备的稳定分散体，通过该方法制备的固体颗粒和使用这种颗粒。