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    Method for crystallization of a weakly acidic and/or weakly basic compound
    1.
    发明授权
    Method for crystallization of a weakly acidic and/or weakly basic compound 有权
    弱酸性和/或弱碱性化合物的结晶方法

    公开(公告)号：US07381265B2

    公开(公告)日：2008-06-03

    申请号：US11511936

    申请日：2006-08-28

    申请人： Lei Du-Cuny ,  Manfred Kansy ,  Jörg Huwyler

    发明人： Lei Du-Cuny ,  Manfred Kansy ,  Jörg Huwyler

    IPC分类号： H01L21/322

    CPC分类号： B01D9/0054

    摘要： A method for crystallization of a weakly acidic and/or weakly basic compound having an uncharged form and at least one charged form comprises the steps of: a) providing a solution of said compound in a solvent having an initial pH-value and an initial total concentration of said compound, said initial pH-value being chosen such that the compound is present in said solution predominantly in said charged form, said initial total concentration being chosen larger than the intrinsic solubility of said uncharged form; b) gradually changing the pH-value of said solution in a direction that leads to a decrease of said compound's solubility until reaching a predetermined target pH-value at which said solution is in a substantially saturated state and the concentration of said uncharged form is substantially equal to said intrinsic solubility thereof; and c) maintaining said solution in a substantially saturated state while allowing formation of crystals of said compound.

    摘要翻译： 用于结晶具有不带电荷形式和至少一种带电形式的弱酸性和/或弱碱性化合物的方法包括以下步骤：a）将所述化合物的溶液提供在具有初始pH值和初始总量的溶剂中 所述化合物的浓度，所述初始pH值被选择为使得化合物主要以所述带电形式存在于所述溶液中，所述初始总浓度选择为大于所述不带电形式的固有溶解度; b）在导致所述化合物溶解度降低的方向上逐渐改变所述溶液的pH值，直到达到所述溶液处于基本饱和状态的预定目标pH值，并且所述不带电形式的浓度基本上 等于其内在溶解度; 和c）将所述溶液保持在基本饱和状态，同时允许所述化合物的晶体形成。

    Method for crystallization of a weakly acidic and/or weakly basic compound
    2.
    发明申请
    Method for crystallization of a weakly acidic and/or weakly basic compound 有权
    弱酸性和/或弱碱性化合物的结晶方法

    公开(公告)号：US20070044705A1

    公开(公告)日：2007-03-01

    申请号：US11511936

    申请日：2006-08-28

    申请人： Lei Du-Cuny ,  Manfred Kansy ,  Jörg Huwyler

    发明人： Lei Du-Cuny ,  Manfred Kansy ,  Jörg Huwyler

    IPC分类号： H01L21/322

    CPC分类号： B01D9/0054

    摘要： A method for crystallization of a weakly acidic and/or weakly basic compound having an uncharged form and at least one charged form comprises the steps of: a) providing a solution of said compound in a solvent having an initial pH-value and an initial total concentration of said compound, said initial pH-value being chosen such that the compound is present in said solution predominantly in said charged form, said initial total concentration being chosen larger than the intrinsic solubility of said uncharged form; b) gradually changing the pH-value of said solution in a direction that leads to a decrease of said compound's solubility until reaching a predetermined target pH-value at which said solution is in a substantially saturated state and the concentration of said uncharged form is substantially equal to said intrinsic solubility thereof; and c) maintaining said solution in a substantially saturated state while allowing formation of crystals of said compound.

    摘要翻译： 用于结晶具有不带电荷形式和至少一种带电形式的弱酸性和/或弱碱性化合物的方法包括以下步骤：a）将所述化合物的溶液提供在具有初始pH值和初始总量的溶剂中 所述化合物的浓度，所述初始pH值被选择为使得化合物主要以所述带电形式存在于所述溶液中，所述初始总浓度选择为大于所述不带电形式的固有溶解度; b）在导致所述化合物溶解度降低的方向上逐渐改变所述溶液的pH值，直到达到所述溶液处于基本饱和状态的预定目标pH值，并且所述不带电形式的浓度基本上 等于其内在溶解度; 和c）将所述溶液保持在基本饱和状态，同时允许所述化合物的晶体形成。

    Determination of high lipophilicity values
    4.
    发明授权
    Determination of high lipophilicity values 有权
    高亲脂性值的测定

    公开(公告)号：US07527975B2

    公开(公告)日：2009-05-05

    申请号：US11375903

    申请日：2006-03-15

    申请人： Holger Fischer ,  Manfred Kansy ,  Bjoern Wagner

    发明人： Holger Fischer ,  Manfred Kansy ,  Bjoern Wagner

    IPC分类号： G01N33/92

    CPC分类号： G01N33/92

    摘要： The present invention relates to a novel method for determining the lipophilicity of a compound of interest comprising a) providing a layer, b) impregnating said layer with a solvent A, c) applying a dissolved compound of interest on the impregnated layer, d) adding a solvent B, e) removing the solvent B after the distribution equilibrium has been reached, and f) determining the quantity of the compound of interest in at least one of the solvent phases.

    摘要翻译： 本发明涉及一种用于测定感兴趣的化合物的亲油性的新方法，其包括a）提供一层，b）用溶剂A浸渍所述层，c）将所需的溶解化合物施加到浸渍层上，d）将 溶剂B，e）在达到分配平衡之后除去溶剂B，以及f）确定至少一个溶剂相中的目标化合物的量。

    Method for assessing absorption properties of low solubility compounds
    6.
    发明授权
    Method for assessing absorption properties of low solubility compounds 有权
    评估低溶解度化合物吸收性能的方法

    公开(公告)号：US08175815B2

    公开(公告)日：2012-05-08

    申请号：US12224449

    申请日：2007-02-27

    申请人： Alex Avdeef ,  Manfred Kansy

    发明人： Alex Avdeef ,  Manfred Kansy

    IPC分类号： G01N31/00 ,  C08B11/20

    CPC分类号： G01N33/15

    摘要： The invention deals with a method for the assessment of the effect of excipients, pH and combinations thereof on the predicted absorption properties of low solubility compounds, comprising the step of assessing a change in a flux function for a combination of a low solubility compound and an excipient at at least one predefined pH value. The method allows a fast, accurate, and economic evaluation of an excipient being capable of optimizing the absorption of drug molecules, i.e. low solubility compounds. Furthermore, animal experiments can be excluded and use of compounds can be reduced in such evaluation. Thus, screening for future formulation efficacy (pH and excipient effects on solubility and permeability) of drug candidates can be justified, since the method is fast, compound-sparing, cost-effective, and reasonably accurate.

    摘要翻译： 本发明涉及评估赋形剂，pH及其组合对低溶解度化合物预测吸收性能的影响的方法，包括评估低溶解度化合物和 赋形剂在至少一个预定的pH值。 该方法允许对能够优化药物分子（即低溶解度化合物）的吸收的赋形剂的快速，准确和经济的评价。 此外，可以排除动物实验，并且可以减少化合物的使用。 因此，由于该方法快速，复合，节省成本，并且相当准确，筛选候选药物的未来制剂功效（pH和赋形剂对溶解性和渗透性的影响）是合理的。

    Cuvette arrays
    7.
    发明申请
    Cuvette arrays 审中-公开
    比色杯阵列

    公开(公告)号：US20050249640A1

    公开(公告)日：2005-11-10

    申请号：US11088049

    申请日：2005-03-23

    申请人： Manfred Kansy ,  Hansjorg Tschirky ,  Werner Schneider ,  Heinrich Buttgen ,  Tilo Callenbach ,  Karl Mazenauer

    发明人： Manfred Kansy ,  Hansjorg Tschirky ,  Werner Schneider ,  Heinrich Buttgen ,  Tilo Callenbach ,  Karl Mazenauer

    IPC分类号： G01N1/10 ,  B01L3/00 ,  G01N21/03 ,  G01N35/00 ,  G01N35/02

    CPC分类号： B01L3/50855 ,  B01L3/50255 ,  B01L2200/025 ,  B01L2200/028 ,  B01L2300/0829 ,  G01N2021/0321 ,  G01N2021/0357

    摘要： An integrally built, linear array of cuvettes is made of a plastic material. This array comprises a plurality of cuvettes arranged along a straight line in an array, each cuvette in the array having the same shape and dimensions, and neighboring cuvettes being connected to each other by a single web. Each of the single webs has a curved shape. The symmetry axis (Y-Y) of every cuvette forming part of said array of cuvettes lies substantially in one and the same plane (A-A) which is a symmetry plane of said cuvette array. The upper part of at least one intermediate cuvette which is located between a first cuvette located at one end of the cuvette array and a second cuvette located at the opposite end of the cuvette array is connected by a first single web to the upper part of a neighboring cuvette lying on one side of said intermediate cuvette and is connected by a second single web to the upper part of a neighboring cuvette lying on the opposite side of said intermediate cuvette.

    摘要翻译： 整体建造的线性排列的比色杯由塑料材料制成。 该阵列包括沿着阵列的直线布置的多个比色皿，阵列中的每个比色皿具有相同的形状和尺寸，并且相邻的比色杯通过单个纤维网彼此连接。 每个单个腹板具有弯曲的形状。 形成所述比色皿阵列的一部分的每个比色皿的对称轴（Y-Y）基本上位于作为所述比色皿阵列的对称平面的同一平面（A-A）中。 位于比色皿阵列的一端的第一比色皿和位于比色皿阵列的相对端的第二比色杯之间的至少一个中间比色皿的上部通过第一单个纤维网连接到一个 相邻的比色杯位于所述中间试管的一侧，并且通过第二单个纤维网连接到位于所述中间试管的相对侧上的邻近比色皿的上部。

    Method for Assessing Absorption Properties of Low Solubility Compounds
    8.
    发明申请
    Method for Assessing Absorption Properties of Low Solubility Compounds 有权
    评估低溶解度化合物吸收性能的方法

    公开(公告)号：US20090187365A1

    公开(公告)日：2009-07-23

    申请号：US12224449

    申请日：2007-02-27

    申请人： Alex Avdeef ,  Manfred Kansy

    发明人： Alex Avdeef ,  Manfred Kansy

    IPC分类号： G01D18/00

    CPC分类号： G01N33/15

    摘要： The invention deals with a method for the assessment of the effect of excipients, pH and combinations thereof on the predicted absorption properties of low solubility compounds, comprising the step of assessing a change in a flux function for a combination of a low solubility compound and an excipient at at least one predefined pH value. The method allows a fast, accurate, and economic evaluation of an excipient being capable of optimizing the absorption of drug molecules, i.e. low solubility compounds. Furthermore, animal experiments can be excluded and use of compounds can be reduced in such evaluation. Thus, screening for future formulation efficacy (pH and excipient effects on solubility and permeability) of drug candidates can be justified, since the method is fast, compound-sparing, cost-effective, and reasonably accurate.

    摘要翻译： 本发明涉及评估赋形剂，pH及其组合对低溶解度化合物预测吸收性能的影响的方法，包括评估低溶解度化合物和 赋形剂在至少一个预定的pH值。 该方法允许对能够优化药物分子（即低溶解度化合物）的吸收的赋形剂的快速，准确和经济的评价。 此外，可以排除动物实验，并且可以减少化合物的使用。 因此，由于该方法快速，复合，节省成本，并且相当准确，筛选候选药物的未来制剂功效（pH和赋形剂对溶解性和渗透性的影响）是合理的。

    Determination of high lipophilicity values
    9.
    发明申请
    Determination of high lipophilicity values 有权

    公开(公告)号：US20060211121A1

    公开(公告)日：2006-09-21

    申请号：US11375903

    申请日：2006-03-15

    申请人： Holger Fischer ,  Manfred Kansy ,  Bjoern Wagner

    发明人： Holger Fischer ,  Manfred Kansy ,  Bjoern Wagner

    IPC分类号： G01N33/92

    CPC分类号： G01N33/92

    摘要： The present invention relates to a novel method for determining the lipophilicity of a compound of interest comprising a) providing a layer, b) impregnating said layer with a solvent A, c) applying a dissolved compound of interest on the impregnated layer, d) adding a solvent B, e) removing the solvent B after the distribution equilibrium has been reached, and f) determining the quantity of the compound of interest in at least one of the solvent phases.