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    Complexes and their compositions
    1.
    发明授权
    Complexes and their compositions 失效
    复合物及其组成

    公开(公告)号：US06432928B1

    公开(公告)日：2002-08-13

    申请号：US08836390

    申请日：1997-08-01

    申请人： Lajos Szente ,  Jozsef Szejtli ,  Maria Vikmon nee Kiraly ,  Julia Szeman

    发明人： Lajos Szente ,  Jozsef Szejtli ,  Maria Vikmon nee Kiraly ,  Julia Szeman

    IPC分类号： A61K31715

    CPC分类号： B82Y5/00 ,  A61K47/6951 ,  C07D305/14

    摘要： This invention provides inclusion complexes of Taxol ((2aR-(a&agr;,4&bgr;,4&agr;&bgr;,6&bgr;,9&agr;(&agr;R*,&bgr;S*),11&agr;,12&agr;,12a&agr;,12b&agr;))-&bgr;-(benzoylamino)-&agr;-hydroxy-benzene-propanoic acid 6,12-b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclo-deca-(3,4)-benz-(1,2-b)-oxeth-9-yl-ester)) or Taxotere (butoxycarbonyl-10-desacetyl-N-debenzoyl-Taxol) or Taxus extracts formed with a cyclodextrin derivative and a co-solvent. This invention relates to pharmaceutical composition with increased water-solubility and stability. This invention provides the process for the preparation of an inclusion complex of Taxol or Taxotere or a brevifolia extract of Taxus formed with a cyclodextrin derivative and a co-solvent. This invention relates to pharmaceutical composition, containing as active ingredient an effective amount of an inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with a cyclodextrin derivative, preferably heptakis-2,6-0 dimethyl-&bgr;-cyclodextrin, random methylated &bgr;-cyclodextrin, succinylmethyl-&bgr;-cyclodextrin and a co-solvent together with usual filling, diluting and other auxiliaries generally used in the pharmaceutical industry.

    摘要翻译： 本发明提供了紫杉醇（（2aR-（aalpha，4beta，4alphabeta，6beta，9alpha（αR*，βS*），11alpha，12alpha，12aalpha，12bapha））-β-（苯甲酰氨基）-α-羟基 - 苯 - 丙酸6,12-b-双（乙酰氧基）-12-（苯甲酰氧基）-2a，3,4,4a，5,6,9,10,11,12,12a，12b-十二氢-4,11- 二羟基-4a，8,13,13-四甲基-5-氧代-7,11-亚甲基-1H-环十二烷基（3,4） - 苯并（1,2-b） - 氧代-9-基 - 酯））或泰索帝（丁氧羰基-10-脱乙酰基-N-脱苯甲酰基紫杉醇）或由环糊精衍生物和共溶剂形成的紫杉提取物。 本发明涉及具有增加的水溶性和稳定性的药物组合物。 本发明提供了制备紫杉醇或泰索帝的包合物的方法或由环糊精衍生物和助溶剂形成的紫杉属的短叶提取物的方法。 本发明涉及药物组合物，其含有有效量的紫杉醇或泰索帝或用环糊精衍生物形成的短叶紫杉提取物的有效量的混合物，优选七 - 2,6-0-二甲基-β-环糊精，随机甲基化β 环糊精，琥珀酰基甲基-β-环糊精和共溶剂，以及通常在制药工业中使用的填充，稀释和其它助剂。

    NOVEL BIOMATERIALS, THEIR PREPARATION AND USE
    3.
    发明申请
    NOVEL BIOMATERIALS, THEIR PREPARATION AND USE 审中-公开
    新生物材料，其制备和使用

    公开(公告)号：US20080299166A1

    公开(公告)日：2008-12-04

    申请号：US12178934

    申请日：2008-07-24

    申请人： Lajos Szente ,  Jozsef Szejtli ,  Gyorgy L. Kis ,  Christian Schoch

    发明人： Lajos Szente ,  Jozsef Szejtli ,  Gyorgy L. Kis ,  Christian Schoch

    IPC分类号： A61K47/30 ,  A61K47/40 ,  A61F2/00 ,  A61K38/02 ,  A61P17/02 ,  A61K31/56 ,  A61K38/43

    CPC分类号： A61K9/0024 ,  A61K9/7015 ,  A61L27/20 ,  A61L27/54 ,  A61L2300/602 ,  A61L2300/802 ,  C08L5/16

    摘要： The present invention relates to novel materials, particularly biomaterials, in form of a precipitate, comprising at least an anionic polymeric component which is as such soluble in water and an amphiphilic ammonium-type component, which precipitate is obtainable by a process including the following steps: 1. contacting the anionic polymeric component and an cyclodextrin component in an aqueous medium, and 2. adding to the mixture obtained in step 1 said amphiphilic ammonium-type component, wherein said components are present in amounts effective to form said precipitate, and preferably to corresponding precipitates additionally comprising said cyclodextrin component. Both types of precipitates may optionally comprise one or more further components. The precipitates are particularly useful as controlled-release depot formulations suitable for long-lasting delivery of said further components. The further components incorporated into the precipitates can be pharmaceutical compounds, pesticides, agrochemicals, colorants, diagnostics, enzymes, foodstuffs etc.

    摘要翻译： 本发明涉及沉淀物形式的新型材料，特别是生物材料，其包含至少一种如此可溶于水的阴离子聚合物组分和两亲性铵型组分，所述沉淀物可通过包括以下步骤 1.将阴离子聚合物组分和环糊精组分在水性介质中接触，2.向步骤1中获得的混合物中加入所述两亲性铵型组分，其中所述组分以有效形成所述沉淀物的量存在，优选 到另外包含所述环糊精组分的相应沉淀物。 两种类型的沉淀物可任选地包含一种或多种另外的组分。 沉淀物特别适用于适用于持久递送所述其它组分的控释剂型剂型。 掺入沉淀物中的其它组分可以是药物化合物，农药，农药，着色剂，诊断，酶，食品等。

    NOVEL BIOMATERIALS, THEIR PREPARATION AND USE
    7.
    发明申请
    NOVEL BIOMATERIALS, THEIR PREPARATION AND USE 审中-公开
    新生物材料，其制备和使用

    公开(公告)号：US20120040901A1

    公开(公告)日：2012-02-16

    申请号：US13281033

    申请日：2011-10-25

    申请人： Lajos Szente ,  Jozsef Szejtli ,  György Lajos Kis ,  Christian Schoch

    发明人： Lajos Szente ,  Jozsef Szejtli ,  György Lajos Kis ,  Christian Schoch

    IPC分类号： A61K38/22 ,  C12N9/00 ,  A61K31/4535 ,  A23L1/48 ,  A61K31/568 ,  A61K31/5575 ,  A61P43/00 ,  A01P15/00 ,  A01N25/00 ,  A61K31/12

    CPC分类号： A61K9/0024 ,  A61K9/7015 ,  A61L27/20 ,  A61L27/54 ,  A61L2300/602 ,  A61L2300/802 ,  C08L5/16

    摘要： The present invention relates to novel materials, particularly biomaterials, in form of a precipitate, comprising at least an anionic polymeric component which is as such soluble in water and an amphiphilic ammonium-type component, which precipitate is obtainable by a process including the following steps: 1. contacting the anionic polymeric component and an cyclodextrin component in an aqueous medium, and 2. adding to the mixture obtained in step 1 said amphiphilic ammonium-type component, wherein said components are present in amounts effective to form said precipitate, and preferably to corresponding precipitates additionally comprising said cyclodextrin component. Both types of precipitates may optionally comprise one or more further components. The precipitates are particularly useful as controlled-release depot formulations suitable for long-lasting delivery of said further components. The further components incorporated into the precipitates can be pharmaceutical compounds, pesticides, agrochemicals, colorants, diagnostics, enzymes, foodstuffs etc.

    摘要翻译： 本发明涉及沉淀物形式的新型材料，特别是生物材料，其包含至少一种如此可溶于水的阴离子聚合物组分和两亲性铵型组分，所述沉淀物可通过包括以下步骤 1.将阴离子聚合物组分和环糊精组分在水性介质中接触，2.向步骤1中获得的混合物中加入所述两亲性铵型组分，其中所述组分以有效形成所述沉淀物的量存在，优选 到另外包含所述环糊精组分的相应沉淀物。 两种类型的沉淀物可任选地包含一种或多种另外的组分。 沉淀物特别适用于适用于持久递送所述其它组分的控释剂型剂型。 掺入沉淀物中的其它组分可以是药物化合物，农药，农药，着色剂，诊断，酶，食品等。

    SIN-1A cyclodextrin inclusion complexes
    8.
    发明授权
    SIN-1A cyclodextrin inclusion complexes 失效
    SIN-1A环糊精包合物

    公开(公告)号：US5698535A

    公开(公告)日：1997-12-16

    申请号：US571853

    申请日：1996-04-16

    申请人： Joseph Geczy ,  Andrasne Vikmon ,  Jozsef Szejtli ,  Lajos Szente ,  Julianna Szeman

    发明人： Joseph Geczy ,  Andrasne Vikmon ,  Jozsef Szejtli ,  Lajos Szente ,  Julianna Szeman

    IPC分类号： C07D271/04 ,  A61K9/00 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/724 ,  A61K33/08 ,  A61K47/40 ,  A61K47/48 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C08B37/00 ,  C08B37/16 ,  A61K31/715 ,  C07D271/02 ,  C08B30/18

    CPC分类号： B82Y5/00 ,  A61K31/5375 ,  A61K47/48969 ,  C08B37/0015

    摘要： New inclusion complexes which are stable in their so-lid state formed of SIN-1A and cyclodextrins or cyclodextrin derivatives and optionally also containing ions as catalyst or stabilizer. The complexes release nitric oxide at room temperature upon dissolving in water or aqueous systems. The ions are preferably carboxylic acid anions such as acetate, formiate, propionate, ascorbinate, tartarate and/or lactate and/or inorganic acid anions such as phosphate, phosphite, borate, carbonate, hydrocarbonate, sulfate, sulfite and/or cations such as alkali and/or ammonium. Pharmaceutical compositions as well as kits containing the complexes. The kits are to be used as NO-liberating standards to release NO in a predictable amount and rate on dissolving in aqueous media. Processes for the preparation of the complexes by subjecting at a suitable pH SIN-1 to the catalytic action of ions to shift the equilibrium towards formation of SIN-1A in the presence of cyclodextrins or cyclodextrin derivatives capable to form inclusion complexes, whereby the SIN-1A formed is immediately complexed and stabilized and isolating in the solid state the obtained new complexes optionally containing ions. A preferred process includes reacting SIN-1 and a cyclodextrin or cyclodextrin derivative in the solid state in the presence of a salt as a catalyst by thoroughly admixing or milling the components together or by freeze drying an aqueous, oxygen-free solution containing the components, followed preferably by "second drying" in vacuo.

    摘要翻译： PCT No.PCT / HU95 / 00011 Sec。 371日期1996年04月16日 102（e）日期1996年4月16日PCT提交1995年4月25日PCT公布。 WO95 / 29172 PCT出版物 日期1995年11月2日在SIN-1A和环糊精或环糊精衍生物形成的其盖状态下稳定的新包合配合物和任选地还含有离子作为催化剂或稳定剂。 当溶解在水或水体系中时，复合物在室温下释放一氧化氮。 离子优选为羧酸阴离子，例如乙酸盐，甲酸盐，丙酸盐，抗坏血酸盐，酒石酸盐和/或乳酸盐和/或无机酸阴离子如磷酸盐，亚磷酸盐，硼酸盐，碳酸盐，烃酸盐，硫酸盐，亚硫酸盐和/或阳离子如碱 和/或铵。 药物组合物以及含有复合物的试剂盒。 这些试剂盒应用作NO释放标准，以可预测的量释放NO，并在溶解在含水介质中的速率。 通过在合适的pH值SIN-1下，在能够形成包合络合物的环糊精或环糊精衍生物的存在下，使离子的转移平衡转化为SIN-1A的形成，从而制备络合物的方法，由此SIN- 1A立即复合并稳定，并在固态中分离得到的任意含有离子的新配合物。 优选的方法包括在盐的存在下，通过将组分完全混合或研磨在一起或通过冷冻干燥含有组分的含水无氧溶液，使SIN-1和环糊精或环糊精衍生物在盐的存在下反应， 之后优选在真空中“二次干燥”。