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    • 1. 发明授权
    • SIN-1A cyclodextrin inclusion complexes
    • SIN-1A环糊精包合物
    • US5698535A
    • 1997-12-16
    • US571853
    • 1996-04-16
    • Joseph GeczyAndrasne VikmonJozsef SzejtliLajos SzenteJulianna Szeman
    • Joseph GeczyAndrasne VikmonJozsef SzejtliLajos SzenteJulianna Szeman
    • C07D271/04A61K9/00A61K31/42A61K31/4245A61K31/535A61K31/5375A61K31/5377A61K31/724A61K33/08A61K47/40A61K47/48A61P9/10A61P35/00A61P43/00C08B37/00C08B37/16A61K31/715C07D271/02C08B30/18
    • B82Y5/00A61K31/5375A61K47/48969C08B37/0015
    • 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.
    • 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”。
    • 4. 发明申请
    • NOVEL BIOMATERIALS, THEIR PREPARATION AND USE
    • 新生物材料,其制备和使用
    • US20080299166A1
    • 2008-12-04
    • US12178934
    • 2008-07-24
    • Lajos SzenteJozsef SzejtliGyorgy L. KisChristian Schoch
    • Lajos SzenteJozsef SzejtliGyorgy L. KisChristian Schoch
    • A61K47/30A61K47/40A61F2/00A61K38/02A61P17/02A61K31/56A61K38/43
    • A61K9/0024A61K9/7015A61L27/20A61L27/54A61L2300/602A61L2300/802C08L5/16
    • 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.
    • 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。
    • 8. 发明申请
    • NOVEL BIOMATERIALS, THEIR PREPARATION AND USE
    • 新生物材料,其制备和使用
    • US20120040901A1
    • 2012-02-16
    • US13281033
    • 2011-10-25
    • Lajos SzenteJozsef SzejtliGyörgy Lajos KisChristian Schoch
    • Lajos SzenteJozsef SzejtliGyörgy Lajos KisChristian Schoch
    • A61K38/22C12N9/00A61K31/4535A23L1/48A61K31/568A61K31/5575A61P43/00A01P15/00A01N25/00A61K31/12
    • A61K9/0024A61K9/7015A61L27/20A61L27/54A61L2300/602A61L2300/802C08L5/16
    • 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.
    • 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。