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1. 发明授权

US5498788A Inclusion complexes of clavulanic acid and of potassium salts thereof with hydrophobic .beta.-cyclodextrin derivatives a process for the preparation thereof 失效
标题翻译：克拉维酸及其钾盐与疏水性β-环糊精衍生物的包合物及其制备方法
公开(公告)号：US5498788A
公开(公告)日：1996-03-12
申请号：US369301
申请日：1995-01-06
申请人： Janko Zmitek , Darja Fercej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kovacic
发明人： Janko Zmitek , Darja Fercej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kovacic
IPC分类号： A61K9/08 , A61K9/107 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/48 , A61K31/42 , A61K31/424 , A61K47/40 , A61K47/48 , A61P31/04 , A61P43/00 , C07D498/00 , C07D503/00 , C07D503/18 , C08B37/16 , C07D487/04 , A61K9/26
CPC分类号： B82Y5/00 , A61K31/42 , A61K31/424 , A61K47/48969
摘要： Described is a new process for the preparation of alkali clavulanate from an aqueous solution of pure clavulanic acid and of pharmaceutically acceptable potassium crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic .beta.-CD derivative such as heptakis-(2,3,6-tri-O-acetyl)-.beta.-CD in equimolar amount or up to 10% excess with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic .beta.-CD derivative in a molar ratio about 1:1 are isolated, purified with water and then converted with potassium 2-ethyl hexanate to the potassium clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable potassium salt both with hydrophilic .beta.-CD derivatives and with hydrophobic .beta.-CD derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.
摘要翻译：描述了从纯克拉维酸的水溶液和药学上可接受的克拉维酸钠制备克拉维酸碱的新方法，其在用产生克拉维酸的微生物发酵后以常规方式获得，用疏水性β-CD衍生物的乙酸乙酯溶液，例如等摩尔量的七（-2,6-三-O-乙酰基）-β-CD或相对于克拉维酸高达10％的过量。所得到的克拉维酸和疏水性β-CD衍生物的新型包合配合物的摩尔比约为1:1，分离，用水纯化，然后用2-乙基己酸钾转化成克拉维酸钾，将其分离。此外，描述了克拉维酸及其药学上可接受的钾盐与亲水性β-CD衍生物和疏水性β-CD衍生物的新的包合物，其制备方法及其用于立即制备galenic形式的用途以及持续的作用，与阿莫西林三水合物组合，这是治疗传染病的有价值的药物。

2. 发明授权

US5614199A Inclusion complexes of clavulanic acid and of alkali salts thereof with hydrophilic and hydrophobic .beta.-cyclodextrin derivatives, a process for the preparation thereof and the use thereof 失效
标题翻译：克拉维酸及其碱金属盐与亲水和疏水性β-环糊精衍生物的包合物，其制备方法及其用途
公开(公告)号：US5614199A
公开(公告)日：1997-03-25
申请号：US470267
申请日：1995-06-06
申请人： Janko Zmitek , Darja Fercej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kovacic
发明人： Janko Zmitek , Darja Fercej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kovacic
IPC分类号： A61K9/08 , A61K9/107 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/48 , A61K31/42 , A61K31/424 , A61K47/40 , A61K47/48 , A61P31/04 , A61P43/00 , C07D498/00 , C07D503/00 , C07D503/18 , C08B37/16 , A61K9/00
CPC分类号： B82Y5/00 , A61K31/42 , A61K31/424 , A61K47/48969
摘要： Described is a new process for the preparation of alkali clavulanate from an aqueous solution of crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic .beta.-CD derivative such as heptakis-(2,3,6-tri-O-acetyl)-.beta.-CD in at least equimolar ratio with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic .beta.-CD derivative in a molar ratio about 1:1 are isolated, purified and then converted with an alkali base or alkali alkanoate to the desired alkali clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable alkali salts both with hydrophilic .beta.-CD derivatives and with hydrophobic .beta.-CD derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.
摘要翻译：描述了一种从粗制棒酸的水溶液制备克拉维酸碱的新方法，该方法是在用产生克拉维酸的微生物发酵之后以常规方式获得的，用疏水性β-葡聚糖的乙酸乙酯溶液萃取， CD衍生物，如克拉维酸至少等摩尔比例的七（ - ） - （2,3,6-三-O-乙酰基）-β-CD。所得到的克拉维酸和疏水性β-CD衍生物的摩尔比约为1:1的新型包合物被分离，纯化，然后用碱金属碱或碱金属酸碱转化成所需的克拉维酸碱盐，将其分离。此外，还描述了克拉维酸及其药学上可接受的碱金属盐与亲水性β-CD衍生物和疏水性β-CD衍生物的新型包合配合物，其制备方法及其用于立即制备盖仑制剂的用途以及持续的作用，与阿莫西林三水合物组合，这是治疗传染病的有价值的药物。

3. 发明授权

US5840714A Inclusion complexes of racemic ibuproxam and of optically active ibuproxam with cyclodextrin derivatives, pharmaceutical preparations containing said inclusion complexes and methods for using same 失效
标题翻译：外消旋布洛康和旋光布洛克星与环糊精衍生物的包合物，含有所述包合物的药物制剂及其使用方法
公开(公告)号：US5840714A
公开(公告)日：1998-11-24
申请号：US602729
申请日：1996-02-20
申请人： Janko Zmitek , Katarina Verhnjak , Darja Fercej-Temeljotov , Mateja Kovacic , Anton Lavric , Breda Bole-Vunduk
发明人： Janko Zmitek , Katarina Verhnjak , Darja Fercej-Temeljotov , Mateja Kovacic , Anton Lavric , Breda Bole-Vunduk
IPC分类号： A61K9/00 , A61K31/165 , A61K47/48 , C07C51/00 , C07C57/00 , C07C259/06 , A61K47/40 , C07H21/00
CPC分类号： B82Y5/00 , A61K31/165 , A61K47/48969 , C07C259/06 , Y10S514/965
摘要： Inclusion Complexes of Racemic Ibuproxam and of Optically Active Ibuproxam with Cyclodextrin Derivatives, Process for the Preparation Thereof, Pharmaceutical Preparations Containing these Inclusion Complexes or Containing Optically Active S-(+)-Ibuproxam, and Use Thereof There are disclosed novel inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone. Further a process for preparing S-(+)-ibuproxam and inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic derivatives of .beta.-cyclodextrin and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, is disclosed. Disclosed are also pharmaceutical compositions containing these inclusion complexes or optically active S-(+)-ibuproxam. Optically active S-(+)-ibuproxam and novel inclusion complexes of racemic ibuproxam and of optically active ibuproxam with cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, are better soluble in water and have improved biopharmaceutical properties such as lesser toxicity, better antiinflammatory action and non-irritation of the gastric mucous membrane.
摘要翻译： PCT No.PCT / SI94 / 00015 Sec。 371日期1996年2月20日 102（e）日期1996年2月20日PCT 1994年9月6日PCT PCT。第WO95 / 07076号公报日期1995年3月16日包含外消旋布洛康和光学活性布洛克星与环糊精衍生物的复合物，其制备方法，含有这些包合配合物或含有光学活性的S - （+） - 布洛克星姆的药物制剂及其用途已经公开了新颖的外消旋布洛克星和光学活性的S - （+） - 布洛克星与亲水和疏水性环糊精衍生物的包合物，以及在光学活性的S - （+） - 布洛克星）的情况下，也仅与β-环糊精一起使用。此外，制备S - （+） - 布洛克星和外消旋布洛克星与光学活性S - （+） - 布洛克星与β-环糊精的亲水和疏水衍生物的包合物的方法，在光学活性S - （+ ） - 吡罗昔康，也是单独使用β-环糊精。还公开了含有这些包合物或光学活性的S - （+） - 布洛康的药物组合物。光学活性的S - （+） - 布洛克星和外消旋布洛克星与光学活性布洛克星与环糊精衍生物的新型包合物，以及光学活性的S - （+） - 布洛克星，单独使用β-环糊精的情况较好并具有改善的生物药物性质，如毒性较小，抗炎作用更好，胃粘膜无刺激性。

4. 发明授权

US5608052A Inclusioin complexes of clavulanic acid and of alkali salts thereof with hydrophilic and hydrophobic beta-cyclodextrin derivatives, a process for the preparation thereof and the use thereof 失效
标题翻译：克拉维酸及其碱金属盐与亲水和疏水性β-环糊精衍生物的包合物，其制备方法及其用途
公开(公告)号：US5608052A
公开(公告)日：1997-03-04
申请号：US469870
申请日：1995-06-06
申请人： Janko Zmitek , Darja Fer cej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kova ci c
发明人： Janko Zmitek , Darja Fer cej-Temeljotov , Katarina Verhnjak , Sonja Kotnik , Mateja Kova ci c
IPC分类号： A61K9/08 , A61K9/107 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/48 , A61K31/42 , A61K31/424 , A61K47/40 , A61K47/48 , A61P31/04 , A61P43/00 , C07D498/00 , C07D503/00 , C07D503/18 , C08B37/16 , A61K31/715 , C07D487/08
CPC分类号： B82Y5/00 , A61K31/42 , A61K31/424 , A61K47/48969
摘要： Described is a new process for the preparation of alkali clavulanate from an aqueous solution of crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic .beta.-cyclodextrin derivative such as heptakis-(2,3,6-tri-O-acetyl)-.beta.-cyclodextrin in at least equimolar ratio with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic .beta.-cyclodextrin derivative in a molar ratio about 1:1 are isolated, purified and then converted with an alkali base or alkali alkanoate to the desired alkali clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable alkali salts both with hydrophilic .beta.-cyclodextrin derivatives and with hydrophobic .beta.-cyclodextrin derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.
摘要翻译：描述了一种从粗制棒酸的水溶液制备克拉维酸碱的新方法，该方法是在用产生克拉维酸的微生物发酵之后以常规方式获得的，用疏水性β-葡聚糖的乙酸乙酯溶液萃取，环糊精衍生物，例如七 - （2,3,6-三-O-乙酰基）-β-环糊精，至少等摩尔比为克拉维酸。所得到的克拉维酸和疏水性β-环糊精衍生物的摩尔比约为1:1的新型包合物被分离，纯化，然后用碱金属碱或碱金属酸碱转化成所需的克拉维酸碱盐，将其分离。此外，还描述了克拉维酸及其药学上可接受的碱金属盐与亲水性β-环糊精衍生物和疏水性β-环糊精衍生物的新型包合物，其制备方法及其用于立即制备盖仑膜形式的用途以及持续的作用，与阿莫西林三水合物组合，这是治疗传染病的有价值的药物。

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