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公开(公告)号:US07033609B2
公开(公告)日:2006-04-25
申请号:US09970792
申请日:2002-01-10
申请人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow , Sören Björn , Jörn Drustrup
发明人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow , Sören Björn , Jörn Drustrup
CPC分类号: A61K38/17 , A61K9/1652 , A61K38/27 , Y10T428/2982 , Y10T428/2991
摘要: A parenterally administrable, biodegradable microparticle preparation containing a biologically active substance which, during the first 24 hours after injection, exhibits a release of the active substance that is less than 25% of the total release, determined from a concentration-time curve in the form of the ratio between the area under the curve during the said first 24 hours and the total area under the curve in question
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公开(公告)号:US06706288B2
公开(公告)日:2004-03-16
申请号:US09970793
申请日:2001-10-05
申请人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
发明人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
IPC分类号: A61K950
CPC分类号: A61K9/1623 , A61K9/1652 , A61K9/1694 , A61K9/5031 , A61K9/5073 , A61K38/00 , B01J13/02 , B01J13/22 , Y10T428/2982 , Y10T428/2991
摘要: A process for producing parenterally administrable microparticles, in which an at least 20% by weight aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are made to gel, and the gelled starch particles are dried. A release-controlling shell is optionally also applied to the particles. Microparticles which essentially consist of said starch, have an amino acid content of less than 50 &mgr;g and have no covalent chemical cross-linking.
摘要翻译: 制备肠胃外给药的微粒的方法,其中制备分子量降低的至少20重量%的纯化支链淀粉基淀粉水溶液,该溶液与生物活性物质组合,淀粉液滴的乳液形成于 聚合物溶液的外相,淀粉液滴凝胶化,凝胶化淀粉颗粒干燥。 释放控制壳任选也被施加到颗粒上。基本上由所述淀粉组成的微粒的氨基酸含量小于50杯,并且没有共价的化学交联。
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公开(公告)号:US06616948B2
公开(公告)日:2003-09-09
申请号:US09970795
申请日:2001-10-05
申请人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso , Mats Reslow
发明人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso , Mats Reslow
IPC分类号: A61K950
CPC分类号: A61K9/1652 , C08B30/04 , C08B30/12 , Y10T428/2982 , Y10T428/2991
摘要: Production of purified, parenterally administrable starch by washing starch containing more than 85% amylopectin in order to remove surface-localized proteins, lipids and endotoxins, subjecting the starch to a molecular weight reduction by acid hydrolysis, and optionally removing residual water-soluble proteins. Purified starch and microparticles based on such starch.
摘要翻译: 通过洗涤含有超过85%的支链淀粉的淀粉来制备纯化的,肠胃外可施用的淀粉,以去除表面定位的蛋白质,脂质和内毒素,通过酸水解使淀粉进行分子量降低,并任选地除去残留的水溶性蛋白质。 基于这种淀粉的纯化淀粉和微粒。
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公开(公告)号:US07119195B2
公开(公告)日:2006-10-10
申请号:US10627920
申请日:2003-07-28
申请人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso
发明人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso
IPC分类号: C08B31/00 , A61K31/717
CPC分类号: A61K9/1652 , C08B30/04 , C08B30/12 , Y10T428/2982 , Y10T428/2991
摘要: Production of purified, parenterally administrable starch by washing starch containing more than 85% amylopectin in order to remove surface-localized proteins, lipids and endotoxins, dissolving the starch in aqueous medium, molecular weight reduction by shearing, and optionally removal of residual water-soluble proteins, preferably by anion exchange chromatography.Purified starch and microparticles based on such starch.
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公开(公告)号:US07105181B2
公开(公告)日:2006-09-12
申请号:US10705204
申请日:2003-11-10
申请人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
发明人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
CPC分类号: A61K9/0024 , A61K9/1652 , A61K9/1694 , A61K9/5031 , A61K38/00 , Y10T428/2982 , Y10T428/2991
摘要: A process for producing parenterally administrable microparticles, in which an at least 20% by weight aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are made to gel, and the gelled starch particles are dried. A release-controlling shell is optionally also applied to the particles.Microparticles which essentially consist of said starch, have an amino acid content of less than 50 μg and have no covalent chemical cross-linking.
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公开(公告)号:US06936278B2
公开(公告)日:2005-08-30
申请号:US10162674
申请日:2002-06-06
申请人: Mats Reslow , Monica Jönsson , Karin Larsson , Timo Laakso
发明人: Mats Reslow , Monica Jönsson , Karin Larsson , Timo Laakso
CPC分类号: A61K9/5073
摘要: A process for producing microparticles, in which an aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are made to gel, the gelled starch particles are dried, and a release-controlling shell is optionally applied to the particles, wherein at least one buffer substance having the ability of keeping the pH of the produced microparticles above 3 if exposing the microparticles to an aqueous evironment is added at any stage during the process.Microparticles which essentially consist of said starch, have an amino acid content of less than 50 μg and have no covalent chemical cross-linking and which have the aktivity of keeping the pH above 3 if exposed to a aqueous environment.
摘要翻译: 制备微粒的方法,其中制备了分子量降低的纯化支链淀粉基淀粉的水溶液,该溶液与生物活性物质组合,在聚合物溶液的外相中形成淀粉液滴的乳液,淀粉 使凝胶凝胶化,凝胶化淀粉颗粒被干燥,并且任选地将颗粒释放控制壳,其中至少一种缓冲物质,如果将微粒暴露于所述微粒上,则具有将所产生的微粒的pH保持在3以上的能力 在该过程的任何阶段加入水性环境。 基本上由所述淀粉组成的微粒具有小于50mug的氨基酸含量并且没有共价的化学交联,并且如果暴露于水性环境中,其具有保持pH高于3的活性。
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公开(公告)号:US06692770B2
公开(公告)日:2004-02-17
申请号:US10461445
申请日:2003-06-16
申请人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
发明人: Nils Ove Gustavsson , Monica Jönsson , Timo Laakso , Mats Reslow
IPC分类号: A61K916
CPC分类号: A61K9/1623 , A61K9/1652 , A61K9/1694 , A61K9/5031 , A61K9/5073 , A61K38/00 , B01J13/02 , B01J13/22 , Y10T428/2982 , Y10T428/2991
摘要: A process for producing parenterally administrable microparticles, in which an at least 20% by weight aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are med to gel, and the gelled starch particles are dried. A release-controlling shell is optionally also applied to the particles. Microparticles which essentially consist of said starch, have an amino acid content of less than 50 &mgr;g and have no covalent chemical cross-linking.
摘要翻译: 制备肠胃外给药的微粒的方法,其中制备分子量降低的至少20重量%的纯化支链淀粉基淀粉水溶液,该溶液与生物活性物质组合,淀粉液滴的乳液形成于 聚合物溶液的外相,淀粉液滴被凝胶化,凝胶化的淀粉颗粒被干燥。 释放控制壳任选地也施加到颗粒上。 基本上由所述淀粉组成的微粒的氨基酸含量小于50杯,并且没有共价的化学交联。
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公开(公告)号:US06689389B2
公开(公告)日:2004-02-10
申请号:US09970648
申请日:2001-10-05
申请人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso , Mats Reslow
发明人: Nils Ove Gustavsson , Monica Jönsson , Per Berdén , Timo Laakso , Mats Reslow
IPC分类号: A61K950
CPC分类号: A61K9/1652 , C08B30/04 , C08B30/12 , Y10T428/2982 , Y10T428/2991
摘要: Production of purified, parenterally administrable starch by washing starch containing more than 85% amylopectin in order to remove surface-localized proteins, lipids and endotoxins, dissolving the starch in aqueous medium, molecular weight reduction by shearing, and optionally removal of residual water-soluble proteins, preferably by anion exchange chromatography. Purified starch and microparticles based on such starch.
摘要翻译: 通过洗涤含有超过85%的支链淀粉的淀粉来生产纯化的,肠胃外可给予的淀粉,以去除表面定位的蛋白质,脂质和内毒素,将淀粉溶解在水性介质中,通过剪切分解重量减少和任选地除去残留的水溶性 蛋白质,优选通过阴离子交换色谱法。基于这种淀粉的纯化淀粉和微粒。
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公开(公告)号:US06616949B2
公开(公告)日:2003-09-09
申请号:US09970796
申请日:2001-10-05
申请人: Monica Jönsson , Timo Laakso , Mats Reslow
发明人: Monica Jönsson , Timo Laakso , Mats Reslow
IPC分类号: B01J1302
CPC分类号: A61K9/5089 , Y10T428/2985
摘要: A process for producing microparticles containing biologically active substance, in which process an aqueous solution of the said substance is prepared, this solution is mixed with an aqueous solution of PEG such that the substance is concentrated and/or solidified, the substance is optionally washed, the substance is mixed with an organic polymer solution, the composition obtained is mixed, after the admixture of said polymer solution, with an aqueous polymer solution, thereby forming an emulsion of droplets of first mentioned polymer as the internal phase, said droplets are solidified into microparticles, the microparticles are dried and a release-controlling shell is optionally applied to these.
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