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1. 发明授权

US6013284A Synthetic particulate vectors and preparation process 失效
标题翻译：合成颗粒载体及其制备方法
公开(公告)号：US6013284A
公开(公告)日：2000-01-11
申请号：US513853
申请日：1996-05-01
申请人： Daniel Samain , Pascal Delrieu , Joelle Gibilaro , Roselyne Dirson , Monique Cervilla , Ignacio De Miguel , Li Ding , Frederique Nguyen , Nadine Soulet , Corinne Soler
发明人： Daniel Samain , Pascal Delrieu , Joelle Gibilaro , Roselyne Dirson , Monique Cervilla , Ignacio De Miguel , Li Ding , Frederique Nguyen , Nadine Soulet , Corinne Soler
IPC分类号： A23L27/00 , A61K8/00 , A61K8/11 , A61K8/14 , A61K8/36 , A61K8/42 , A61K8/64 , A61K8/66 , A61K8/68 , A61K8/73 , A61K8/92 , A61K8/97 , A61K8/99 , A61K9/16 , A61K9/50 , A61K9/51 , A61Q19/00 , A61Q90/00
CPC分类号： A61K9/5123 , A23L27/70 , A23L27/72 , A61K8/11 , A61K8/14 , A61K8/66 , A61K8/97 , A61K9/1652 , A61K9/5015 , A61K9/5161 , A61Q19/00 , B82Y5/00 , A61K2800/412 , A61K2800/413 , Y10S514/951 , Y10S514/952 , Y10T428/2991
摘要： A synthetic particulate vector comprising a non-liquid hydrophilic nucleus and an outer layer at least partially consisting of amphiphilic compounds, which is combined with the nucleus by hydrophobic interactions and/or ionic bonds. A process for preparing a particulate vector by encapsulating an ionizable active principle, vectors obtained according to such a process, and pharmaceutical, cosmeticological and food compositions comprising such vectors are also disclosed.
摘要翻译： PCT No.PCT / FR94 / 00228 Sec。 371日期：1996年5月1日 102（e）日期1996年5月1日PCT 1994年3月1日PCT公布。 WO94 / 20078 PCT公开号日期1994年9月15日一种包含非液体亲水核和至少部分由两亲化合物组成的外层的合成颗粒载体，其通过疏水相互作用和/或离子键与核结合。还公开了通过包封可离子化活性成分，根据这种方法获得的载体以及包含这种载体的药物，美容和食用组合物来制备颗粒载体的方法。

2. 发明授权

US5736371A Biodegradable particulate vector for transporting molecules having biological activity 失效
标题翻译：用于输送具有生物活性的分子的可生物降解的颗粒载体
公开(公告)号：US5736371A
公开(公告)日：1998-04-07
申请号：US243079
申请日：1994-05-16
申请人： Daniel Samain , Ignacio De Miguel , Jaouad Meniali , Karim Ioualalen , Li Ding , Monique Cervilla , Valerie Rieumajou , Pascal Delrieu , Laurent Imbertie
发明人： Daniel Samain , Ignacio De Miguel , Jaouad Meniali , Karim Ioualalen , Li Ding , Monique Cervilla , Valerie Rieumajou , Pascal Delrieu , Laurent Imbertie
IPC分类号： A61K9/127 , A61K9/16 , A61K9/51 , C12N11/12 , A61K38/43 , C07K17/12 , C12N11/10
CPC分类号： A61K9/5161 , A61K9/127 , A61K9/167 , A61K9/5192 , Y10S530/813 , Y10S530/814
摘要： A biodegradable particulate vector for transporting biologically active molecules is prepared containing a nucleus for containing a biologically active molecule, a first layer of fatty acid compounds covalently bonded to the nucleus and a second layer of phospholipids hydrophobically bonded to the first layer. The nucleus is between 10 nm and 10 .mu.m in size and is formed of a cross-linked polysaccharide or oligosaccharide matrix onto which ionic ligands are uniformly grafted. The cross-linked polysaccharide may be dextran, cellulose or starch cross-linked with epichlorohydrin. The ligand may be an acidic compound selected from succinic acid, phosphoric acid, citric acid, glycine, alanine, glutamic acid and aspartic acid, or a basic compound such as choline, hydroxycholine, 2-(dimethylamino)ethanol or 2-(dimethylamino)ethylamine fastened onto the matrix via the acidic compound. The polysaccharide or oligosaccharide may be co-cross-linked with a protein such as keratin/collagen or elastase. The vector may be prepared by reacting succinic acid monochloride in aqueous solution with a cross-linked polysaccharide or oligosaccharide matrix to graft succinic acid onto the matrix to form the nucleus, grinding the nucleus to a size between 10 nm and 10 .mu.m, drying the ground nucleus, coupling fatty acid compounds to the nucleus to form a first layer and hydrophobically bonding phospholipids to the first layer to form a second layer. The succinic acid monochloride is preferably prepared by reacting succinic acid dichloride with free succinic acid to form pure crystalline succinic acid monochloride.
摘要翻译：制备用于输送生物活性分子的可生物降解的颗粒载体，其包含含有生物活性分子的核，与核共价键合的第一层脂肪酸化合物和与第一层疏水结合的第二层磷脂。核的尺寸在10nm和10μm之间，并且由交联的多糖或寡糖基质形成，其上离子配体被均匀地接枝到其上。交联多糖可以是与表氯醇交联的葡聚糖，纤维素或淀粉。配体可以是选自琥珀酸，磷酸，柠檬酸，甘氨酸，丙氨酸，谷氨酸和天冬氨酸的酸性化合物，或碱性化合物如胆碱，羟基胆碱，2-（二甲基氨基）乙醇或2-（二甲基氨基）乙胺通过酸性化合物固定在基质上。多糖或寡糖可以与蛋白质如角蛋白/胶原或弹性蛋白酶共交联。载体可以通过使琥珀酸一氯化物在水溶液中与交联的多糖或寡糖基质反应来将琥珀酸接枝到基质上以形成核，将细胞核研磨至10nm至10μm的大小，干燥研磨核，将脂肪酸化合物偶联到细胞核上形成第一层，并将磷脂与第一层疏水结合形成第二层。琥珀酸一氯化物优选通过琥珀酸二氯化物与游离琥珀酸反应形成纯结晶琥珀酸一氯化物来制备。

3. 发明授权

US5968794A Biodegradable particulate vector for transporting molecules having biological activity 失效
标题翻译：用于输送具有生物活性的分子的可生物降解的颗粒载体
公开(公告)号：US5968794A
公开(公告)日：1999-10-19
申请号：US12645
申请日：1998-01-23
申请人： Daniel Samain , Ignacio De Miguel , Jaouad Meniali , Karim Ioualalen , Li Ding , Monique Cervilla , Valerie Rieumajou , Pascal Delrieu , Laurent Imbertie
发明人： Daniel Samain , Ignacio De Miguel , Jaouad Meniali , Karim Ioualalen , Li Ding , Monique Cervilla , Valerie Rieumajou , Pascal Delrieu , Laurent Imbertie
IPC分类号： A61K9/127 , A61K9/16 , A61K9/51 , C12N11/12 , A61K38/43 , C07H1/02 , C07K1/04
CPC分类号： A61K9/5161 , A61K9/127 , A61K9/167 , A61K9/5192 , Y10S530/813 , Y10S530/814
摘要： A biodegradable particulate vector for transporting biologically active molecules is prepared containing a nucleus formed of a cross-linked polysaccharide or oligosaccharide matrix having grafted ionic ligands, a layer of fatty acid compounds covalently bonded to the nucleus and a layer of phospholipids hydrophobically bonded to the layer of fatty acid compounds. Dextran, cellulose or starch may be cross-linked with epichlorohydrin to form a cross-linked polysaccharide matrix. Ionic ligands may be grafted using an acidic compound such as succinic acid, phosphoric acid or phosphorous oxychloride, or a basic compound such as choline, hydroxycholine, 2-(dimethylamino)ethanol or 2-(dimethylamino) ethylamine fastened onto the grafted acidic compound. Phosphoric acid or phosphorous oxychloride in one step provide both cross-linking and ionic ligands. Co-cross-linking can be obtained using a protein such as keratin, collagen or elastase. The vector may be prepared by reacting succinic acid monochloride with a cross-linked polysaccharide matrix to graft succinic acid onto the matrix to form the nucleus having ionic ligands, grinding the nucleus to a size between 10 .mu.nm and 10 .mu.m, drying, coupling fatty acid compounds to the nucleus and hydrophobically bonding phospholipids to the fatty acid compounds. After coupling the fatty acid compounds and before bonding the phospholipids, a molecule having biological activity may be added. The succinic acid monochloride is preferably prepared by reacting succinic acid dichloride with free succinic acid to form pure crystalline succinic acid monochloride.
摘要翻译：制备用于输送生物活性分子的可生物降解的颗粒载体，其含有由具有接枝离子配体的交联多糖或寡糖基质形成的核，与核共价键合的脂肪酸化合物层和与层疏水结合的磷脂层的脂肪酸化合物。葡聚糖，纤维素或淀粉可以与表氯醇交联以形成交联的多糖基质。离子配体可以使用酸性化合物如琥珀酸，磷酸或三氯氧磷，或碱性化合物如胆碱，羟基胆碱，2-（二甲基氨基）乙醇或2-（二甲基氨基）乙胺接枝在接枝的酸性化合物上。磷酸或磷酰氯在一个步骤中提供交联和离子配体。可以使用蛋白质如角蛋白，胶原或弹性蛋白酶获得共交联。载体可以通过使琥珀酸一氯化物与交联的多糖基质反应来制备，以将琥珀酸接枝到基质上以形成具有离子配体的核，将细胞核研磨至10μm至10μm之间的大小，干燥，偶联脂肪酸化合物到细胞核并将磷脂疏水性结合到脂肪酸化合物上。偶联脂肪酸化合物之后，在磷脂结合之前，可以加入具有生物活性的分子。琥珀酸一氯化物优选通过琥珀酸二氯化物与游离琥珀酸反应形成纯结晶琥珀酸一氯化物来制备。

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