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1.发明授权公开(公告)号：US08716217B2
公开(公告)日：2014-05-06
申请号：US12149542
申请日：2008-05-05
CPC分类号： C08G69/10 , A61K9/10 , A61K47/34 , A61K47/645 , C08G69/48
摘要： The present invention relates to novel biodegradable materials based on modified polyamino acids that are useful in particular in the vectorization of active principle(s) (APs). The invention is also directed to novel pharmaceutical, cosmetic, health-food or plant-protection compositions based on these polyamino acids.The aim of the invention is to provide a novel polymeric starting material which can be used for AP vectorization and which satisfy all the requirements: biocompatibility, biodegradability, ability to easily associate with or dissolve numerous active principles and to release these active principles in vivo. This goal is achieved by the present invention, which relates to novel polyglutamates modified by cationic groups, which, if they can be deprotonated, exhibit a pKa equal to or greater than 7, and by hydrophobic groups comprising from 8 to 30 carbon atoms.These polyglutamates modified by cationic groups are easily and economically converted into particles for the vectorization of active principles, these particles being themselves capable of forming stable aqueous colloidal suspensions. These modified polyglutamates exhibit the advantage of being less viscous than other analogous polymers while retaining an ability to associate proteins, such as insulin. Some are soluble in water at acidic pH and become insoluble at physiological pH (7.4) and should thus, during subcutaneous injection, precipitate on the site of injection.
摘要翻译： 本发明涉及基于改性聚氨基酸的新型可生物降解材料，其特别用于活性成分（AP）的向量化。 本发明还涉及基于这些聚氨基酸的新型药物，化妆品，保健食品或植物保护组合物。 本发明的目的是提供一种新颖的聚合起始材料，其可用于AP向量化，并且其满足所有要求：生物相容性，生物降解性，容易地与许多活性成分缔合或溶解的能力，并在体内释放这些活性成分。 该目的通过本发明来实现，本发明涉及由阳离子基团修饰的新的聚谷氨酸，如果它们可以去质子化，表现出等于或大于7的pKa，以及含有8至30个碳原子的疏水基团。 通过阳离子基团改性的这些聚谷氨酸可容易且经济地转化成用于活性成分载体化的颗粒，这些颗粒本身能够形成稳定的水性胶态悬浮液。 这些改性的聚谷氨酸显示出比其它类似聚合物粘稠度较低的优点，同时保留了使蛋白质如胰岛素相关联的能力。 一些在酸性pH下溶于水，在生理pH（7.4）下变得不溶，因此皮下注射时，在注射部位沉淀。
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2.发明申请公开(公告)号：US20080026070A1
公开(公告)日：2008-01-31
申请号：US11808456
申请日：2007-06-11
申请人： Cecile Bonnet-Gonnet
发明人： Cecile Bonnet-Gonnet
IPC分类号： A61K9/14 , A61K31/70 , A61K31/715 , A61K38/02 , A61K38/21 , A61P3/00 , A61P35/00 , A61P25/00 , A61K38/27 , A61K38/28 , A61K47/30
CPC分类号： A61K9/10 , A61K9/1635 , A61K31/70 , A61K31/715 , A61K38/212 , A61K38/27 , A61K38/28 , A61K47/34
摘要： The present invention relates to novel pharmaceutical formulations based on aqueous colloidal suspensions for the prolonged release of one or more active principles—AP—particularly protein and peptide active principles, and to the applications, especially therapeutic applications, of these formulations. This formulation comprises an aqueous colloidal suspension of low viscosity based on micrometric particles of a water-soluble, biodegradable, amphiphilic polymer PO carrying hydrophobic groups (GH)— alpha-tocopherol—and ionizable hydrophilic groups (GI)—Glu—that are at least partially ionized, said particles being capable of associating spontaneously and non-covalently with an AP, at pH=7.0, under isotonic conditions, and having a size of between 0.5 and 100 μm. This suspension contains multivalent ions (Mg++) of opposite polarity to that of the group GI of the PO, the ratio r, defined by the formula r = n × [ IM ] [ GI ] , where n is the valency of said multivalent ions, [IM] is the molar concentration of multivalent ions, [GI] is the molar concentration of ionizable groups GI, being between 0.3 and 10.
摘要翻译： 本发明涉及基于水性胶体悬浮液的新型药物制剂，用于延长释放这些制剂的一种或多种活性成分，特别是蛋白质和肽活性成分，以及应用，特别是治疗应用。 该制剂包含基于水溶性，可生物降解的两亲性聚合物PO的微量颗粒的低粘度的水性胶体悬浮液，其携带疏水基团（GH）-α-生育酚和可离子化亲水基团（GI）-Glu-至少是至少 部分电离，所述颗粒能够在等渗条件下在pH = 7.0下自发和非共价地与AP缔合，并且具有0.5至100μm的大小。 该悬浮液含有与PO的组GI相反极性的多价离子（Mg ++），由式
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3.发明申请公开(公告)号：US20090011028A1
公开(公告)日：2009-01-08
申请号：US12149541
申请日：2008-05-05
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/1641 , A61K38/02 , A61K47/645 , A61K48/00
摘要： The present invention relates to novel pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time of several days, or even several weeks.The invention relates, in a first aspect, to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloïdal particles of a polymer (PO), wherein said formulation satisfies the following four conditions:(a) the polymer (PO) is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said cationic groups being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said hydrophobic groups (GH) being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the polymer (PO) forms a colloïdal solution which associates spontaneously and noncovalently with the active principle (AP); (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp. The invention also relates to a process for the preparation of such formulations and to a process for the preparation of medicaments including such formulations.
摘要翻译： 本发明涉及用于在持续的几天甚至几周的时间内释放活性成分（AP）的新型药物制剂。 本发明在第一方面涉及包含至少一种活性成分（AP）和基于聚合物（PO）的胶体颗粒的水性悬浮液的液体制剂，其中所述制剂满足以下四个条件：（a） 聚合物（PO）是包含谷氨酸残基的聚氨基酸，其中一些谷氨酸残基各自携带阳离子基团（CG），所述阳离子基团彼此相同或不同，并且其它谷氨酸残基各自携带悬垂疏水基团（GH） ，所述疏水基团（GH）彼此相同或不同，（b）所述制剂的pH值的pHf值为3.0至6.5; （c）在pHf值下，聚合物（PO）形成一种自发和非共价结合活性成分（AP）的胶体溶液; （d）1ml所述制剂在与1ml测试缓冲溶液Tp的体积混合期间沉淀。 本发明还涉及一种制备这些制剂的方法以及制备包括这些制剂的药物的方法。
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4.发明申请Use of block copolymers bearing phosphate and/or phosphonate functions as adhesion promoters or as protecting agents against the corrosion of a metallic surface 有权使用带有磷酸盐和/或膦酸盐的嵌段共聚物作为粘合促进剂或作为防止金属表面腐蚀的保护剂公开(公告)号：US20050119386A1
公开(公告)日：2005-06-02
申请号：US10507329
申请日：2003-03-13
IPC分类号： C08F2/38 , C08F293/00 , C09D5/08 , C09D5/34 , C09D7/12 , C09D153/00 , C08L1/00
CPC分类号： C09D153/00 , C08F293/005 , C08L53/00 , C09D5/086 , C09D5/34 , C09D7/65
摘要： The invention relates to the use of a block copolymer having at least one block that comprises phosphate and/or phosphonate functions, as an additive for film-forming compositions, such as paint, latex or mastic which is optionally siliconised in order to ensure or promote the adhesion of the aforementioned compositions on a metallic surface or to protect said metallic surface against corrosion. The invention also relates to film-forming compositions comprising the abovementioned block copolymers.
摘要翻译： 本发明涉及使用具有至少一个包含磷酸酯和/或膦酸酯官能团的嵌段的嵌段共聚物作为成膜组合物的添加剂，例如涂料，胶乳或乳香，其任选地被硅化以确保或促进 上述组合物在金属表面上的粘附或保护所述金属表面免受腐蚀。 本发明还涉及包含上述嵌段共聚物的成膜组合物。
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5.发明授权公开(公告)号：US08236353B2
公开(公告)日：2012-08-07
申请号：US12149541
申请日：2008-05-05
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/1641 , A61K38/02 , A61K47/645 , A61K48/00
摘要： The present invention relates to pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time. The invention relates to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloidal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the PO is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said CG being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said GH being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the PO forms a colloidal solution which associates spontaneously and noncovalently with the AP; (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp.
摘要翻译： 本发明涉及用于在持续时间内释放活性成分（AP）的药物制剂。 本发明涉及包含至少一种活性成分（AP）和基于聚合物（PO）的胶体颗粒的水性悬浮液的液体制剂，其中所述制剂满足以下四个条件：（a）PO是聚氨基酸，其包含 谷氨酸残基，其中一些谷氨酸残基各自携带阳离子基团（CG），所述CG彼此相同或不同，其他谷氨酸残基各自携带悬垂疏水基团（GH），所述GH彼此相同或不同 ，（b）所述制剂的pH值的pHf值为3.0至6.5; （c）在pHf值下，PO形成胶体溶液，其与AP自发地和非共价结合; （d）1ml所述制剂在与1ml测试缓冲溶液Tp的体积混合期间沉淀。
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6.发明申请公开(公告)号：US20090011039A1
公开(公告)日：2009-01-08
申请号：US12149552
申请日：2008-05-05
CPC分类号： A61K9/5146 , A61K9/1641
摘要： The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles.These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.The invention relates, in a first aspect, to particles comprising: a) a first polyelectrolyte polymer (PE1) in a charged state, carrying side hydrophobic groups (GH), wherein said first polyelectrolyte polymer (PE1) can spontaneously form, in water, a colloidal solution of particles at least one pHm value of the pH of between 3 and 8; b) a second polyelectrolyte polymer (PE2) of opposite polarity to the first polyelectrolyte polymer (PE1), wherein said second polyelectrolyte polymer (PE2) forms, in water, a solution or a colloidal solution at said pHm value of the pH; and c) at least one active principle (AP) associated noncovalently with the particles of the colloidal solution of the first polyelectrolyte polymer (PE1); wherein said particles are obtained by mixing, at a pH equal to pHm, the first polyelectrolyte polymer (PE1), in the form of a colloidal solution of particles associated with the active principle (AP), with the second polyelectrolyte polymer (PE2), in the form of a solution or colloidal solution. The invention also relates to the process for the preparation of these particles, to a pharmaceutical formulation comprising such particles and to a process for the preparation of medicaments.
摘要翻译： 本发明涉及包含聚电解质聚合物的新型颗粒，其为活性成分（AP）的转运体，特别是蛋白质和肽活性成分，以及包含所述AP微粒的新型改性释放药物制剂。 装载AP的这些新型颗粒在几天甚至几周的较长时间内释放AP。 本发明在第一方面涉及包含以下的颗粒：a）带电状态的第一聚电解质聚合物（PE1），其携带侧疏水基团（GH），其中所述第一聚电解质聚合物（PE1）可在水中自发形成， 颗粒的胶体溶液，其pH值在3至8之间的至少一个pHm值; b）与第一聚电解质聚合物（PE1）相反极性的第二聚电解质聚合物（PE2），其中所述第二聚电解质聚合物（PE2）在水中以所述pHm的pH值在水中形成溶液或胶体溶液; 和c）与第一聚电解质聚合物（PE1）的胶体溶液的颗粒非共价结合的至少一种活性成分（AP）; 其中所述颗粒是通过在等于pHm的pH下，以与活性成分（AP）相关的颗粒的胶态溶液与第二聚电解质聚合物（PE2）的形式混合第一聚电解质聚合物（PE1）而获得的， 以溶液或胶体溶液的形式存在。 本发明还涉及制备这些颗粒的方法，包括这种颗粒的药物制剂和制备药物的方法。
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公开(公告)号：US08481019B2
公开(公告)日：2013-07-09
申请号：US12149552
申请日：2008-05-05
IPC分类号： A61K31/74
CPC分类号： A61K9/5146 , A61K9/1641
摘要： The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles.These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.The invention relates, in a first aspect, to particles comprising: a) a first polyelectrolyte polymer (PE1) in a charged state, carrying side hydrophobic groups (GH), wherein said first polyelectrolyte polymer (PE1) can spontaneously form, in water, a colloidal solution of particles at least one pHm value of the pH of between 3 and 8; b) a second polyelectrolyte polymer (PE2) of opposite polarity to the first polyelectrolyte polymer (PE1), wherein said second polyelectrolyte polymer (PE2) forms, in water, a solution or a colloidal solution at said pHm value of the pH; and c) at least one active principle (AP) associated noncovalently with the particles of the colloidal solution of the first polyelectrolyte polymer (PE1); wherein said particles are obtained by mixing, at a pH equal to pHm, the first polyelectrolyte polymer (PE1), in the form of a colloidal solution of particles associated with the active principle (AP), with the second polyelectrolyte polymer (PE2), in the form of a solution or colloidal solution. The invention also relates to the process for the preparation of these particles, to a pharmaceutical formulation comprising such particles and to a process for the preparation of medicaments.
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8.发明申请NANOPARTICLES HAVING AT LEAST ONE ACTIVE INGREDIENT AND AT LEAST TWO POLYELECTROLYTES 审中-公开具有至少一个活性成分和至少两个聚电解质的纳米颗粒公开(公告)号：US20120156256A1
公开(公告)日：2012-06-21
申请号：US13328696
申请日：2011-12-16
CPC分类号： A61K9/5146 , A61K9/0019 , A61K9/10 , A61K9/5192 , B82Y5/00 , Y10T428/2982
摘要： The present invention relates to novel nanoparticles formed by at least one active ingredient and by at least two polyelectrolytes of opposite polarity, in particular characterized in that at least one of the two polyelectrolytes bears hydrophobic side groups and at least one of the two polyelectrolytes bears side groups of the polyalkylene glycol type, said nanoparticles having an average diameter ranging from 10 to 100 nm and comprising a quantity of groups of the polyalkylene glycol type such that the mass ratio wPAG of polyalkylene glycol relative to the total polymer is greater than or equal to 0.05.
摘要翻译： 本发明涉及由至少一种活性成分和至少两种相反极性的聚电解质形成的新型纳米颗粒，其特征在于两种聚电解质中的至少一种具有疏水性侧基，并且两种聚电解质中的至少一种具有侧面 聚亚烷基二醇型的基团，所述纳米颗粒的平均直径范围为10至100nm，并且包含一定量的聚亚烷基二醇型，使得聚亚烷基二醇的质量比wPAG相对于总聚合物大于或等于 0.05。
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9.发明申请公开(公告)号：US20090012028A1
公开(公告)日：2009-01-08
申请号：US12149542
申请日：2008-05-05
IPC分类号： A61K47/36 , A61K31/711 , A61K31/7105 , C08G63/685
CPC分类号： C08G69/10 , A61K9/10 , A61K47/34 , A61K47/645 , C08G69/48
摘要： The present invention relates to novel biodegradable materials based on modified polyamino acids that are useful in particular in the vectorization of active principle(s) (APs). The invention is also directed to novel pharmaceutical, cosmetic, health-food or plant-protection compositions based on these polyamino acids.The aim of the invention is to provide a novel polymeric starting material which can be used for AP vectorization and which satisfy all the requirements: biocompatibility, biodegradability, ability to easily associate with or dissolve numerous active principles and to release these active principles in vivo. This goal is achieved by the present invention, which relates to novel polyglutamates modified by cationic groups, which, if they can be deprotonated, exhibit a pKa equal to or greater than 7, and by hydrophobic groups comprising from 8 to 30 carbon atoms.These polyglutamates modified by cationic groups are easily and economically converted into particles for the vectorization of active principles, these particles being themselves capable of forming stable aqueous colloidal suspensions. These modified polyglutamates exhibit the advantage of being less viscous than other analogous polymers while retaining an ability to associate proteins, such as insulin. Some are soluble in water at acidic pH and become insoluble at physiological pH (7.4) and should thus, during subcutaneous injection, precipitate on the site of injection.
摘要翻译： 本发明涉及基于改性聚氨基酸的新型可生物降解材料，其特别用于活性成分（AP）的向量化。 本发明还涉及基于这些聚氨基酸的新型药物，化妆品，保健食品或植物保护组合物。 本发明的目的是提供一种新颖的聚合起始材料，其可用于AP向量化，并且其满足所有要求：生物相容性，生物降解性，容易地与许多活性成分缔合或溶解的能力，并在体内释放这些活性成分。 该目的通过本发明来实现，本发明涉及由阳离子基团修饰的新的聚谷氨酸，如果它们可以去质子化，表现出等于或大于7的pKa，以及含有8至30个碳原子的疏水基团。 通过阳离子基团改性的这些聚谷氨酸可容易且经济地转化成用于活性成分载体化的颗粒，这些颗粒本身能够形成稳定的水性胶态悬浮液。 这些改性的聚谷氨酸显示出比其它类似聚合物粘稠度较低的优点，同时保留了使蛋白质如胰岛素相关联的能力。 一些在酸性pH下溶于水，在生理pH（7.4）下变得不溶，因此皮下注射时，在注射部位沉淀。
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10.发明申请Use of block copolymers bearing phosphate and/or phosphonate functions as adhesion promoters or as protecting agents against the corrosion of a metallic surface 审中-公开使用带有磷酸盐和/或膦酸盐的嵌段共聚物作为粘合促进剂或作为防止金属表面腐蚀的保护剂公开(公告)号：US20050181225A1
公开(公告)日：2005-08-18
申请号：US10507330
申请日：2003-03-12
IPC分类号： C08F2/38 , C08F293/00 , C09D5/00 , C09D7/12 , C09J153/00 , B05D7/00 , B05D1/18 , B21C1/00
CPC分类号： C09J153/00 , C08F293/005 , C09D5/002 , Y10T428/12
摘要： The invention relates to the use of a block copolymer having at least one block that comprises phosphate and/or phosphonate functions in order to produce a deposit on a metallic surface, such as a steel or aluminium surface, which can be used, for example, to improve the effectiveness of the subsequent application of a film-forming composition on the thus altered surface or to protect the metallic surface against corrosion. The invention also relates to a method of applying paint or mastic compositions to a metallic surface, which involves the above-mentioned inventive use of said block copolymers, and the coated metallic materials that can be produced using said application method.
摘要翻译： 本发明涉及具有至少一个包含磷酸盐和/或膦酸盐的嵌段的嵌段共聚物的用途，以便在诸如钢或铝表面的金属表面上产生沉积物，其可以用于例如， 以提高随后在如此改变的表面上施用成膜组合物的有效性，或者保护金属表面免受腐蚀。 本发明还涉及将油漆或乳胶组合物施加到金属表面上的方法，其涉及上述本发明使用的所述嵌段共聚物，以及可使用所述涂布方法制备的涂覆的金属材料。
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