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    Colloidal suspension of submicronic particles for delivering active principles and method for preparing same
    1.
    发明申请
    Colloidal suspension of submicronic particles for delivering active principles and method for preparing same 审中-公开
    用于递送活性成分的亚微粒子的胶体悬浮液及其制备方法

    公开(公告)号：US20070190162A1

    公开(公告)日：2007-08-16

    申请号：US11583941

    申请日：2006-10-20

    申请人： Sylvain Caillol ,  Remi Meyruiex ,  Nathan Bryson ,  Alain Soum ,  Gerard Soula ,  Anne-Francoise Mingotaud

    发明人： Sylvain Caillol ,  Remi Meyruiex ,  Nathan Bryson ,  Alain Soum ,  Gerard Soula ,  Anne-Francoise Mingotaud

    IPC分类号： A61K9/14

    CPC分类号： A61K8/88 ,  A61K8/0241 ,  A61K9/5153 ,  A61K9/5192 ,  A61K2800/413 ,  A61K2800/56 ,  A61Q19/00 ,  B82Y5/00 ,  C08G81/00 ,  C08J3/14 ,  C08J2377/12

    摘要： The present invention is directed to a suspension of particles for delivering active principles, in particular proteins. Said particles are based on a diblock copolymer consisting of a neutral hydrophobic alpha hydroxy carboxylic acid polymer block and a hydrophilic linear polyaminoacid block with peptide alpha chaining, at least partly ionized. Said alpha hydroxy carboxylic acid polymer/linear polyaminoacid delivery particles spontaneously obtainable in the absence of surfactant can be stable. Said delivery particles are capable of being associated undissolved in colloidal suspension with at least an active principle and of delayed or prolonged release thereof. The invention is also directed to a powdery solid from which are derived the delivery particles and the preparation of said solid and said delivery particle suspension.

    摘要翻译： 本发明涉及用于递送活性成分的颗粒的悬浮液，特别是蛋白质。 所述颗粒基于由中性疏水性α羟基羧酸聚合物嵌段和具有至少部分电离的肽α链的亲水性线性聚氨基酸嵌段组成的二嵌段共聚物。 在不存在表面活性剂的情况下自发获得的所述α羟基羧酸聚合物/线性聚氨基酸输送颗粒可以是稳定的。 所述递送颗粒能够以至少一种活性成分和延迟或延长释放的胶体悬浮液的形式相互不溶解。 本发明还涉及粉末状固体，其衍生自所述输送颗粒以及所述固体和所述输送颗粒悬浮液的制备。

    Microcapsules with modified release of active principles with low solubility for oral delivery
    2.
    发明申请
    Microcapsules with modified release of active principles with low solubility for oral delivery 有权
    具有改进释放活性成分的微胶囊，具有低溶解性用于口服递送

    公开(公告)号：US20070160678A1

    公开(公告)日：2007-07-12

    申请号：US11583940

    申请日：2006-10-20

    申请人： Florence Guimberteau ,  Catherine Castan ,  Remi Meyruiex ,  Gerard Soula

    发明人： Florence Guimberteau ,  Catherine Castan ,  Remi Meyruiex ,  Gerard Soula

    IPC分类号： A61K31/55 ,  A61K31/551 ,  A61K31/522 ,  A61K31/405 ,  A61K31/192 ,  A61K9/50

    CPC分类号： A61K9/5015 ,  A61K9/5026 ,  A61K9/5047

    摘要： The present invention is directed to microcapsules for reliably modified release and adapted to industrial reproduction of an active principle hardly water-soluble, other than anti-hyperglycemia agents. Each of said microcapsules comprises a core of hardly soluble active principle and a coating film applied on the core. Their mean diameter is less than 1000 microns. The coating film contains a film-forming polymer (PI) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said coating film represents at least 4% p/p of dry matter of their total weight, and its components P1, P2, PL satisfy the following characteristics: dry weight mass fraction of PI relative to the total coating weight ranging between 40 and 90%; dry matter weight fraction of PL/P1 +P2 ranging between 15 and 60%; dry matter weight fraction of PL/P1+P2 ranging between 1 and 30%. The present invention is also directed to the uses of said microcapsules in galenic formulation.

    摘要翻译： 本发明涉及用于可靠改性释放的微胶囊，并且适用于除抗高血糖剂之外的几乎不溶于水的活性成分的工业繁殖。 所述微胶囊中的每一个都包含难溶于活性成分的核心和涂覆在芯上的涂膜。 它们的平均直径小于1000微米。 涂膜含有不溶于胃肠道液的成膜聚合物（PI），水溶性聚合物（P2），增塑剂（PL）和任选的润滑表面活性剂（TA）。 所述涂膜占其总重量的干物质的至少4％p / p，其组分P1，P2，PL满足以下特征：相对于总涂层重量的干重质量分数为40-90％ ; PL / P1 + P2的干物质重量分数在15〜60％之间; PL / P1 + P2的干物质重量分数范围在1％至30％之间。 本发明还涉及所述微胶囊在盖仑制剂中的用途。

    Colloidal suspension of submicronic particles for carrying active principles and their mode of preparation
    3.
    发明申请
    Colloidal suspension of submicronic particles for carrying active principles and their mode of preparation 审中-公开
    用于携带活性成分的亚微粒子的胶体悬浮液及其制备方式

    公开(公告)号：US20080015332A1

    公开(公告)日：2008-01-17

    申请号：US11878364

    申请日：2007-07-24

    申请人： Nathan Bryson ,  Gerard Soula

    发明人： Nathan Bryson ,  Gerard Soula

    IPC分类号： C08G69/08

    CPC分类号： A61Q19/00 ,  A61K8/11 ,  A61K9/5138 ,  A61K9/5146 ,  A61K2800/413 ,  B01J13/0021

    摘要： The invention concerns a suspension of biocompatible particles for carrying active principles. Said carrier particles are based on a double-block hydrophilic neutral polyaminoacid/hydrophobic neutral polyaminoacid copolymer. Said hydrophilic neutral polyaminoacid/hydrophobic neutral polyaminoacid particles are capable of combining in colloidal suspension in non-dissolved state, at least an active principle and of releasing same, in particular in vivo, in prolonged and/or delayed delivery. The invention also concerns a powdery solid from which are derived the carrier particles and the preparation of said solid and of said suspension of active principle based on hydrophilic neutral polyaminoacids/hydrophobic neutral polyaminoacids. Said carrier particles form spontaneously and in the absence of surfactants or organic solvents, stable aqueous suspensions. The invention also concerns the carrier particles in dry form, the method for preparing them, and pharmaceutical compositions (in dry form or suspension) comprising said carrier particles associated with an active principle.

    摘要翻译： 本发明涉及用于携带活性成分的生物相容性颗粒的悬浮液。 所述载体颗粒基于双嵌段亲水性中性聚氨基酸/疏水性中性聚氨基酸共聚物。 所述亲水性中性聚氨基酸/疏水性中性聚氨基酸颗粒能够在非溶解状态的胶体悬浮液，至少一种活性成分和在其延长和/或延迟递送中特别是在体内释放它们的胶态混合物中结合。 本发明还涉及一种粉末状固体，其衍生为载体颗粒，以及基于亲水性中性聚氨基酸/疏水性中性聚氨基酸的所述固体和所述活性成分悬浮液的制备。 所述载体颗粒自发形成，并且在不存在表面活性剂或有机溶剂的情况下形成稳定的水悬浮液。 本发明还涉及干燥形式的载体颗粒，其制备方法和包含与活性成分相关联的所述载体颗粒的药物组合物（干燥形式或悬浮液）。

    Complex consisted of a polysaccharide and an HBP
    6.
    发明申请
    Complex consisted of a polysaccharide and an HBP 有权
    复合物由多糖和HBP组成

    公开(公告)号：US20100184965A1

    公开(公告)日：2010-07-22

    申请号：US12585886

    申请日：2009-09-28

    申请人： Olivier Soula ,  Remi Soula ,  Martin Gaudier ,  Gerard Soula

    发明人： Olivier Soula ,  Remi Soula ,  Martin Gaudier ,  Gerard Soula

    IPC分类号： A61K47/48 ,  C08B37/04 ,  C08B15/06 ,  C08B37/00

    CPC分类号： A61K9/0019 ,  A61K9/19 ,  A61K38/1825 ,  A61K38/185 ,  A61K38/1866 ,  A61K38/27 ,  A61K38/29 ,  A61K47/42 ,  A61K47/61

    摘要： The invention relates to a complex consisted of a polysaccharide and an HBP, said polysaccharide being consisted from glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative. The invention also relates to a pharmaceutical composition comprising a complex according to the invention and to the use of a polysaccharide consisted of glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative, for the preparation of a pharmaceutical formulation of stable HBPs.

    摘要翻译： 本发明涉及由多糖和HBP组成的复合物，所述多糖由（1,6）和/或（1,4）和/或（1,3）和/或（1,2）的糖苷键组成 ）类型并用至少一种可成盐或盐化的色氨酸衍生物官能化。 本发明还涉及包含根据本发明的复合物和由（1,6）和/或（1,4）和/或（1,3）和/或（1,3）的糖苷键组成的多糖和/ 或（1,2）型，并用至少一种可成盐或盐化的色氨酸衍生物官能化，用于制备稳定HBP的药物制剂。

    Angiogenic composition
    8.
    发明申请
    Angiogenic composition 审中-公开
    血管生成成分

    公开(公告)号：US20080293635A1

    公开(公告)日：2008-11-27

    申请号：US12078443

    申请日：2008-03-31

    申请人： Olivier Soula ,  Gerard Soula ,  Remi Soula ,  Rosy Eloy

    发明人： Olivier Soula ,  Gerard Soula ,  Remi Soula ,  Rosy Eloy

    IPC分类号： A61K38/16 ,  A61P9/00

    CPC分类号： A61K9/0014 ,  A61K38/1858 ,  A61K47/61

    摘要： The present invention relates to a amphiphilic polymer in the preparation of a therapeutic composition for promoting angiogenesis at its site of administration, comprising a complex between a polymer and a PDGF, wherein the polymer is amphiphilic.In an embodiment, the PDGF is selected from the group of the PDGFs (platelet-derived growth factors) and the amphiphilic polymer is selected from the group: The invention relates also to the therapeutic composition is in the form of a gel, a cream, a solution, a spray, a paste or a patch or a dressing.

    摘要翻译： 本发明涉及制备用于在其施用部位促进血管发生的治疗组合物的两亲性聚合物，其包含聚合物和PDGF之间的复合物，其中所述聚合物是两亲性的。 在一个实施方案中，PDGF选自PDGF（血小板衍生生长因子）组，两亲性聚合物选自：本发明还涉及治疗组合物，其形式为凝胶，霜剂， 溶液，喷雾剂，糊剂或贴剂或敷料。

    Telechelic Homopolyamino Acids Functionalized with Hydrophobic Groups, and Their Applications, Especially Therapeutic Applications
    9.
    发明申请
    Telechelic Homopolyamino Acids Functionalized with Hydrophobic Groups, and Their Applications, Especially Therapeutic Applications 失效
    用疏水基团功能化的远端肝氨基酸及其应用，特别是治疗应用

    公开(公告)号：US20070265192A1

    公开(公告)日：2007-11-15

    申请号：US10574475

    申请日：2004-09-28

    申请人： Rémi Soula ,  You-Ping Chan ,  Gerard Soula ,  Olivier Breyne

    发明人： Rémi Soula ,  You-Ping Chan ,  Gerard Soula ,  Olivier Breyne

    IPC分类号： A61K47/30 ,  A61K38/28 ,  A61P3/10 ,  C07C229/12

    CPC分类号： A61K8/88 ,  A61K9/1075 ,  A61K9/5146 ,  A61K47/34 ,  A61K47/645 ,  A61Q19/00 ,  C08G69/10 ,  C08G73/028 ,  C08L79/02

    摘要： The invention relates to novel materials based on biodegradable homopolyamino acids and which can be used for the vectorization of (an) active ingredient(s) (AI). The invention also relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on said homopolyamino acids. The aim of the invention is to produce a novel polymer raw material which can be used for the vectorization of AI and which meets all specifications in an optimum manner: biocompatibility, biodegradability, the ability to become easily associated with a large number of active ingredients or to solubilize them and to release said ingredients in vivo. According to the present invention, which primarily relates to linear homopolyamino acids having aspartic or glutamic units and whose extremities include hydrophobic groups having 8-30 carbon atoms. Said homopolymers are amphiphilic and anionic and can easily be transformed at low cost into particles for the vectorization of active ingredients. Said particles can form stable aqueous colloidal suspensions.

    摘要翻译： 本发明涉及基于可生物降解的均聚氨基酸的新型材料，其可用于（a）活性成分（AI）的向量化。 本发明还涉及基于所述均聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明的目的是生产一种新颖的聚合物原料，其可用于AI的载体化并且以最佳方式满足所有规格：生物相容性，生物降解性，与许多活性成分容易相关的能力或 以溶解它们并在体内释放所述成分。 根据本发明，其主要涉及具有天冬氨酸或谷氨酸单元的线性均聚氨基酸，其末端包括具有8-30个碳原子的疏水基团。 所述均聚物是两亲性的和阴离子的，并且可以容易地以低成本转化成用于活性成分载体化的颗粒。 所述颗粒可以形成稳定的水性胶体悬浮液。

    Oral ribavirin pharmaceutical compositions
    10.
    发明申请
    Oral ribavirin pharmaceutical compositions 审中-公开

    公开(公告)号：US20070166378A1

    公开(公告)日：2007-07-19

    申请号：US11449675

    申请日：2006-06-09

    申请人： Florence Guimberteau ,  Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

    发明人： Florence Guimberteau ,  Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

    IPC分类号： A61K31/7056 ,  A61K9/22

    CPC分类号： A61K9/5026 ,  A61K9/2077 ,  A61K9/48 ,  A61K9/5042 ,  A61K31/7056

    摘要： The invention relates to oral pharmaceutical compositions for the prevention and/or the treatment of viral diseases. This invention also addresses methods of prevention and/or treatment of these viral diseases, using these oral compositions. One of the main problems considered in the present invention is to enhance the efficiency of anti-viral treatments, especially against Hepatitis C virus by means of ribavirin, for example in combination with interferon. The oral ribavirin antiviral composition according to the invention increases the bio-absorption time of ribavirin, and thus improves the treatment of patients. Said composition comprises at least one modified release form of ribavirin, the bio-absorption time BAT of which is greater than the bio-absorption time BAT* of a reference* immediate release form of ribavirin administered at the same dose; BAT being preferably comprised between 2 and 15 h and more preferably between 4 and 12 h. Said composition is a reservoir type form or a matrix type form. Said composition is a gastric retentive system or a multiparticulate form.