公开(公告)号：US20070196497A1

公开(公告)日：2007-08-23

申请号：US10580023

申请日：2004-11-19

申请人： Gauthier Pouliquen ,  Olivier Soula ,  Remi Meyrueix ,  Florence Nicolas

发明人： Gauthier Pouliquen ,  Olivier Soula ,  Remi Meyrueix ,  Florence Nicolas

IPC分类号： A61K9/14

CPC分类号： A61K9/0024 ,  A61K38/2013 ,  A61K38/212 ,  A61K47/42 ,  A61K47/645 ,  A61K51/1217

摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of active principle(s), particularly protein active principle(s), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of active principle(s) that makes it possible, after parenteral injection, to increase significantly the in vivo release time of a therapeutic protein while at the same time reducing the plasma concentration peak of the active protein, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance. The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one active principle (AP) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.

摘要翻译： 本发明涉及基于用于延长释放活性成分（特别是蛋白质活性成分）的稳定的流体水性胶体悬浮液以及这些制剂的应用，特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放活性成分的流体药物制剂，其使得在胃肠外注射后可以显着增加治疗性蛋白质的体内释放时间，同时减少 活性蛋白质的血浆浓度峰值，所述制剂还在储存时稳定，并且还具有生物相容性，可生物降解，无毒和非免疫原性并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团（HG）的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶体悬浮液，所述颗粒与至少一种活性成分（AP）非共价缔合并形成 在注射部位的凝胶沉积物，这种胶凝是由存在于生理介质中的蛋白质引起的。

公开(公告)号：US20070269517A1

公开(公告)日：2007-11-22

申请号：US10580037

申请日：2004-11-19

申请人： Gauthier Pouliquen ,  Remi Meyrueix ,  Olivier Soula

发明人： Gauthier Pouliquen ,  Remi Meyrueix ,  Olivier Soula

IPC分类号： A61K9/10 ,  A61K38/21

CPC分类号： A61K47/42 ,  A61K9/0024 ,  A61K38/21 ,  A61K47/645 ,  A61K47/665 ,  B82Y5/00

摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of an interferon (IFN) (and one or more other possible active principles), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of interferon(s) (and one or more other possible active principles) that makes it possible, after parenteral injection, significantly to increase the in vivo release time of the interferons while at the same time reducing the plasma concentration peak of this IFN, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance. The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one interferon (and one or more other possible active principles) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.

摘要翻译： 本发明涉及基于用于延长释放干扰素（IFN）（和一种或多种其它可能的活性成分）的稳定的流体水性胶体悬浮液以及这些制剂的应用，特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放干扰素（和一种或多种其它可能的活性成分）的流体药物制剂，其使得在肠胃外注射后可以显着地增加体内释放时间 干扰素，同时降低该IFN的血浆浓度峰值，所述制剂还在储存时稳定，并且还是生物相容的，可生物降解的，无毒的和非免疫原性的并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团（HG）的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶态悬浮液，所述颗粒与至少一种干扰素（和一种或多种其它 可能的活性成分），并在注射部位形成凝胶沉积物，该胶凝是由存在于生理介质中的蛋白质引起的。

公开(公告)号：US20090110742A1

公开(公告)日：2009-04-30

申请号：US11632992

申请日：2005-06-09

申请人： Alain Constancis ,  Florence Nicolas ,  Remi Meyrueix ,  Olivier Soula

发明人： Alain Constancis ,  Florence Nicolas ,  Remi Meyrueix ,  Olivier Soula

IPC分类号： A61K9/14 ,  A61K38/28 ,  A61P3/10

CPC分类号： A61K38/28 ,  A61K9/1075 ,  A61K9/5138 ,  A61K9/5146 ,  A61K9/5192 ,  Y10S977/773 ,  Y10S977/906

摘要： The invention relates to injectable long-acting insulin formulations for the treatment of types I and II diabetes in humans and animals.The essential object of the invention is to provide an injectable long-acting insulin formulation in the form of a colloidal suspension which is stable, which has a good local tolerance and toxicity compatible with the chronic treatment of diabetics, and which maintains a substantial hypoglycemic effect extending over at least 24 hours after a single administration, e.g. by the subcutaneous route.To achieve this object, the invention relates to a stable aqueous colloidal formulation of insulin-laden nanoparticles of at least one poly(Leu-block-Glu) in which the pH is between 5.8 and 7.0, the osmolarity O (in mOsmol) . . . : 270≦O≦800, and the viscosity v (in mPa.s) is low, namely v≦40. The nanoparticles of poly(Leu-block-Glu) have a mean hydrodynamic diameter Dh such that: 15≦Dh≦40.The invention relates to an antidiabetic drug based on this long-acting insulin formulation and injectable using needles of gauge 29G, 30G or 31G.

摘要翻译： 本发明涉及用于治疗人和动物中I型和II型糖尿病的可注射长效胰岛素制剂。 本发明的基本目的是提供一种稳定的胶体悬浮液形式的可注射的长效胰岛素制剂，其具有与糖尿病患者的慢性治疗相适应的良好的局部耐受性和毒性，并且其保持显着的降血糖效应 在单次给药后延长至少24小时，例如 通过皮下途径。 为了实现这个目的，本发明涉及至少一种pH（在5.8至7.0之间），渗透压浓度O（以mOsmol计）的至少一种聚（Leu-block-Glu）的含胰岛素的纳米颗粒的稳定水性胶体制剂。 。 。 ：270 <= 0 <= 800，粘度v（mPa.s）低，即v <= 40。 聚（Leu-block-Glu）的纳米颗粒具有平均流体动力学直径Dh，使得：15 <= Dh <= 40。 本发明涉及基于该长效胰岛素制剂的抗糖尿病药物，并使用量规29G，30G或31G的针头进行注射。

公开(公告)号：US6133199A

公开(公告)日：2000-10-17

申请号：US124318

申请日：1998-07-29

申请人： Gerard G. Soula ,  Remi Meyrueix ,  Alain J. L. Lemercier ,  Nathan J. Bryson ,  Olivier Soula ,  Anthony J. I. Ward ,  Jane L. Gillespie ,  Ronald J. Brinker

发明人： Gerard G. Soula ,  Remi Meyrueix ,  Alain J. L. Lemercier ,  Nathan J. Bryson ,  Olivier Soula ,  Anthony J. I. Ward ,  Jane L. Gillespie ,  Ronald J. Brinker

IPC分类号： A01N25/04 ,  A01N25/30 ,  A01N57/20 ,  C07F9/38

CPC分类号： C07F9/3813 ,  A01N25/04 ,  A01N25/30 ,  A01N57/20

摘要： A plant treatment composition for application of an anionic exogenous chemical substance such as glyphosate herbicide to foliage of a plant is provided. The composition is a colloidal dispersion having supramolecular aggregates dispersed in an aqueous application medium. The supramolecular aggregates comprise one or more amphiphilic salt(s) having anions of the exogenous chemical substance and cations derived by protonation of one or more polyamine(s) or polyamine derivative(s) each having (a) at least two nitrogen-containing groups, of which a number n not less than 1 are amino groups that can be protonated to form cationic primary, secondary or tertiary ammonium groups, and (b) at least one hydrocarbyl or acyl group having about 6 to about 30 carbon atoms. The composition contains (i) a molar amount X in total of the exogenous chemical substance, in all salt and acid forms thereof present, sufficient to elicit a biological response when the composition is applied to the foliage of the plant at a rate of about 10 to about 1000 l/ha, (ii) a molar amount A in total of said polyamine(s) and derivative(s) thereof and cations derived therefrom, and (iii) a zero or molar amount B in total of one or more monovalent base(s) and cations derived therefrom, said base(s) being other than a polyamine or derivative thereof, such that nA/(nA+B) is about 0.01 to 1, and (nA+B)/X is about 0.5 to about 10.Also provided are a liquid concentrate composition which, upon dilution with water, forms a plant treatment composition as described above, and a process for making such a liquid concentrate composition. Plant treatment compositions of the invention are useful for eliciting a biological activity, for example herbicidal activity, in a plant when applied to foliage thereof.

摘要翻译： 提供了一种用于将阴离子外源化学物质如草甘膦除草剂施用于植物叶子的植物处理组合物。 该组合物是具有分散在水溶液介质中的超分子聚集体的胶态分散体。 超分子聚集体包含一种或多种具有外源化学物质的阴离子的两亲盐和通过一种或多种多胺或多胺衍生物的质子化产生的阳离子，每个多胺或多胺衍生物各自具有（a）至少两个含氮基团 其数n为不小于1的氨基可以被质子化形成阳离子伯，仲或叔铵基团，和（b）至少一个具有约6至约30个碳原子的烃基或酰基。 所述组合物包含（i）外源化学物质的总量X，其存在的所有盐和酸形式，足以引起组合物以约10的速率施用于植物的叶子时的生物反应 至约1000l / ha，（ii）所述多胺及其衍生物的总摩尔量A和由其衍生的阳离子，和（iii）零或摩尔量B总计为一种或多种一价 碱和其衍生的阳离子，所述碱不是多胺或其衍生物，使得nA /（nA + B）为约0.01至1，和（nA + B）/ X为约0.5至 还提供了液体浓缩组合物，其在用水稀释时形成如上所述的植物处理组合物，以及制备这种液体浓缩组合物的方法。 本发明的植物处理组合物可用于在施用于其叶面时在植物中引发生物活性，例如除草活性。

公开(公告)号：US20070218142A1

公开(公告)日：2007-09-20

申请号：US10580035

申请日：2004-11-19

申请人： Sophie Bignon ,  Remi Meyrueix ,  Olivier Soula

发明人： Sophie Bignon ,  Remi Meyrueix ,  Olivier Soula

IPC分类号： A61K9/14

CPC分类号： A61K38/2013 ,  A61K9/0024 ,  A61K38/20 ,  A61K47/34 ,  A61K47/6921 ,  A61K47/6935

摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of an interleukin (IL) (and one or more other possible active principles), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of interleukin(s) (and one or more other possible active principles) that makes it possible, after parenteral injection, significantly to increase the in vivo release time of the IL while at the same time reducing the plasma concentration peak of this IL, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance. The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one interleukin (and one or more other possible active principles) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.

摘要翻译： 本发明涉及基于用于延长释放白介素（IL）（和一种或多种其它可能的活性成分）的稳定的流体水性胶体悬浮液以及这些制剂的应用，特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放白细胞介素（和一种或多种其它可能的活性成分）的流体药物制剂，其使得在胃肠外注射后可显着地增加体内释放时间 IL，同时降低该IL的血浆浓度峰值，所述制剂还在储存时稳定，并且也是生物相容的，可生物降解的，无毒的和非免疫原性的并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团（HG）的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶态悬浮液，所述颗粒与至少一种白细胞介素（和一种或多种其它物质）非共价结合 可能的活性成分），并在注射部位形成凝胶沉积物，该胶凝是由存在于生理介质中的蛋白质引起的。

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.

公开(公告)号：US20060110463A1

公开(公告)日：2006-05-25

申请号：US10510621

申请日：2003-04-07

申请人： Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix

发明人： Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix

IPC分类号： A61K31/43 ,  A61K9/50 ,  A61K9/16

CPC分类号： A61K9/5015 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/43

摘要： The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

摘要翻译： 本发明涉及用于阿莫西林的改性释放的口服给药的液体药物制剂，所述制剂由阿莫西林（微胶囊）的包衣颗粒的悬浮液组成。 根据本发明，构成悬浮液分散相的微胶囊被设计成允许根据在液体悬浮液储存过程中不变化的分布来改变阿莫西林的释放。 为了做到这一点，发明人提出了选择用于微胶囊的特定涂料组合物，其由至少四种组分组成，这些组分允许这些微胶囊储存在水中而不改变其改性释放的阿莫西林的性质，此液相还饱和 阿莫西林

公开(公告)号：US5535048A

公开(公告)日：1996-07-09

申请号：US210995

申请日：1994-03-21

申请人： Gerard Mignani ,  Gerard Soula ,  Remi Meyrueix

发明人： Gerard Mignani ,  Gerard Soula ,  Remi Meyrueix

IPC分类号： G02F1/35 ,  C07C211/44 ,  C07C215/16 ,  C07C255/37 ,  C07C255/42 ,  C07D215/12 ,  C07D217/04 ,  C07D221/06 ,  C07D339/06 ,  C07D455/04 ,  C07D471/04 ,  G02F1/355 ,  G02F1/361 ,  C07D451/02

CPC分类号： G02F1/3612 ,  C07C255/37 ,  C07C255/42 ,  C07D455/04 ,  G02F1/3611 ,  G02F1/3614 ,  C07C2101/16

摘要： Novel nonlinearly optically active compound's, well suited for electrooptical applications, have the following general formulae: ##STR1## wherein D is an electron donor group; A and A.sub.1, which may be identical or different, are each an electron acceptor group; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a lower alkyl radical or a hydrogen atom.

摘要翻译： 新的非线性光学活性化合物，非常适合于电光学应用，具有以下通式：（I）和oup; A和A1可以相同或不同，各自为电子受体基团; 并且R 1，R 2，R 3和R 4各自为低级烷基或氢原子。

公开(公告)号：US5359072A

公开(公告)日：1994-10-25

申请号：US714585

申请日：1991-06-13

申请人： Gerard Mignani ,  Gerard Soula ,  Remi Meyrueix

发明人： Gerard Mignani ,  Gerard Soula ,  Remi Meyrueix

IPC分类号： G02F1/35 ,  C07C211/44 ,  C07C215/16 ,  C07C255/37 ,  C07C255/42 ,  C07D215/12 ,  C07D217/04 ,  C07D221/06 ,  C07D339/06 ,  C07D455/04 ,  C07D471/04 ,  G02F1/355 ,  G02F1/361 ,  C07D451/02

CPC分类号： G02F1/3612 ,  C07C255/37 ,  C07C255/42 ,  C07D455/04 ,  G02F1/3611 ,  G02F1/3614 ,  C07C2101/16

摘要： Novel nonlinearly optically active compounds, well suited for electrooptical applications, have the following general formulae: ##STR1## wherein D is an electron donor group; A and A.sub.1, which may be identical or different, are each an electron acceptor group; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a lower alkyl radical or a hydrogen atom.

摘要翻译： 非常适合于电光应用的新型非线性光学活性化合物具有以下通式：（I）及以上; A和A1可以相同或不同，各自为电子受体基团; 并且R 1，R 2，R 3和R 4各自为低级烷基或氢原子。

公开(公告)号：US20090041838A1

公开(公告)日：2009-02-12

申请号：US11883935

申请日：2006-02-08

申请人： Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

发明人： Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

IPC分类号： A61K9/50 ,  A61K9/14 ,  A61K9/22

CPC分类号： A61K9/5047 ,  A61K9/5078 ,  A61K31/196 ,  A61K31/522

摘要： The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form. More specifically, the invention relates to a solid oral drug form comprising anti-misuse means and at least one active ingredient, which is characterized in that: at least part of the active ingredient is contained in microparticles; and the anti-misuse means comprise anti-crushing means (a) which enable the microparticles of the active ingredient to resist crushing, such as to prevent the misuse thereof. According to the invention, the drug form can also comprise means (b) for preventing the misuse of the active ingredient following a possible liquid extraction process.

摘要翻译： 本发明涉及具有防止滥用其中所含的活性药物成分（API）的组合物的固体微粒口服剂型。 本发明的目的是防止不适当地使用固体口服药物以用于由适当的公共卫生当局正式批准的治疗用途以外的任何用途。 本发明的另一个目的是提供新的止痛药，其可用于：防止某些止痛剂的滥用和成瘾和/或控制血浆浓度变异性和/或促进口服; 行政; 和/或将镇痛药彼此和/或以相同口服形式的一种或多种活性成分组合。 更具体地，本发明涉及包含抗滥用手段和至少一种活性成分的固体口服药物形式，其特征在于：至少部分活性成分包含在微粒中; 并且防误用手段包括能够使活性成分的微粒抵抗破碎的抗破碎装置（a），以防止其误用。 根据本发明，药物形式还可以包括用于防止在可能的液体提取过程后滥用活性成分的装置（b）。