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    Self-precipitating pharmaceutical formulations for the modified release of an active principle
    1.
    发明授权
    Self-precipitating pharmaceutical formulations for the modified release of an active principle 失效
    用于改性释放活性成分的自沉淀药物制剂

    公开(公告)号：US08236353B2

    公开(公告)日：2012-08-07

    申请号：US12149541

    申请日：2008-05-05

    申请人： Frédéric Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    发明人： Frédéric Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    IPC分类号： A61K9/14 ,  A61K9/64 ,  A61K9/58 ,  A61K38/00 ,  A61K9/52

    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。

    Self-precipitating pharmaceutical formulations for the moified release of an active principle
    2.
    发明申请
    Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
    用于释放活性成分的自沉淀药物制剂

    公开(公告)号：US20090011028A1

    公开(公告)日：2009-01-08

    申请号：US12149541

    申请日：2008-05-05

    申请人： Frederic Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    发明人： Frederic Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    IPC分类号： A61K47/42 ,  A61K9/10 ,  A61K38/20

    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。

    Polyesterimides for use in linear and/or non-linear optics, and one method for preparing same
    4.
    发明授权
    Polyesterimides for use in linear and/or non-linear optics, and one method for preparing same 失效
    用于线性和/或非线性光学的聚酰亚胺及其制备方法

    公开(公告)号：US5811507A

    公开(公告)日：1998-09-22

    申请号：US628639

    申请日：1996-11-14

    申请人： You-Ping Chan ,  Gilles Tapolsky ,  Remi Meyrueix ,  Jean-Pierre Lecomte ,  Michael Dickens

    发明人： You-Ping Chan ,  Gilles Tapolsky ,  Remi Meyrueix ,  Jean-Pierre Lecomte ,  Michael Dickens

    IPC分类号： G02F1/01 ,  C08G63/685 ,  C08G73/16 ,  G02F1/35 ,  G02F1/355 ,  G02F1/361

    CPC分类号： G02F1/3617 ,  C08G63/6856 ,  C08G73/16

    摘要： The present invention relates to a new polyesterimide of the type containing ester repeat functional groups E=--CO--O--, imide repeat functional groups I: ##STR1## and at least one chromophore, characterized in that it contains a quantity of recurrent amide functional groups capable of ring closure to imides which is smaller than or equal to 5 mol % relative to the sum of the imide functional groups and of the amide functional groups capable of ring closure to imides, which are present, and in that the polymerization functional groups consist essentially of E functional groups. This polyesterimide is preferably free from amide functional groups capable of ring closure to imides. One of the processes for obtaining this polyesterimide constitutes another subject-matter of the invention. Such a polymer is advantageously capable of behaving like a material that is transparent and/or active in nonlinear optics. It therefore constitutes a raw material of choice for producing LO and/or NLO devices: filters, polarizers, waveguides, a modulator, directional coupler, optical flip-flop and photoconductive film.

    摘要翻译： PCT No.PCT / FR94 / 01219 Sec。 371日期：1996年11月14日 102（e）日期1996年11月14日PCT 1994年10月20日PCT PCT。 第WO95 / 11476号公报 日期：1995年04月27日本发明涉及含有酯重复官能团的类型的新的聚酯酰亚胺E = -CO-O-，酰亚胺重复官能团I：＆lt; IMAGE＆gt;和至少一种发色团，其特征在于它含有 能够闭环的酰胺官能团的量相对于酰亚胺官能团和能够闭合的酰胺官能团的总和小于或等于5摩尔％，其存在和存在于酰亚胺中 聚合官能团基本上由E官能团组成。 该聚酯酰亚胺优选不含能够闭合成酰亚胺的酰胺官能团。 获得该聚酯酰亚胺的方法之一构成本发明的另一主题。 这种聚合物有利地能够表现得像非线性光学中透明和/或有活性的材料。 因此，它构成了生产LO和/或NLO器件的首选材料：滤波器，偏振器，波导，调制器，定向耦合器，光学触发器和光电导膜。

    Oral ribavirin pharmaceutical compositions
    5.
    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.

    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin
    6.
    发明申请
    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin 失效
    用于阿莫西林改性释放的微胶囊水性悬浮液形式的口服药物制剂

    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

    Process and compositions promoting biological effectiveness of exogenous chemical substances in plants
    7.
    发明授权
    Process and compositions promoting biological effectiveness of exogenous chemical substances in plants 失效
    促进植物中外源化学物质生物有效性的方法和成分

    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。

    Anti-Misuse Microparticulate Oral Drug Form
    10.
    发明申请
    Anti-Misuse Microparticulate Oral Drug Form 审中-公开
    反滥用微量口服药物形式

    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）。