公开(公告)号：US4429160A

公开(公告)日：1984-01-31

申请号：US296214

申请日：1981-08-25

申请人： Louis Linguenheld ,  Gerard Soula

发明人： Louis Linguenheld ,  Gerard Soula

IPC分类号： C09K3/00 ,  B01F1/00 ,  B01J25/00 ,  B01J25/02 ,  C07B61/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/08 ,  C07C93/04

CPC分类号： C07C213/02

摘要： Novel polyoxaalkyl aminoalcohols, well adapted for the complexation/solubilization of a wide variety of cations, have the structural formula: ##STR1##

摘要翻译： 新的聚氧杂烷基氨基醇，适用于各种阳离子的络合/溶解，具有以下结构式：

公开(公告)号：US4322369A

公开(公告)日：1982-03-30

申请号：US216363

申请日：1980-12-15

申请人： Michel Desbois ,  Gerard Soula

发明人： Michel Desbois ,  Gerard Soula

IPC分类号： C07C255/19 ,  C07C67/00 ,  C07C253/00 ,  C07C120/04

CPC分类号： C07C255/00 ,  C07C253/14

摘要： The alkyl cyanoacetates are prepared by reacting an alkyl chloracetate with an excess of an alkali metal cyanide, in an inert solvent and in the presence of at least one tertiary amine sequestering agent having the formula:N--CHR.sub.1 --CHR.sub.2 --O--CHR.sub.3 --CHR.sub.4 --O.sub.n R.sub.5 ].sub.3 (I).

摘要翻译： 氰基乙酸烷基酯通过使氯代乙酸烷基酯与过量的碱金属氰化物在惰性溶剂中并在至少一种具有下式的叔胺螯合剂的存在下反应制备：N-CHR1-CHR2-O-CHR3-CHR4 -OnR5] 3（I）。

公开(公告)号：US4094802A

公开(公告)日：1978-06-13

申请号：US782881

申请日：1977-03-30

申请人： Gerard Soula ,  Philippe Duteurtre

发明人： Gerard Soula ,  Philippe Duteurtre

IPC分类号： B01D19/04 ,  C07D207/40 ,  C07D207/412 ,  C10M133/16 ,  C10M133/56 ,  C10N30/04 ,  C10N30/12 ,  C10N30/18 ,  C10N40/25 ,  C10M1/32 ,  C10M3/26 ,  C10M5/20 ,  C10M7/30

CPC分类号： C07D207/412 ,  C10M133/16 ,  C10M133/56 ,  C10M2203/02 ,  C10M2203/022 ,  C10M2203/024 ,  C10M2203/04 ,  C10M2203/06 ,  C10M2205/02 ,  C10M2207/028 ,  C10M2207/04 ,  C10M2207/282 ,  C10M2207/34 ,  C10M2209/00 ,  C10M2209/02 ,  C10M2209/10 ,  C10M2209/103 ,  C10M2209/108 ,  C10M2209/109 ,  C10M2215/04 ,  C10M2215/26 ,  C10M2217/046 ,  C10M2217/06 ,  C10M2219/044 ,  C10M2223/04 ,  C10M2223/042 ,  C10M2223/045 ,  C10M2229/02 ,  C10M2229/05 ,  C10N2210/02 ,  C10N2230/12

摘要： Novel lubricant additives are provided comprising compositions based on alkenylsuccinimides containing at least one alkenylsuccinimide of the formula: ##STR1## WHERE R is an alkenyl group of about C.sub.20 to C.sub.200, m is an integer equal to 0, 1 or 2, and n is an integer equal to 0 or 1. These compositions can be prepared by condensation of an alkenylsuccinic anhydride with N,N,N',N'-tetrakis-(3-aminopropyl)-ethylenediamine.

摘要翻译： 提供新的润滑剂添加剂，其包含基于含有至少一个下式的链烯基琥珀酰亚胺的烯基琥珀酰亚胺的组合物：其中R为约C20至C200的烯基，m为等于0,1或2的整数 ，n是等于0或1的整数。这些组合物可以通过烯基琥珀酸酐与N，N，N'，N'-四（3-氨基丙基） - 乙二胺缩合来制备。

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）。

公开(公告)号：US20080260844A1

公开(公告)日：2008-10-23

申请号：US11791471

申请日：2005-11-21

申请人： Gerard Soula ,  Florence Guimberteau

发明人： Gerard Soula ,  Florence Guimberteau

IPC分类号： A61K9/14 ,  A61K31/522

CPC分类号： A61K31/196 ,  A61K9/0053 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047 ,  A61K9/5078

摘要： The invention relates to the field of solid, oral, microparticulate dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient contained therein. The aim of the invention is to prevent the improper use of solid oral medicaments for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. More specifically, the invention relates to a solid, oral drug form which is characterised in that at least one part of the active pharmaceutical ingredient is contained in the microparticles thereof and in that the inventive form comprises anti-crushing means which are intended to impede or completely prevent the crushing of the microparticles of the active pharmaceutical ingredient, such as to preclude the misuse thereof.

摘要翻译： 本发明涉及具有防止其中含有的活性药物成分的滥用的组合物的固体，口服，微粒剂型的领域。 本发明的目的是防止固体口服药物用于除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。 更具体地，本发明涉及固体口服药物形式，其特征在于活性药物成分的至少一部分包含在其微粒中，并且本发明形式包括抗破碎装置，其旨在阻止或 完全防止活性药物成分的微粒的破碎，排除其滥用。

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）。

公开(公告)号：US20070264326A1

公开(公告)日：2007-11-15

申请号：US11648605

申请日：2007-01-03

申请人： Florence Guimberteau ,  Gerard Soula

发明人： Florence Guimberteau ,  Gerard Soula

IPC分类号： A61K9/58 ,  A61K9/16 ,  A61K9/48 ,  A61K9/62 ,  A61K9/64 ,  A61K9/60 ,  A61K9/50

CPC分类号： A61K9/5078 ,  A61K9/0095 ,  A61K9/5047

摘要： The field of the present invention is that of solid microparticulate analgesic oral medicines. The invention is that of providing novel analgesic medicines which allow at the same time the prevention of misuse and of addiction to certain analgesics, and/or the control of variability in the plasma concentration and/or the facilitation of oral administration; and/or the combination of analgesics with one another and/or with one or more active ingredients in the same oral form. The medicine according to the invention comprises (i) anti-misuse means and a plurality of microcapsules with modified release of analgesic(s), having a mean diameter of between 50 and 600 μm, (ii) at least 1000 microcapsules per dose; it being possible for this medicine to be administered once or twice a day for analgesic purposes.

摘要翻译： 本发明的领域是固体微粒止痛口服药物。 本发明是提供新的止痛药物，其同时可以防止某些止痛剂的滥用和成瘾，和/或控制血浆浓度和/或促进口服给药的变异性; 和/或镇痛剂与彼此和/或与一种或多种相同口服形式的活性成分的组合。 根据本发明的药物包括（i）抗滥用装置和多个具有镇痛剂释放的微胶囊，平均直径为50至600μm，（ii）每剂量至少1000个微胶囊; 该药可以每天一次或两次给药，用于镇痛目的。

公开(公告)号：US20070207214A1

公开(公告)日：2007-09-06

申请号：US11723553

申请日：2007-03-21

申请人： Catherine Castan ,  Valerie Legrand ,  Remi Meyrueix ,  Gerard Soula

发明人： Catherine Castan ,  Valerie Legrand ,  Remi Meyrueix ,  Gerard Soula

IPC分类号： A61K9/14

CPC分类号： A61K9/5073 ,  A61K9/2081 ,  A61K9/4858 ,  A61K9/4866

摘要： The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability). To achieve this, the invention provides a composition comprising two controlled release systems associated in series, namely: individualised coated particles (microcapsules) of active principle forming an internal phase, the coating comprising a film-forming polymer P1 (ethylcellulose), a nitrogenous polymer (polyvinylpyrrolidone), a softener (castor oil) and a lubricant (magnesium stearate), and an external phase of functional carriers: polyelectrolytic hydrophilic polymer: (alginate), neutral hydrophilic polymer (hydroxypropylmethylcellulose) and a gelling additive (calcium acetate), said composition spontaneously forming in the presence of water, a cohesive and stable composite macroscopic solid, wherein the external continuous phase is a gelled matrix including the active principle microcapsules. The invention is useful for delayed oral galenic formulation of metformin.

摘要翻译： 本发明涉及用于口服给药的药物和/或营养活性成分的延长/受控释放的盖仑系统。 目的是提供一种能够以一个单一可耐受和可接受剂量的活性成分获得的系统，24小时以上的有效治疗保护（增加生物吸收时间而不影响生物利用度）。 为了实现这一目的，本发明提供了包含两个串联相关的控制释放系统的组合物，即形成内相的活性成分的单独的涂覆颗粒（微胶囊），该涂层包含成膜聚合物P 1 （乙基纤维素），含氮聚合物（聚乙烯吡咯烷酮），软化剂（蓖麻油）和润滑剂（硬脂酸镁）和功能性载体的外相：聚电解亲水性聚合物：（藻酸盐），中性亲水性聚合物（羟丙基甲基纤维素）和 凝胶添加剂（乙酸钙），所述组合物在水的存在下自发形成，粘性和稳定的复合宏观固体，其中外部连续相是包含活性成分微胶囊的凝胶基质。 本发明可用于二甲双胍延迟口服盖仑制剂。

公开(公告)号：US20070178126A1

公开(公告)日：2007-08-02

申请号：US11601691

申请日：2006-11-20

申请人： Stephanie Angot ,  You-Ping Chan ,  Gerard Soula

发明人： Stephanie Angot ,  You-Ping Chan ,  Gerard Soula

IPC分类号： A61K8/02

CPC分类号： A61K8/88 ,  A61K47/645 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08L51/04 ,  C08L77/00 ,  C08L77/02 ,  C08L77/06 ,  C08L2666/08 ,  C08L51/00

摘要： The invention relates to novel biodegradable polyamino acid based materials which can be used for the vectorization of (an) active substance(s) (PA). The invention also relates to novel pharmaceutical, cosmetic, dietary or phytosanitary compositions based on said polyamino acids. The present invention which primarily relates to polyamino acids comprising aspartic units and/or glutamic unites some of which bearing at least one graft, characterized in that at least one of said grafts is joined to an aspartic or glutamic unite by means of an amide bond and in that at least one of said grafts comprises at least one oligoamino acid which is Leu, and/or Ileu, and/or Val, and/or Phe based. Said amide function ensure better stability with respect to hydrolysis than similar products of prior art. Advantageously, said polymers can be easily and economically transformed into active substance vectorization particles, said particles being able to form stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及可用于（an）活性物质（PA）的向量化的新型可生物降解的聚氨基酸基材料。 本发明还涉及基于所述多氨基酸的新型药物，化妆品，膳食或植物检疫组合物。 本发明主要涉及包含天冬氨酸单元和/或谷氨酸单元的聚氨基酸，其中一些具有至少一个接枝物，其特征在于，所述移植物中的至少一个通过酰胺键与天冬氨酸或谷氨酸团结连接， 其中至少一个所述移植物包含至少一种Leu，和/或Ileu和/或Val和/或Phe基的寡氨基酸。 与现有技术的相似产物相比，所述酰胺功能确保了相对于水解的更好的稳定性。 有利地，所述聚合物可以容易且经济地转化成活性物质载体化颗粒，所述颗粒能够形成稳定的水性胶体悬浮液。

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。