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1. 发明申请

US20080152675A1 Dispersion of polyamino acids in a continuous lipid phase 审中-公开
标题翻译：聚氨基酸在连续脂质相中的分散
公开(公告)号：US20080152675A1
公开(公告)日：2008-06-26
申请号：US12003095
申请日：2007-12-20
申请人： Gauthier POULIQUEN
发明人： Gauthier POULIQUEN
IPC分类号： A61K47/32 , A61K47/36 , A61K9/107
CPC分类号： A61K47/36 , A61K9/107 , A61K47/34
摘要： The invention relates to injectable pharmaceutical compositions for the prolonged release of at least one active principle, comprising at least one active principle in an aqueous phase of amphiphilic polymer, said aqueous phase being in the form of a dispersion in a continuous lipid phase. The composition is in the form of a water-in-oil emulsion comprising: a pharmaceutically acceptable, continuous lipid phase, an aqueous disperse phase containing at least one amphiphilic polymer and at least one active principle not covalently bonded to said amphiphilic polymer, and at least one pharmaceutically acceptable surfactant.
摘要翻译：本发明涉及用于延长释放至少一种活性成分的可注射药物组合物，其包含至少一种活性成分在两亲性聚合物的水相中，所述水相以连续脂质相中的分散体的形式。该组合物为油包水型乳状液，其包含药学上可接受的连续脂质相，含有至少一种两亲聚合物的水分散相和至少一种不共价键合到所述两亲性聚合物的活性成分，以及在至少一种药学上可接受的表面

2. 发明申请

US20140105993A1 MODIFIED-RELEASE MICROPARTICLES BASED ON AMPHIPHILIC COPOLYMER AND ON ACTIVE PRINCIPLE(S) AND PHARMACEUTICAL FORMULATIONS COMPRISING THEM 审中-公开
标题翻译：基于AMPHIPHILIC共聚物和活性原料（S）和包含它们的药物制剂的改性释放微生物
公开(公告)号：US20140105993A1
公开(公告)日：2014-04-17
申请号：US14086635
申请日：2013-11-21
申请人： Flamel Technologies, S.A.
发明人： Alain Constancis , You-Ping Chan
IPC分类号： A61K47/42 , A61K9/16 , A61K38/28 , A61K38/27 , A61K38/21 , A61K38/20
CPC分类号： A61K47/42 , A61K9/0019 , A61K9/0075 , A61K9/1658 , A61K9/19 , A61K38/2013 , A61K38/212 , A61K38/27 , A61K38/28
摘要： The present invention relates to novel microparticles formed of amphiphilic polyamino acids which transport active principle(s), AP(s), in particular protein and peptide active principle(s), and to novel modified-release pharmaceutical formulations comprising said AP microparticles. Microparticles of amphiphilic polyamino acid (PO) may include at least one AP (associated noncovalently) which spontaneously form a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions. The microparticles may be obtained by atomization of a solution or colloidal suspension of PO comprising at least one AP, may have a size of between 0.5 and 100 microns, and may be dispersible in colloidal suspension.
摘要翻译：本发明涉及由两亲多聚氨基酸形成的新型微粒，其中所述两亲性聚氨基酸输送活性成分，特别是蛋白质和肽活性成分的AP，以及包含所述AP微粒的新型改性释放药物制剂。两亲性聚氨基酸（PO）的微粒可以包括至少一种AP（非共价相关的），其在等渗条件下自发形成纳米颗粒在水中的胶态悬浮液，pH 7.0。微粒可以通过雾化包含至少一种AP的PO的溶液或胶体悬浮液获得，其可以具有0.5至100微米的尺寸，并且可以分散在胶体悬浮液中。

3. 发明申请

US20100068291A1 Oral Medicament Based on a Proton Pump Inhibitor 审中-公开
标题翻译：基于质子泵抑制剂的口服药物
公开(公告)号：US20100068291A1
公开(公告)日：2010-03-18
申请号：US11920278
申请日：2006-05-15
申请人： Philippe CAISSE , Catherine CASTAN , Rémi MEYRUEIX , Gérard SOULA
发明人： Philippe CAISSE , Catherine CASTAN , Rémi MEYRUEIX , Gérard SOULA
IPC分类号： A61K9/50 , A61K31/4439 , A61K31/426 , A61K31/4164 , A61K31/341 , A61K47/02 , A61K47/06
CPC分类号： A61K9/5047 , A61K9/5015 , A61K9/5026 , A61K31/00 , A61K31/4184 , A61K31/4439
摘要： The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily. To this end, the microcapsules of the invention, preferably non-enteric, are constituted of PPI microparticles coated with ethyl cellulose, an ammonio methacrylate copolymer (Eudragit® RL 100), polyvinylpyrrolidone, castor oil and polyoxyethylenated hydrogenated castor oil (40). This medicament is designed so that after its ingestion for a once daily administration, it makes it possible to maintain, from the first day of treatment onward, an average gastric pH, between 0 and 24 h, of greater than or equal to the average gastric pH between 0 and 24 h obtained by an enteric oral medicament having a reference* immediate release, administered under the same conditions. The invention also relates to these microcapsules per se.
摘要翻译：本发明涉及具有特别可用于预防和治疗胃肠道疾病的质子泵抑制剂（PPI's）的改良释放的口服药物。本发明的目的是提供一种基于PPI的新型口服药物，其理想地具有以下所有或一些特征：a）通过在口服给药药物后增加胃pH，快速地向患者提供缓解; b）加速患者的恢复，同时在药物口服给药后，尽可能长时间地保持胃pH的增加，特别是在夜间; c）通过每天服用一次药物来改善患者的治疗和舒适度。为此，本发明的微胶囊优选为非肠溶性，由涂覆有乙基纤维素的PPI微粒，氨基甲基丙烯酸共聚物（RL100），聚乙烯吡咯烷酮，蓖麻油和聚氧乙烯化氢化蓖麻油（40）构成。这种药物被设计成使其在摄入一次每日给药后，可以从治疗的第一天开始维持0至24小时之间的平均胃pH大于或等于胃平均值通过具有参考*立即释放的肠溶口服药物在相同条件下给药获得的0至24小时的pH。本发明还涉及这些微胶囊本身。

4. 发明申请

US20090041838A1 Anti-Misuse Microparticulate Oral Drug Form 审中-公开
标题翻译：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）。

5. 发明申请

US20100266701A1 ANTI-MISUSE MICROPARTICULATE ORAL DRUG FORM 审中-公开
标题翻译：抗微生物口服药物形式
公开(公告)号：US20100266701A1
公开(公告)日：2010-10-21
申请号：US12560044
申请日：2009-09-15
申请人： Florence Guimberteau , Remi Meyrueix , Gerard Soula
发明人： Florence Guimberteau , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/14 , A61K31/52 , A61K31/155
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）。

6. 发明申请

US20090311315A1 Multimicroparticulate Oral Pharmaceutical Form with Modified Release of Angiotensin II Receptor Antagonists 审中-公开
标题翻译：具有血管紧张素II受体拮抗剂修饰释放的多重微量口服药物形式
公开(公告)号：US20090311315A1
公开(公告)日：2009-12-17
申请号：US11884549
申请日：2006-02-21
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix , Gérard Soula
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix , Gérard Soula
IPC分类号： A61K9/52 , A61K9/14 , A61K9/22 , A61K31/4178 , A61K31/4184 , A61K9/26
CPC分类号： A61K9/2081 , A61K9/5073 , A61K9/5078 , A61K9/5084 , A61K31/415 , A61K31/417
摘要： The invention relates to oral pharmaceutical forms with modified release of ARB, and to related treatments and delivery methods.The invention concerns a form with modified release of ARB which prolongs the bioabsorption time and enables the pharmaceutical form to be administered only once daily.Therefore, the invention is an oral pharmaceutical form with modified ARB release comprising a plurality of ARB microunits (mean diameter: 50-1000 μm) leading, after being taken, to a plasma profile wherein C18 h*≦C18 h, with C18 h=plasma ARB concentration, 18 h after being taken, C18 h*=plasma ARB concentration corresponding to C18 h and obtained under the same conditions as C18 h, with a reference immediate-release oral pharmaceutical form*, containing the same dose of ARB, Cmax=maximum plasma ARB concentration after being taken, Cmax*=maximum plasma ARB concentration corresponding to Cmax and obtained under the same conditions as Cmax, with a reference immediate-release oral pharmaceutical form*, containing the same dose of ARB.
摘要翻译：本发明涉及具有ARB修饰释放的口服药物形式，以及相关治疗和递送方法。本发明涉及延长生物吸收时间并延长药物形式每天只能施用一次的ARB的释放形式。因此，本发明是具有改良的ARB释放的口服药物形式，其包含多个ARB微单位（平均直径：50-1000μm），其被引导至血浆曲线，其中C18h * <= C18h，C18h =血浆ARB浓度，服用18小时后，C18h * =对应于C18h的血浆ARB浓度，并且在与C18h相同的条件下获得，含有相同剂量的ARB的参考速释口服药物形式* Cmax =服用后最大血浆ARB浓度，Cmax * =对应于Cmax的最大血浆ARB浓度，并且在与Cmax相同的条件下获得，含有相同剂量的ARB的参考即释释口服药物形式*。

7. 发明申请

US20090011028A1 Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
标题翻译：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。

8. 发明申请

US20120172220A1 N-PHOSPHONOMETHYLGLYCINE GUANIDINE DERIVATIVE SALTS 有权
标题翻译： N-膦酰基乙醇胺衍生物衍生物
公开(公告)号：US20120172220A1
公开(公告)日：2012-07-05
申请号：US13381457
申请日：2010-06-24
申请人： Ronald J. Brinker , Olivier Soula , Alain Lemercier
发明人： Ronald J. Brinker , Olivier Soula , Alain Lemercier
IPC分类号： A01N57/20 , C07C279/04 , C07C279/12 , C08G73/04 , A01N59/02 , A01N55/02 , A01P13/00 , C07F9/38 , A01N47/44
CPC分类号： A01N47/44 , A01N37/40 , A01N39/04 , A01N57/20 , C07C279/02 , C07C279/04 , C07C279/12 , C07C279/20 , C07F9/3813 , C07F9/3817 , C08G73/0206 , A01N2300/00
摘要： The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
摘要翻译：本发明提供N-膦酰基甲基甘氨酸胍盐。 N-膦酰基甲基甘氨酸胍盐具有比单独的草甘膦更好的除草效力。本发明还提供胍化合物及其盐。

9. 发明申请

US20110159088A1 ORAL PHARMACEUTICAL FOR BASED ON AT LEAST ONE ACTIVE PRINCIPLE WHOSE SOLUBILITY VARIES AS A FUNCTION OF THE GASTRIC pH CONDITIONS 审中-公开
标题翻译：基于至少一个活性原理的口服药物，其溶解度变量作为pH条件的函数
公开(公告)号：US20110159088A1
公开(公告)日：2011-06-30
申请号：US11920741
申请日：2006-05-24
申请人： Florence Guimberteau , Gérard Soula
发明人： Florence Guimberteau , Gérard Soula
IPC分类号： A61K9/52 , A61K9/00 , A61K9/28 , A61K31/4178 , A61K31/41 , A61K31/522 , A61P3/00 , A61P9/00 , A61P31/00 , A61P35/00 , A61P25/00
CPC分类号： A61K9/5026 , A61K9/5078
摘要： The field of the present invention is that of oral pharmaceutical forms of at least one active principle AP whose solubility varies greatly as a function of the gastric pH, and also treatments and administration methods relating thereto.The invention relates to the use, in an oral pharmaceutical form comprising AP, of a coating or of a matrix including the said AP and allowing the controlled release of the said AP, in order for this form administered orally to a sample of individuals to lead, irrespective of the fed or fasted state of the individuals, to a reduction in the inter- and/or intra-individual standard deviation of the Cmax, which makes it possible to ensure lower variability of the efficacy and of the therapeutic safety of the pharmaceutical form, compared with an immediate-release AP pharmaceutical form administered to this same sample of individuals, at the same dose.
摘要翻译：本发明的领域是口服药物形式的至少一种活性成分AP，其溶解度随着胃pH的变化而变化很大，以及与之有关的治疗和给药方法。本发明涉及以包含AP的口服药物形式的包衣或包含所述AP的基质并允许所述AP的受控释放的用途，以便将该形式口服给予个体样品以引导，无论个体的喂养状态或禁食状态如何，降低Cmax的个体间和/或个体内标准偏差，这使得可以确保药物的功效和治疗安全性的较低变异性形式，与以相同剂量施用于该相同样品的立即释放的AP药物形式相比。

10. 发明申请

US20090291137A1 Solid oral form provided with a double release profile 审中-公开
标题翻译：固体口服形式提供双重释放特征
公开(公告)号：US20090291137A1
公开(公告)日：2009-11-26
申请号：US12425875
申请日：2009-04-17
申请人： Florence Guimberteau , Anne-Sophie Daviaud
发明人： Florence Guimberteau , Anne-Sophie Daviaud
IPC分类号： A61K9/26 , A61K9/14
CPC分类号： A61K9/2081 , A61K9/5026 , A61K9/5047 , A61K9/5078 , A61K9/5084
摘要： The present invention relates to a solid form, intended for the administration by oral route of at least one active ingredient and capable of guaranteeing a double release mechanism of said active ingredient, the first being determined by time and the second being determined by the pH, characterized in that said active ingredient is present there in the form of a microparticle system the microparticles of which possess a core formed wholly or partly by said active ingredient and coated with at least one layer determining said release profile of said active ingredient and formed by a material composed at least (i) 25 to 75% by weight relative to the total weight of said coating of at least one polymer A which is insoluble in the gastro-intestinal fluids, (ii) 25 to 75% by weight relative to the total weight of said coating of at least one polymer B possessing a solubilization pH value comprised within the pH range from 5 to 7, and (iii) 0 to 25% by weight relative to the total weight of said coating of at least one plasticizer, said polymers A and B being present in a polymer(s) B/polymer(s) A weight ratio at least equal to 0.25It moreover relates to a method for the preparation of this solid form and of the corresponding microparticles.
摘要翻译：本发明涉及一种固体形式，其用于通过口服途径施用至少一种活性成分并且能够保证所述活性成分的双重释放机制，第一种是由时间确定的，而第二种由pH决定，其特征在于所述活性成分以微粒系统的形式存在，其微粒具有完全或部分由所述活性成分形成的核，并涂覆有至少一层，其确定所述活性成分的所述释放曲线并由相对于不溶于胃肠液的至少一种聚合物A的至少一种聚合物A的总重量的至少（i）25至75重量％的材料，（ii）相对于总量的25至75重量％至少一种聚合物B的所述涂层的重量，其具有包含在5至7的pH范围内的增溶pH值，和（iii）0至25重量％，相对于所述的至少一种增塑剂的涂层，所述聚合物A和B存在于聚合物B /聚合物A中，至少等于0.25的重量比。此外，还涉及制备该固体形式和相应的微粒。

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