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1. 发明申请

US20110117205A1 ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AQUEOUS SUSPENSION FOR MODIFIED RELEASE OF ACTIVE PRINCIPLE(S) 有权
标题翻译：用于改性活性原料释放的水性悬浮剂形式的口服药物制剂（S）
公开(公告)号：US20110117205A1
公开(公告)日：2011-05-19
申请号：US13014137
申请日：2011-01-26
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
IPC分类号： A61K9/62 , A61K9/58 , A61K31/522 , A61K31/58 , A61K31/155
CPC分类号： A61K9/5047 , A61K9/0053 , A61K9/0095 , A61K9/10 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K31/155 , A61K31/192 , A61K31/43 , A61K31/522 , A61K31/585
摘要： The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) 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 active principle, this liquid phase furthermore being saturated with active principle(s).
摘要翻译：本发明涉及用于口服给药的液体药物制剂，其具有活性成分的释放，不包括阿莫西林，所述制剂由活性成分的包被颗粒（微胶囊）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改变的分布的活性成分的改性释放。为此，本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活性成分的改性释放性质，该液相还饱和具有积极的原则。

2. 发明授权

US07910133B2 Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin 失效
标题翻译：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：US07910133B2
公开(公告)日：2011-03-22
申请号：US10510621
申请日：2003-04-07
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
IPC分类号： A61K9/14 , A61K9/16 , A61K9/40
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

3. 发明授权

US07906145B2 Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s) 有权
标题翻译：用于修饰释放活性成分的水性悬浮液形式的口服药物制剂
公开(公告)号：US07906145B2
公开(公告)日：2011-03-15
申请号：US10510643
申请日：2003-04-07
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
IPC分类号： A61K9/14 , A61K9/16 , A61K9/40
CPC分类号： A61K9/5047 , A61K9/0053 , A61K9/0095 , A61K9/10 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K31/155 , A61K31/192 , A61K31/43 , A61K31/522 , A61K31/585
摘要： The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of active principle(s) excluding amoxicillin and consisting of suspensions of coated particles of active principles (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of the active principle(s), in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of the active principle, said liquid phase being furthermore saturated with active principle(s).
摘要翻译：本发明涉及用于口服递送的液体药物制剂，其具有除阿莫西林以外的活性成分的改进释放，并且由活性成分的包被颗粒（微胶囊）的悬浮液组成。根据本发明，构成悬浮液分散相的微胶囊根据在液体悬浮体的保质期内保持不变的轮廓来实现活性成分的改性释放。因此，本发明在于选择由至少四种组分组成的微胶囊特性的涂料组合物，所述组合物能够在水中保存所述微胶囊，而不改变其活性成分的改性释放性质，所述液相还用活性成分）。

4. 发明授权

US10004693B2 Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s) 有权
公开(公告)号：US10004693B2
公开(公告)日：2018-06-26
申请号：US13014137
申请日：2011-01-26
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
IPC分类号： A61K9/50 , A61K31/522 , A61K9/10 , A61K9/00 , A61K31/585 , A61K31/155 , A61K31/192 , A61K31/43
CPC分类号： A61K9/5047 , A61K9/0053 , A61K9/0095 , A61K9/10 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K31/155 , A61K31/192 , A61K31/43 , A61K31/522 , A61K31/585
摘要： The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) 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 active principle, this liquid phase furthermore being saturated with active principle(s).

5. 发明授权

US08652523B2 Oral pharmaceutical formulation in the form of a plurality of microcapsules for prolonged release of active principle(s) with slow solubility 有权
标题翻译：多种微胶囊形式的口服药物制剂，用于延长释放缓慢溶解度的活性成分
公开(公告)号：US08652523B2
公开(公告)日：2014-02-18
申请号：US10522252
申请日：2003-07-28
申请人： Florence Guimberteau , Catherine Castan , Rémi Meyrueix
发明人： Florence Guimberteau , Catherine Castan , Rémi Meyrueix
IPC分类号： A61K9/14 , A61K9/16
CPC分类号： A61K9/5047 , A61K9/5015 , A61K9/5026 , A61K9/5078
摘要： The invention concerns microcapsules with prolonged release of active principles with low solubility, consisting of a core containing the active principle and coated with a polymer layer which controls the release of the active principle. The aim is that said oral microcapsules containing hardly soluble active principles, should have a coating film of sufficient thickness to ensure controlled permeability and should be adapted to industrial reproduction. This is achieved by the inventive microcapsules of mean diameter less than 1000 microns, and whereof the coating film contains a film-forming polymer (P1) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said microcapsules are characterized in that their coating films represents at least 3% p/p of dry matter, relative to their total weight and their core contains a hardly soluble active principle and a solubilizing agent (polyoxyethylene hydrogenated castor oil) which provides the core wherein it is contained with properties such that the behavior of the exposed core (non-coated) in a given dissolving test (TD), is as follows: release of 80% of active principle in less than two hours. The invention also concerns the use of such microcapsules in galenic formulation.
摘要翻译：本发明涉及具有低溶解度的活性成分的延长释放的微胶囊，其由含有活性成分的核心组成并涂覆有控制活性成分释放的聚合物层。目的是所述含有难溶性活性成分的口服微胶囊应具有足够厚度的涂膜以确保受控的渗透性，并且应适于工业繁殖。这通过本发明的平均直径小于1000微米的微胶囊实现，并且其中的涂膜含有不溶于胃肠道液体的成膜聚合物（P1），水溶性聚合物（P2），增塑剂（PL），和任选的润滑表面活性剂（TA）。所述微胶囊的特征在于，它们的涂膜相对于它们的总重量表示至少3％的干物质的p / p，并且它们的芯含有难溶的活性成分和提供核的增溶剂（聚氧乙烯氢化蓖麻油），其中含有这样的性质，使得在给定的溶解试验（TD）中暴露的芯（未涂覆）的行为如下：在少于两小时内释放80％的活性成分。本发明还涉及这种微胶囊在盖仑制剂中的用途。

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

US20110129539A1 ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AN AQUEOUS SUSPENSION OF MICROCAPSULES FOR MODIFIED RELEASE OF AMOXICILLIN 审中-公开
标题翻译：氨苄青霉素修饰释放微球悬浮液形式的口服药物制剂
公开(公告)号：US20110129539A1
公开(公告)日：2011-06-02
申请号：US13024835
申请日：2011-02-10
申请人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Rémi Meyrueix
IPC分类号： A61K9/50 , A61K31/43 , A61P31/04
CPC分类号： A61K9/5015 , A61K9/5026 , A61K9/5047 , A61K31/43
摘要： The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of amoxicillin and consisting of suspensions of coated particles of amoxicillin (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of amoxicillin, in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of amoxicillin, said liquid phase being furthermore saturated with amoxicillin.
摘要翻译：本发明涉及用于口服递送的液体药物制剂，其具有阿莫西林的改良释放并由阿莫西林（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根据在液体悬液的保质期内保持不变的轮廓来实现阿莫西林的改进释放。因此，本发明在于选择由至少四种组分组成的微胶囊特异性的涂料组合物，其能够在水中保存所述微胶囊，而不改变其改性释放阿莫西林的性质，所述液相还用阿莫西林进行饱和。

8. 发明授权

US08101209B2 Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles 有权
标题翻译：用于延迟和控制释放药物活性成分的微孔口服盖仑形式
公开(公告)号：US08101209B2
公开(公告)日：2012-01-24
申请号：US10826690
申请日：2004-04-19
申请人： Valérie Legrand , Catherine Castan , Rémi Meyrueix , Gérard Soula
发明人： Valérie Legrand , Catherine Castan , Rémi Meyrueix , Gérard Soula
IPC分类号： A61K9/16 , A61K9/50
CPC分类号： A61K9/5078 , A61K9/5015 , A61K9/5026 , Y10S514/951 , Y10S514/963 , Y10S514/965
摘要： The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 μm) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
摘要翻译：本发明涉及一种用于延迟和控制释放活性成分（AP）的微粒体系，其活性成分体系中的吸收窗口基本上限于胃肠道的上部，该系统用于口服给药。本发明的目的是提供一种确保通过“时间依赖”和“依赖于pH”释放的双重机制确定地释放AP的系统。为了实现该目的，本发明提出了一种多微囊口服盖仑型，其设计以保证治疗功效，并且其中AP的释放由双时间触发机制（“触发时间”和“pH- 触发“。该系统包括微胶囊（200至600μm），其包含涂覆有包含亲水性聚合物A（Eudragit L）和疏水化合物B（植物蜡，熔点= 40）的膜（最大40重量％））的AP芯 -90℃），B / A在0.2和1.5之间。这些微胶囊在体外具有溶解行为，使得在1.4的恒定pH下，观察到1至5小时的潜伏期，随后释放AP，并且使得从pH1.4变为pH6.8的结果在AP的释放中没有潜伏期在体外。

9. 发明授权

US07879362B2 Oral pharmaceutical compositions with controlled release and prolonged absorption 有权
标题翻译：具有控制释放和延长吸收的口服药物组合物
公开(公告)号：US07879362B2
公开(公告)日：2011-02-01
申请号：US11723553
申请日：2007-03-21
申请人： Catherine Castan , Valerie Legrand , Rémi Meyrueix , Gérard Soula
发明人： Catherine Castan , Valerie Legrand , Rémi Meyrueix , Gérard Soula
IPC分类号： A61K9/16
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）。为了实现这一点，本发明提供了一种组合物，其包含两个串联的控制释放系统，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P1（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）和胶凝添加剂（乙酸钙），所述在水的存在下自发形成的组合物，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。

10. 发明授权

US08734850B2 Oral medicinal product with modified release of at least one active principle in multimicrocapsular form 有权
标题翻译：具有多微囊形式的至少一种活性成分释放的口服药物
公开(公告)号：US08734850B2
公开(公告)日：2014-05-27
申请号：US10996780
申请日：2004-11-24
申请人： Catherine Castan , Florence Guimberteau , Remi Meyrueix , Gerard Soula
发明人： Catherine Castan , Florence Guimberteau , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/16 , A61K9/22
CPC分类号： A61K9/1635 , A61K9/1641 , A61K9/1658 , A61K9/2077 , A61K31/403
摘要： The field of the invention is that of oral pharmaceutical medicinal products or compositions, more particularly of the type of those comprising one or more active principles.The aim of the invention is to provide an improved oral medicinal product that can be administered in one or more daily doses, with modified release of active principle (in particular an active principle), for improving the prophylactic and therapeutic efficacy of such a medicinal product.This aim is achieved by means of the multimicrocapsular oral pharmaceutical form according to the invention in which the release of the AP is controlled by means of a double mechanism of triggering the release: “time triggering” and “pH triggering”. This medicinal product comprises microcapsules with modified release of active principle, each containing a core comprising the active principle and one or more swelling agents, and at least one coating making possible the modified release of the active principle.
摘要翻译：本发明的领域是口服药物药物产品或组合物的领域，更特别是包含一种或多种活性成分的那些类型。本发明的目的是提供一种改进的口服药物产品，其可以以一种或多种日剂量施用，具有改进的活性成分释放（特别是活性成分），用于改善这种药物的预防和治疗功效。该目的通过根据本发明的多微囊口服药物形式实现，其中AP的释放通过触发释放的双重机制来控制：“时间触发”和“pH触发”。这种药用产品包括具有活性成分释放的微胶囊，每个微胶囊含有包含活性成分的核心和一种或多种溶胀剂，以及至少一种使活性成分的修饰释放成为可能的涂层。

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