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1. 发明申请

US20070166378A1 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.

2. 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。

3. 发明授权

US08197850B2 Medicine based on anti-hyperglycaemic microcapsules with prolonged release and method for preparing same 失效
标题翻译：基于抗高血糖微胶囊延长释药的药物及其制备方法
公开(公告)号：US08197850B2
公开(公告)日：2012-06-12
申请号：US10415850
申请日：2001-11-19
申请人： Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/14
CPC分类号： A61K31/155 , A61K9/5015 , A61K9/5047 , A61K31/00
摘要： The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine. The invention is applicable to the treatment of type II diabetes.
摘要翻译：本发明涉及用于延长释放抗高血糖（二甲双胍）活性成分的口服盖仑制剂。所述药物通过克服吸收窗旁路的问题和主动原理的大量局部释放，能够在24小时内获得有效的治疗保护。因此，所述药物包含数千种抗高血糖（二甲双胍）微胶囊，每个微胶囊由包含至少抗高血糖剂的芯和涂覆在芯上的涂膜构成，并且能够在体内延长抗高血糖剂的释放。所述微胶囊具有在50和100微米之间的粒度分布。运输动力学和生物利用度的重现性非常高。结果，患者血糖过低或低血糖的风险较小。本发明还涉及所述药物的制备以及多种所述微胶囊用于制备抗高血糖药物的用途。本发明适用于II型糖尿病的治疗。

4. 发明申请

US20080026056A1 Antibiotic-Based Pharmaceutical Formulation in Microcapsular Form 审中-公开
标题翻译：基于抗微生物剂的药物制剂
公开(公告)号：US20080026056A1
公开(公告)日：2008-01-31
申请号：US11631030
申请日：2005-05-25
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： A61K9/50 , A61K31/43 , A61P31/04
CPC分类号： A61K9/5084 , A61K9/5047 , A61K31/43
摘要： The invention relates to oral antibiotic drugs. The object of the invention is to limit or even stop the increase in antibiotic resistance without sacrificing the requirements of (a) increased efficacy of oral antibiotics, particularly for pediatric applications, (b) tolerance, (c) broad spectra of activity, and (d) good patient compliance. This object is achieved by the invention, which proposes the use of modified-release microcapsules, comprising a core that contains at least one active principle AP1 formed of at least one antibiotic, and a coating for said core that governs the modified release of said active principle, for the manufacture of a drinkable or orally dispersible antibiotic pharmaceutical formulation that makes it possible to limit the increase in the antibiotic resistance of the target germs, this formulation being: capable of administration in one or two, preferably two, intakes per day, and definable as follows, relative to an immediate-release oral formulation (IRF*) comprising at least one active principle API, and for the same dose D of API as IRF*: Tmic>T*micof IRF*
摘要翻译：本发明涉及口服抗生素药物。本发明的目的是限制或甚至阻止抗生素耐药性的增加，而不会牺牲（a）口服抗生素的功效增加，特别是儿科应用的要求，（b）耐受性，（c）活性的广谱谱和（ d）良好的患者依从性。该目的是通过本发明来实现的，本发明提出使用包含至少一种由至少一种抗生素形成的至少一种活性成分AP1的芯的改性释放微胶囊和用于所述核心的涂层，所述涂层控制所述活性物质的修饰释放原理，用于制造可以限制目标细菌的抗生素抗性增加的可饮用或口服分散的抗生素药物制剂，该制剂是：能够每天摄入一次或两次，优选两次，并且可定义如下，相对于包含至少一种活性成分API的立即释放口服制剂（IRF *），和与IRF *相同的API剂量D：<？in-line-formula description =“In-line IRF *的公式“end =”lead“？> T > T * 在线公式描述=”在线公式“end =” 尾巴“？>

5. 发明申请

US20070173464A1 Oral ribavirin pharmaceutical compositions 审中-公开
标题翻译：口服利巴韦林药物组合物
公开(公告)号：US20070173464A1
公开(公告)日：2007-07-26
申请号：US11707034
申请日：2007-02-16
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.
摘要翻译：本发明涉及用于预防和/或治疗病毒性疾病的口服药物组合物。本发明还涉及使用这些口服组合物预防和/或治疗这些病毒性疾病的方法。本发明中考虑的主要问题之一是提高抗病毒治疗的效率，特别是通过利巴韦林（例如与干扰素组合）来抗丙型肝炎病毒。根据本发明的口服利巴韦林抗病毒组合物增加了利巴韦林的生物吸收时间，从而改善了患者的治疗。所述组合物包含至少一种改进释放形式的利巴韦林，其生物吸收时间BAT大于以相同剂量施用的参考*立即释放形式的利巴韦林的生物吸收时间BAT *; BAT优选包含2至15小时，更优选4至12小时。所述组合物是储层型或矩阵型。所述组合物是胃保持系统或多颗粒形式。

6. 发明申请

US20070207214A1 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：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。

7. 发明申请

US20050175695A1 Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods 审中-公开
标题翻译：卡维地洛游离碱，盐，无水形式或溶剂化物，相应的药物组合物，控制释放制剂和治疗或递送方法
公开(公告)号：US20050175695A1
公开(公告)日：2005-08-11
申请号：US10997836
申请日：2004-11-24
申请人： Catherine Castan , Patrick Crowley , Florence Guimberteau , Remi Meyrueix , Chooh Oh , Gerard Soula
发明人： Catherine Castan , Patrick Crowley , Florence Guimberteau , Remi Meyrueix , Chooh Oh , Gerard Soula
IPC分类号： A61K20060101 , A61K9/16 , A61K9/22 , A61K9/50 , A61K31/403
CPC分类号： A61K9/1635 , A61K9/1641 , A61K9/1658 , A61K9/2077 , A61K31/403
摘要： The present invention also relates to carvedilol free base, carvedilol salts, anhydrous forms, or solvates thereof, corresponding pharmaceutical compositions or controlled release formulations, and delivery or dosing methods of carvedilol forms to the lower gastrointestingal tract or methods to treat cardiovascular diseases, which may include, but are not limited to hypertension, congestive heart failure, atherosclerosis, and angina. The present invention relates to controlled release formulations, which comprise various carvedilol forms, which may include, but are not limited to a carvedilol free base or corresponding carvedilol salts, anhydrous forms or solvates thereof.
摘要翻译：本发明还涉及卡维地洛游离碱，卡维地洛盐，无水形式或其溶剂合物，相应的药物组合物或控释制剂，以及卡维地洛形式向下胃肠道输送或给药方法或治疗心血管疾病的方法，包括但不限于高血压，充血性心力衰竭，动脉粥样硬化和心绞痛。本发明涉及包含各种卡维地洛形式的控释制剂，其可以包括但不限于卡维地洛游离碱或相应的卡维地洛盐，无水形式或溶剂化物。

8. 发明申请

US20050037077A1 Galenic microparticulate oral formulation for delayed and controlled release of pharmaceutical active principles 审中-公开
标题翻译：用于延迟和控制释放药物活性成分的Galenic微粒口服制剂
公开(公告)号：US20050037077A1
公开(公告)日：2005-02-17
申请号：US10492129
申请日：2002-10-09
申请人： Valerie Legrand , Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Valerie Legrand , Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/14 , A61K9/22 , A61K9/26 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/155 , A61K31/522 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/36 , A61K47/38 , A61P3/10 , A61P7/02 , A61P15/18 , A61P25/00 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12
CPC分类号： A61K9/5078
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 consists 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，其活性成分在体内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“。该系统由包含涂覆有包含亲水性聚合物A（EudragitL）和疏水性化合物B（植物蜡，熔点）的膜（最大40重量％））的AP芯组成的微胶囊（200至600μm） = 40-90℃），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. 发明申请

US20090220611A1 Microparticles With Modified Release of At Least One Active Principle and Oral Pharmaceutical Form Comprising Same 审中-公开
标题翻译：微粒修饰释放至少一个主动原理和口服药物组成
公开(公告)号：US20090220611A1
公开(公告)日：2009-09-03
申请号：US11992769
申请日：2006-09-27
申请人： Frederic Dargelas , Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Frederic Dargelas , Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/16
CPC分类号： A61K9/5073 , A61K9/2077
摘要： The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel pharmaceutical with time-dependent and pH-dependent release mechanism, enabling: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®). The invention also concerns medicines based on said microparticles.
摘要翻译：本发明涉及具有口腔活性成分释放的微粒体系。本发明旨在提供具有时间依赖性和pH依赖性释放机制的新型药物，其能够：a）在胃中释放活性成分之前的潜伏期; b）pH触发在肠中释放活性成分; c）有效原理的释放速度。这通过使用由各自涂覆有两个涂膜A和B的活性成分的颗粒制成的涂覆微粒来实现.A包括：不溶于胃肠道流体的成膜（共）聚合物（A1）可溶于胃肠道液体的乙基纤维素（共）聚合物（A2）; 增塑聚乙烯吡咯烷酮（A3）; 蓖麻油/任选的表面活性剂和/或硬脂酸镁润滑剂（A4）。 B包含具有中性pH（EUDRAGITL100-55）和疏水性化合物（B2）（LUBRITAB）的离子化基团的亲水性聚合物（B1）。本发明还涉及基于所述微粒的药物。

10. 发明申请

US20090123536A1 Oral Pharmaceutical Form of Losartan 审中-公开
标题翻译：氯沙坦的口服药物形式
公开(公告)号：US20090123536A1
公开(公告)日：2009-05-14
申请号：US11884534
申请日：2006-02-21
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： A61K9/54 , A61K31/4178 , A61K9/16 , A61K9/26
CPC分类号： A61K9/5084 , A61K9/2081 , A61K9/5073 , A61K9/5078 , A61K31/417
摘要： The field of the present invention is that of oral pharmaceutical forms of losartan, and also treatments and administration methods relating thereto.The invention relates to the use, in an oral pharmaceutical form comprising losartan, of a coating or matrix including said losartan and allowing controlled release of said losartan, such that this form orally administered to a sample of individuals leads, irrespective of the fed or fasted state of the individuals, to a reduction of the interindividual standard deviation of the Cmax, which ensures lower variability of the efficacy and of the therapeutic safety of the pharmaceutical form relative to an immediate-release pharmaceutical form of losartan administered to this same sample of individuals, at the same dose.Another aim of the invention is to provide an oral pharmaceutical form of losartan that can be administered once a day and that is just as effective as the “one dose intake per day” forms and the “two dose intakes per day” forms.The invention is thus a modified-release oral pharmaceutical form of losartan comprising a plurality of losartan microunits (mean diameter: 50-1000 μm) making it possible to obtain, after a dose intake, a plasmatic profile of the type shown in FIG. 10.
摘要翻译：本发明的领域是氯沙坦的口服药物形式，以及与其有关的治疗和给药方法。本发明涉及以包含氯沙坦的口服药物形式使用包含所述氯沙坦的包衣或基质并允许控制释放所述氯沙坦的方法，使得该形式经口给予个体样品导致，不管进食或禁食个体的状态，减少Cmax的个体间标准差，其确保药物形式相对于施用于该相同个体样品的立即释放药物形式的氯沙坦的功效和治疗安全性的较低变异性，以相同的剂量。本发明的另一个目的是提供一种可以每天一次给药的氯沙坦的口服药物形式，并且与“每天一次剂量摄取”形式和“每日两次摄入量”形成同样有效。因此，本发明是包含多个氯沙坦微单位（平均直径：50-1000μm）的氯沙坦的改进释放的口服药物形式，使得可以在剂量摄取后获得图1所示类型的血浆谱。 10。

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