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1.发明申请Microcapsules with modified release of active principles with low solubility for oral delivery 有权具有改进释放活性成分的微胶囊，具有低溶解性用于口服递送公开(公告)号：US20070160678A1
公开(公告)日：2007-07-12
申请号：US11583940
申请日：2006-10-20
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。
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公开(公告)号：US20070166378A1
公开(公告)日：2007-07-19
申请号：US11449675
申请日：2006-06-09
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.
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3.发明授权Oral medicinal product with modified release of at least one active principle in multimicrocapsular form 有权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
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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公开(公告)号：US20080026056A1
公开(公告)日：2008-01-31
申请号：US11631030
申请日：2005-05-25
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“？>
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公开(公告)号：US20070173464A1
公开(公告)日：2007-07-26
申请号：US11707034
申请日：2007-02-16
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。
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6.发明申请Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods 审中-公开卡维地洛游离碱，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。
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7.发明申请公开(公告)号：US20090220611A1
公开(公告)日：2009-09-03
申请号：US11992769
申请日：2006-09-27
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（EUDRAGITL100-55）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。
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公开(公告)号：US20090123536A1
公开(公告)日：2009-05-14
申请号：US11884534
申请日：2006-02-21
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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9.发明申请Oral Medicament For The Modified Release Of At Least One Active Principle, In Multimicrocapsule Form 审中-公开口服药物的修饰释放至少一个主动原则，在多微囊形式公开(公告)号：US20080305160A1
公开(公告)日：2008-12-11
申请号：US11791466
申请日：2005-11-02
IPC分类号： A61K9/52 , A61K9/26 , A61K31/585 , A61K31/4166 , A61K31/435 , A61K31/43 , A61K31/522
CPC分类号： A61K9/5031
摘要： The field of the invention is that of oral medicaments or pharmaceutical compositions, in particular of the type including one or more active principles. The aim of the invention is to provide an improved oral medicament to be administered in one or several daily doses and enabling the modified release of active principles (in particular of one active principle), whereby the prophylactic and therapeutic effectiveness of said medicament is improved. This aim is achieved by the oral multimicrocapsule galenic form according to the invention, in which the active principle release is controlled by a dual release trigger mechanism: “time-dependent trigger” and “pH-dependent trigger”. Said medicament includes microcapsules providing the modified release of the active principle, each comprising a core containing
摘要翻译： 本发明的领域是口服药物或药物组合物，特别是包括一种或多种活性成分的类型。 本发明的目的是提供一种或多种日剂量施用的改进的口服药物，并且能够改变释放活性成分（特别是一种活性成分），从而提高所述药物的预防和治疗效果。 该目的通过根据本发明的口服多微囊盖仑型形式实现，其中主动释放由双重释放触发机制控制：“时间依赖性触发”和“依赖于pH的触发”。 所述药物包括提供活性成分的改性释放的微胶囊，每个包含含有的核心
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10.发明申请Microcapsules with modified release of active principles with low solubility for oral delivery 审中-公开具有改进释放活性成分的微胶囊，具有低溶解性用于口服递送公开(公告)号：US20060275376A1
公开(公告)日：2006-12-07
申请号：US10522234
申请日：2003-07-28
CPC分类号： A61K9/5015 , A61K9/5026 , A61K9/5047
摘要： The invention concerns 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 (P1) 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 mraner 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 invention also concerns the uses of said microcapsules in galenic formulation.
摘要翻译： 本发明涉及用于可靠调节释放的微胶囊，并且适用于除抗高血糖剂以外的几乎不溶于水的活性成分的工业复制。所述微胶囊中的每一种都包含难溶的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（P1），水溶性聚合物（P2），增塑剂（PL）和任选的润滑表面活性剂（TA）。 所述涂膜占其总重量的至少4％p / p干燥颗粒。 及其部件P1，P2。 PL满足以下特征：相对于总涂层重量的40重量％至90重量％的PI的干重质量分数; PL / P1 + P2的干物质重量分数在15和60％之间：PL / P1 + P2的干物质重量分数范围在1％和30％之间。 本发明还涉及所述微胶囊在盖仑制剂中的用途。
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