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31.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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32.发明申请公开(公告)号：US20070196497A1
公开(公告)日：2007-08-23
申请号：US10580023
申请日：2004-11-19
IPC分类号： A61K9/14
CPC分类号： A61K9/0024 , A61K38/2013 , A61K38/212 , A61K47/42 , A61K47/645 , A61K51/1217
摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of active principle(s), particularly protein active principle(s), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of active principle(s) that makes it possible, after parenteral injection, to increase significantly the in vivo release time of a therapeutic protein while at the same time reducing the plasma concentration peak of the active protein, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance. The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one active principle (AP) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.
摘要翻译： 本发明涉及基于用于延长释放活性成分（特别是蛋白质活性成分）的稳定的流体水性胶体悬浮液以及这些制剂的应用，特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放活性成分的流体药物制剂，其使得在胃肠外注射后可以显着增加治疗性蛋白质的体内释放时间，同时减少 活性蛋白质的血浆浓度峰值，所述制剂还在储存时稳定，并且还具有生物相容性，可生物降解，无毒和非免疫原性并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团（HG）的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶体悬浮液，所述颗粒与至少一种活性成分（AP）非共价缔合并形成 在注射部位的凝胶沉积物，这种胶凝是由存在于生理介质中的蛋白质引起的。
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33.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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公开(公告)号：US20060165808A1
公开(公告)日：2006-07-27
申请号：US10519641
申请日：2003-06-24
CPC分类号： A61K9/5015 , A61K9/5026 , A61K9/5078 , A61K31/405
摘要： The present invention relates to A microcapsule composition allowing the delayed and controlled release of perindopril, or of a pharmaceutically acceptable salt thereof, for administration by the oral route.
摘要翻译： 本发明涉及一种微胶囊组合物，其允许延迟和控制释放培哚普利或其药学上可接受的盐，用于通过口服途径施用。
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35.发明申请Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s) 有权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：US20060165807A1
公开(公告)日：2006-07-27
申请号：US10510643
申请日：2003-04-07
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 ）。
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36.发明申请Carvedilol salts, anhydrates and/or solvate thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods 有权卡维地洛盐，其水合物和/或溶剂合物，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：US20050196459A1
公开(公告)日：2005-09-08
申请号：US10996780
申请日：2004-11-24
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 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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37.发明授权Optionally oriented, monomeric and polymeric nonlinearly optically active materials and derivatives thereof 失效任选取向的单体和聚合物非线性光学活性材料及其衍生物
公开(公告)号：US5444136A
公开(公告)日：1995-08-22
申请号：US213090
申请日：1994-03-15
申请人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
发明人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
IPC分类号： C08F20/60 , C07D207/44 , C07D207/452 , C07D207/456 , C08F20/52 , C08F22/36 , C08F22/40 , C08G73/10 , C08G73/14 , G02F1/35 , G02F1/355 , G02F1/361 , G03F7/027 , C08F226/06
CPC分类号： C07D207/452 , C07D207/456 , C08G73/1067 , C08G73/14 , G02F1/361 , G03F7/027
摘要： Nonlinearly optically active monomer species comprising at least two carbon-carbon activated double bonds, i.e., the polymerization of which is facilitated by the presence of an electron attracting function, and a non-centrosymmetric system of pi (.pi.) conjugated bonds bearing at least one electron attracting group on one terminal thereof and at least one electron donor group on the other terminal, are readily (co)polymerized and optionally oriented and crosslinked into shaped articles well adopted for the manufacture of a variety of electrooptical devices; such monomer species can have, for example, the following structural formula (I): ##STR1##
摘要翻译： 包含至少两个碳 - 碳活化双键的非线性光学活性单体物质，即其聚合通过存在吸电子功能而促进，以及带有至少一个的π（π）共轭键的非中心对称体系 其一端上的吸电子基团和另一个末端上的至少一个电子给体基团容易（共）聚合并任选取向并交联成良好地用于制造各种电光器件的成形制品; 这样的单体物质可以具有例如以下结构式（I）：
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