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    Anti-misuse microparticulate oral pharmaceutical form
    1.
    发明授权
    Anti-misuse microparticulate oral pharmaceutical form 有权
    反滥用微粒口服药物形式

    公开(公告)号：US08445023B2

    公开(公告)日：2013-05-21

    申请号：US12638739

    申请日：2009-12-15

    Applicant: Florence Guimberteau ,  Frederic Dargelas

    Inventor： Florence Guimberteau ,  Frederic Dargelas

    IPC: A61K9/16

    CPC classification number: A61K9/5021 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/4866 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/485 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38 ,  A61K47/44

    Abstract: The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain.The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs.The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.

    Abstract translation: 本发明涉及固体微粒口服药物形式，其组成和结构使得可以避免滥用其含有的药物活性成分（AP）。 本发明的目的是为了防止固体口服药物被用于除主管公共卫生当局正式批准的治疗用途之外的任何用途。 换句话说，目的是避免自愿或非自愿滥用固体口服药物。 本发明涉及一种固体口服药物形式，其特征在于其含有抗滥用手段，因为其包含的至少部分AP包含在用于AP的改性释放的包被微粒中，并且其中涂覆的微粒 AP具有涂层（Ra），其确保AP的改性释放并同时赋予AP的涂覆微粒耐破碎性，从而避免误用。

    ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AQUEOUS SUSPENSION FOR MODIFIED RELEASE OF ACTIVE PRINCIPLE(S)
    2.
    发明申请
    ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AQUEOUS SUSPENSION FOR MODIFIED RELEASE OF ACTIVE PRINCIPLE(S) 有权
    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

    Applicant: Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

    Inventor： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

    IPC: A61K9/62 ,  A61K9/58 ,  A61K31/522 ,  A61K31/58 ,  A61K31/155

    CPC classification number: A61K9/5047 ,  A61K9/0053 ,  A61K9/0095 ,  A61K9/10 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5042 ,  A61K31/155 ,  A61K31/192 ,  A61K31/43 ,  A61K31/522 ,  A61K31/585

    Abstract: 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).

    Abstract translation: 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。

    Oral ribavirin pharmaceutical compositions
    3.
    发明申请
    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

    Applicant: Florence Guimberteau ,  Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

    Inventor： Florence Guimberteau ,  Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

    IPC: A61K31/7056 ,  A61K9/22

    CPC classification number: A61K9/5026 ,  A61K9/2077 ,  A61K9/48 ,  A61K9/5042 ,  A61K31/7056

    Abstract: 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.

    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin
    4.
    发明申请
    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin 失效
    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：US20060110463A1

    公开(公告)日：2006-05-25

    申请号：US10510621

    申请日：2003-04-07

    Applicant: Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix

    Inventor： Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix

    IPC: A61K31/43 ,  A61K9/50 ,  A61K9/16

    CPC classification number: A61K9/5015 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/43

    Abstract: 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.

    Abstract translation: 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

    Oral dosage form comprising an antimisuse system
    6.
    发明授权
    Oral dosage form comprising an antimisuse system 有权
    包含抗炎系统的口服剂型

    公开(公告)号：US08895063B2

    公开(公告)日：2014-11-25

    申请号：US11651577

    申请日：2007-01-10

    Applicant: Florence Guimberteau ,  Frederic Dargelas ,  Gérard Soula ,  Rémi Soula

    Inventor： Florence Guimberteau ,  Frederic Dargelas ,  Gérard Soula ,  Rémi Soula

    IPC: A61K8/20 ,  A61K9/50 ,  A61K45/06 ,  A61K33/30 ,  A61K33/26 ,  A61K33/06 ,  A61K9/48

    CPC classification number: A61K9/5047 ,  A61K9/4825 ,  A61K9/5078 ,  A61K9/5084 ,  A61K33/06 ,  A61K33/26 ,  A61K33/30 ,  A61K45/06 ,  A61K2300/00

    Abstract: An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents.Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.

    Abstract translation: 含有一种或多种具有止痛特性的活性成分的口服固体剂型，所述剂型的组成使得其通过液体提取其中包含的活性成分来防止所述剂型的滥用，其使用 常用的溶剂。 所述口服固体剂型含有至少一种至少一种止痛活性成分的盐，以及包含至少一种猝灭剂的抗滥用系统，所述猝灭剂适合于诱导所述止痛活性成分盐在所述止痛活性成分 在所述口服固体剂型的溶液中，盐不适当地提取，特别是药物滥用者。

    Oral medicinal product with modified release of at least one active principle in multimicrocapsular form
    7.
    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

    Applicant: Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

    Inventor： Catherine Castan ,  Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

    IPC: A61K9/16 ,  A61K9/22

    CPC classification number: A61K9/1635 ,  A61K9/1641 ,  A61K9/1658 ,  A61K9/2077 ,  A61K31/403

    Abstract: 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.

    Abstract translation: 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。

    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin
    8.
    发明授权
    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin 失效
    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

    Applicant: Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

    Inventor： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

    IPC: A61K9/14 ,  A61K9/16 ,  A61K9/40

    CPC classification number: A61K9/5015 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/43

    Abstract: 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.

    Abstract translation: 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

    Novel acetysalicylic acid formulations
    9.
    发明申请
    Novel acetysalicylic acid formulations 审中-公开
    新型乙酸水溶液配方

    公开(公告)号：US20100009005A1

    公开(公告)日：2010-01-14

    申请号：US11920749

    申请日：2006-05-24

    Applicant: Gérard Soula ,  Florence Guimberteau

    Inventor： Gérard Soula ,  Florence Guimberteau

    IPC: A61K9/50 ,  A61K31/60 ,  A61P29/00

    CPC classification number: A61K9/5084 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/60 ,  A61K45/06 ,  A61K2300/00

    Abstract: The invention relates to pharmaceutical compositions of acetylsalicylic acid-based microcapsules to selectively inhibit the COX in the portal vein and/or in the liver to reduce the production of thromboxane. Further, the pharmaceutical composition minimizes COX inhibition in the systemic circulation to optimize the inhibition of platelet aggregation. Certain embodiments also address methods of prevention and/or treatment of these diseases, using these oral compositions such as enhancing the safety of antithrombotic treatments. Other embodiments contemplate oral pharmaceutical compositions that combine acetylsalicylic acid with anti-platelet aggregation drugs, without inducing gastric side effects.

    Abstract translation: 本发明涉及基于乙酰水杨酸的微胶囊的药物组合物，以选择性地抑制门静脉和/或肝脏中的COX以减少血栓素的产生。 此外，药物组合物使全身循环中的COX抑制最小化，以优化血小板聚集的抑制。 某些实施方案还涉及使用这些口服组合物来预防和/或治疗这些疾病的方法，例如增强抗血栓治疗的安全性。 其它实施方案考虑了将乙酰水杨酸与抗血小板聚集药物组合的口服药物组合物，而不诱导胃副作用。

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