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    TRANSDERMAL DELIVERY OF SYSTEMICALLY ACTIVE CENTRAL NERVOUS SYSTEM DRUGS
    2.
    发明申请
    TRANSDERMAL DELIVERY OF SYSTEMICALLY ACTIVE CENTRAL NERVOUS SYSTEM DRUGS 审中-公开
    系统主动中枢神经系统药物的转运

    公开(公告)号：US20070225379A1

    公开(公告)日：2007-09-27

    申请号：US11755923

    申请日：2007-05-31

    申请人： Dario Norberto Carrara ,  Arnaud Grenier ,  Igno Alberti ,  Laetitia Henry ,  Celine Decaudin

    发明人： Dario Norberto Carrara ,  Arnaud Grenier ,  Igno Alberti ,  Laetitia Henry ,  Celine Decaudin

    IPC分类号： A61K47/00 ,  A61K31/025

    CPC分类号： A61K47/10 ,  A61K9/006 ,  A61K9/08 ,  A61K9/7015 ,  A61K31/025 ,  A61K31/135 ,  A61K31/27 ,  A61K31/404 ,  A61K31/427 ,  A61K31/428 ,  A61K31/439 ,  A61K31/4468 ,  A61K31/4745 ,  A61K47/08

    摘要： The invention relates to a transdermal or transmucosal non-occlusive, semi-solid pharmaceutical formulation that includes at least one systemically active agent that acts on the Central Nervous System (CNS) of a mammal; and a permeation enhancing solvent system present in an amount sufficient to solubilize the at least one active ingredient. The permeation enhancing solvent system includes a pharmaceutically acceptable monoalkyl ether of diethylene glycol; a pharmaceutically acceptable glycol; preferably also a fatty alcohol and or a fatty acid; and a mixture of a C2 to C4 alcohol and water so that the permeation enhancing solvent system (a) inhibits crystallization of the at least one active ingredient on a skin or mucosal surface of a mammal, (b) reduces or prevents transfer of the formulation to clothing or to another being, (c) modulates biodistribution of the at least one active agent within different layers of skin, (d) facilitates absorption of the at least one active agent by a skin or a mucosal surface of a mammal, or (e) provides a combination of one or more of (a) through (d).

    摘要翻译： 本发明涉及透皮或透粘膜非闭塞性半固体药物制剂，其包括作用于哺乳动物的中枢神经系统（CNS）的至少一种全身活性剂; 和渗透增强溶剂系统，其量足以溶解至少一种活性成分。 渗透增强溶剂系统包括药学上可接受的二甘醇单烷基醚; 药学上可接受的二醇; 优选还包括脂肪醇和/或脂肪酸; 和C 2〜C 4醇与水的混合物，使得渗透促进溶剂体系（a）抑制至少一种活性成分在皮肤上的结晶或 哺乳动物的粘膜表面，（b）减少或阻止制剂向衣服或另一种转移，（c）调节至少一种活性剂在不同皮肤层内的生物分布，（d）促进吸收至少 一种由哺乳动物的皮肤或粘膜表面活性剂，或（e）提供（a）至（d）中的一种或多种的组合。

    LOW-FRIABILITY, PATIENT-FRIENDLY ORALLY DISINTEGRATING FORMULATIONS
    3.
    发明申请
    LOW-FRIABILITY, PATIENT-FRIENDLY ORALLY DISINTEGRATING FORMULATIONS 审中-公开
    低适应性，患者友好的ORALLY DISINC制剂

    公开(公告)号：US20070196494A1

    公开(公告)日：2007-08-23

    申请号：US11670293

    申请日：2007-02-01

    申请人： Arnaud Grenier ,  Celine Decaudin ,  Dario Norberto Carrara ,  Ubaldo Conte ,  Lauretta Maggi

    发明人： Arnaud Grenier ,  Celine Decaudin ,  Dario Norberto Carrara ,  Ubaldo Conte ,  Lauretta Maggi

    IPC分类号： A61K31/78

    CPC分类号： A61K9/0056 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/78

    摘要： The present invention relates to a rapidly disintegrating orally administratable solid dosage formulation that includes at least one active ingredient, at least one first disintegration agent that is at least one type-C methacrylic acid copolymer according to the U.S. Pharmacopoeia National Formulary US/NF, a second disintegration agent of crospovidone or a cross-linked povidone polymer derivative thereof, and a non-cariogenic diluent that does not increase glucose blood levels. The at least one first disintegration agent does not function as an enteric coating, insulation coating intended to protect active ingredient(s), or coating intended to mask taste or smell. The solid dosage form has a mass of about 50 to about 1000 mg, and the at least one first disintegration agent is present in the dosage form in an amount not exceeding 15%, with respect to the total weight of the dosage form. The second disintegration agent is present in the dosage form in an amount not exceeding 15% with respect to the total weight of the dosage form. The first and the second disintegration agent are present in total amounts that provide a weight ratio of about 1:1 to about 1:3, wherein the dosage form provides at least one of the in vitro or in vivo disintegration time that is less than 30 seconds, and has a friability of 1% or less according to the U.S. Pharmacopoeia test.

    摘要翻译： 本发明涉及快速崩解的可口服给药的固体剂型制剂，其包含至少一种活性成分，至少一种第一崩解剂，其是根据US Pharmacopoeia National Formulary US / NF至少一种C型甲基丙烯酸共聚物， 交联聚维酮的第二崩解剂或其交联聚维酮聚合物衍生物和不增加葡萄糖血液水平的非致龋剂稀释剂。 至少一种第一崩解剂不用作肠溶衣，旨在保护活性成分的绝缘涂层或旨在掩蔽味道或气味的涂层。 相对于剂型的总重量，固体剂型具有约50至约1000mg的质量，并且至少一种第一崩解剂以不超过15％的量存在于剂型中。 相对于剂型的总重量，第二崩解剂以不超过15％的量存在于剂型中。 第一和第二崩解剂以提供重量比为约1:1至约1:3的总量存在，其中该剂型提供至少一种体外或体内崩解时间小于30 秒，根据美国药典测试，其脆度为1％以下。

    ORAL FORMULATION AND SUSPENSION OF AN ONCOLOGY DRUG
    4.
    发明申请
    ORAL FORMULATION AND SUSPENSION OF AN ONCOLOGY DRUG 有权
    口服药物的口服制剂和悬浮液

    公开(公告)号：US20160008369A1

    公开(公告)日：2016-01-14

    申请号：US14769110

    申请日：2014-02-21

    申请人： Celine DECAUDIN ,  Vincent ROGUE

    发明人： Celine Decaudin ,  Vincent Rogue

    IPC分类号： A61K31/5377 ,  A61K9/00 ,  A61K47/38 ,  B65D81/32 ,  A61K47/26 ,  A61K47/02 ,  A61K47/14 ,  A61K9/10 ,  A61K47/12

    CPC分类号： A61K31/5377 ,  A61K9/0095 ,  A61K9/10 ,  A61K47/02 ,  A61K47/12 ,  A61K47/14 ,  A61K47/26 ,  A61K47/38 ,  B65D81/32

    摘要： Dry powder formulations for inhalation and their use in the treatment diseases and conditions. The formulation contains a uniform blend of a first spray-dried powder and a second spray-dried powder. The first spray-dried powder contains spray-dried particles of a therapeutically active ingredient dispersed in a pharmaceutically acceptable hydrophobic excipient. The second spray-dried powder contains spray-dried particles formed from a pharmaceutically acceptable hydrophobic excipient but are substantially free of any therapeutically active ingredient. The active ingredient in the first spray-dried powder is loaded sufficiently high to compensate for the second spray-dried powder being substantially free of any active ingredient. A process for preparing such formulations is also described.

    摘要翻译： 用于吸入的干粉配方及其用于治疗疾病和病症。 该制剂含有第一喷雾干燥粉末和第二喷雾干燥粉末的均匀混合物。 第一喷雾干燥的粉末包含分散在药学上可接受的疏水性赋形剂中的治疗活性成分的喷雾干燥颗粒。 第二喷雾干燥粉末含有由药学上可接受的疏水性赋形剂形成的喷雾干燥颗粒，但基本上不含任何治疗活性成分。 第一喷雾干燥粉末中的活性成分被充分地加载以补偿基本上没有任何活性成分的第二喷雾干燥粉末。 还描述了制备这种制剂的方法。