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    • 1. 发明申请
    • LOW-FRIABILITY, PATIENT-FRIENDLY ORALLY DISINTEGRATING FORMULATIONS
    • 低适应性,患者友好的ORALLY DISINC制剂
    • WO2007093305A2
    • 2007-08-23
    • PCT/EP2007/001011
    • 2007-02-06
    • ANTARES PHARMA IPL AGGRENIER, ArnaudDECAUDIN, CelineCARRARA, Dario, NorbertoCONTE, UbaldoMAGGI, Lauretta
    • GRENIER, ArnaudDECAUDIN, CelineCARRARA, Dario, NorbertoCONTE, UbaldoMAGGI, Lauretta
    • A61K9/0056A61K9/2018A61K9/2027A61K9/2095A61K31/78
    • 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.
    • 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盖味道或气味的涂层。 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。
    • 2. 发明申请
    • THERAPEUTIC SYSTEM FOR THE CONTROLLED RELEASE OF ACTIVE INGREDIENTS
    • 用于控制释放活性成分的治疗系统
    • WO2003075897A1
    • 2003-09-18
    • PCT/EP2003/002536
    • 2003-03-12
    • JAGOTEC AGMAGGI, LaurettaCONTE, Ubaldo
    • MAGGI, LaurettaCONTE, Ubaldo
    • A61K9/28
    • A61K9/209A61K9/2072A61K9/2886
    • A system designed to release one or more active substances in different, previously programmable modes, is described. The system is constituted by a tablet in three layers, two of which (the outer layers) vehicularise the active ingredient(s), whilst the third (the central layer) is constituted of a polymeric barrier which does not contain active substance and has the appropriate characteristics of erodibility or gelation. The tablet is completely coated with a film of polymeric material insoluble in water and/or in aqueous fluids, on which one or more incisions delimiting an area of exactly calculated geometric shape and size, have been made through the use of a laser beam of appropriate power and intensity. The removal of the film inside the incision(s) allows the release of the active ingredient(s) into aqueous fluid in predetermined amounts and times. The procedure for the production of the aforementioned pharmaceutical form is also described.
    • 描述了设计用于释放不同的先前可编程模式中的一种或多种活性物质的系统。 该系统由三层的片剂构成,其中两层(外层)是活性成分,而第三层(中心层)由不含活性物质的聚合物屏障构成,并具有 适当的可蚀性或凝胶化特性。 片剂完全涂覆有不溶于水和/或水性流体的聚合物材料薄膜,其中通过使用适当的激光束制成限定精确计算的几何形状和尺寸的区域的一个或多个切口 功率和强度。 在切口内去除膜允许以预定量和次数将活性成分释放到水性流体中。 还描述了用于生产上述药物形式的方法。