COMPOSITIONS OF LOPINAVIR
    4.
    发明公开
    COMPOSITIONS OF LOPINAVIR 审中-公开
    洛匹那韦,ZUSAMMENSETZUNGEN

    公开(公告)号:EP2753307A1

    公开(公告)日:2014-07-16

    申请号:EP12758882.0

    申请日:2012-09-07

    IPC分类号: A61K9/19 A61K9/51 A61K31/536

    摘要: The present invention relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug lopinavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof. The present invention also relates to processes for preparing both the solid composition and the aqueous dispersion, as well as to their use in therapy for the treatment and/or prevention of retroviral infections such as human immunodeficiency virus (HIV).

    摘要翻译: 本发明涉及包含抗逆转录病毒药物洛匹那韦的纳米颗粒的固体组合物和水分散体。 固体组合物和水分散体另外包含亲水性聚合物和表面活性剂的混合物。 表面活性剂选自维生素E-聚乙二醇 - 琥珀酸酯(Vit-E-PEG-琥珀酸酯),聚氧乙烯脱水山梨醇脂肪酸酯,N-烷基二甲基苄基氯化铵,脱氧胆酸钠,二辛基磺基琥珀酸钠,聚乙二醇12-羟基硬脂酸酯,聚乙烯醇 (PVA)和聚氧乙烯和聚氧丙烯的嵌段共聚物,或其组合。 亲水性聚合物适当地选自聚乙烯醇(PVA),聚乙烯醇 - 聚乙二醇接枝共聚物,聚氧乙烯和聚氧丙烯的嵌段共聚物,聚乙二醇,羟丙基甲基纤维素(HPMC)和聚乙烯吡咯烷酮或其组合。 本发明还涉及制备固体组合物和水性分散体的方法,以及它们在治疗和/或预防逆转录病毒感染如人类免疫缺陷病毒(HIV)中的用途。

    IMPROVEMENTS RELATING TO PHARMACEUTICAL COMPOSITIONS
    6.
    发明授权
    IMPROVEMENTS RELATING TO PHARMACEUTICAL COMPOSITIONS 有权
    与药物组合物有关的改进

    公开(公告)号:EP2040681B1

    公开(公告)日:2017-08-09

    申请号:EP07786933.7

    申请日:2007-06-29

    IPC分类号: A61K9/16 A61K31/496

    摘要: The invention provides a solvent-free biocidal composition of improved efficacy comprising at least one water insoluble biocide (preferably a herbicide) and a water-soluble carrier material, wherein the water-insoluble biocide is dispersed through the carrier material in nano-disperse form having a peak diameter of the nano-disperse form below 1000nm. The invention also provides a process which comprises spray drying a solution of the biocide and a solution of a water-soluble carrier to obtain a solvent free dispersion of the biocide in the carrier, which, when dissolved in water, produces a nano-disperse biocide. The invention also provides an aqueous dispersion of a water insoluble biocide and a water-soluble carrier obtained by the dispersion of the composition of the solvent free composition in water.

    摘要翻译: 本发明提供具有改进功效的无溶剂杀生物组合物,其包含至少一种水不溶性杀生物剂(优选除草剂)和水溶性载体材料,其中水不溶性杀生物剂以纳米分散体形式分散通过载体材料, 在1000nm以下的纳米分散体的峰值直径。 本发明还提供了一种方法,该方法包括喷雾干燥杀生物剂溶液和水溶性载体溶液以获得杀生物剂在载体中的无溶剂分散体,其在溶于水时产生纳米分散杀生物剂 。 本发明还提供了通过将无溶剂组合物的组合物分散在水中获得的水不溶性杀生物剂和水溶性载体的水分散体。