首页> 外国专利> PHARMACEUTICAL FORMULATION FOR SUBLINGUAL OR BUCCAL DELIVERY OF EPINEPHRINE OR A PRO-DRUG THEREOF

PHARMACEUTICAL FORMULATION FOR SUBLINGUAL OR BUCCAL DELIVERY OF EPINEPHRINE OR A PRO-DRUG THEREOF

机译:依非那明的舌下或口腔药物制剂或其前药

摘要

The present invention relates to a pharmaceutical composition for the treatment of anaphylaxis formulated for rapid delivery, in one embodiment, the delivery vehicle is a rapidly dissolving film. The films contain an epinephrine or a novel epinephrine pro-drag for fee rapid treatment of anaphylaxis in a patient. This invention relates to pharmaceutical compositions made by modifying the physicochemical properties of epinephrine in order to enhance its permeability through biological membranes (sublingual and buccal membranes). Several prodrugs of epinephrine are shown by modifying the two hydroxyl (phenolic) groups in positions 3 and 4 on the benzene ring, by chemically reacting the two groups with several acid moieties to form an ester bond with different alkyl chains. The addition of an alkyl group will enhance the lipophilicity of epinephrine (increase log P) and will consequently increase its permeability through the biological membranes (sublingual and buccal tissues in the oral cavity).
机译:本发明涉及配制用于快速递送的用于治疗过敏反应的药物组合物,在一个实施方案中,递送载体是快速溶解膜。所述膜包含肾上腺素或新型肾上腺素前药,用于快速治疗患者的过敏反应。本发明涉及通过改变肾上腺素的理化特性以增强其通过生物膜(舌下和颊膜)的渗透性而制备的药物组合物。通过修饰苯环上3和4位的两个羟基(酚基),使两个基团与几个酸部分化学反应形成具有不同烷基链的酯键,可以显示出几种肾上腺素的前药。烷基的添加将增强肾上腺素的亲脂性(增加log P),并因此增加其通过生物膜(口腔中舌下和颊组织)的渗透性。

著录项

  • 公开/公告号US2019337886A1

    专利类型

  • 公开/公告日2019-11-07

    原文格式PDF

  • 申请/专利权人 LONO PHARMA LLC;

    申请/专利号US201716347625

  • 发明设计人 HASSAN ALMOAZEN;

    申请日2017-11-09

  • 分类号C07C219/30;A61K9;A61K47/02;A61K47/10;A61K47/26;A61K47/12;A61K47/46;

  • 国家 US

  • 入库时间 2022-08-21 12:08:26

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