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    • 21. 发明公开
    • Sustained release formulation for Venlafaxine hydrochloride
    • 文拉法辛盐酸氟沙星
    • EP1502587A1
    • 2005-02-02
    • EP03386019.8
    • 2003-07-30
    • Pharmathen S.A.
    • Karavas, EvangelosLioumis, KonstantinosPolitis, Stavros
    • A61K9/48A61K31/137
    • A61K9/4808A61K31/137
    • The invention provides a sustained release composition that;

      1. Is free of initially increased drug delivery that occurs in sustained release systems containing the water soluble drug venlafaxine HCl, known as burst phenomenon, by using a functional core partially or totally coated by a functional coating layer or film.
      2. Delivers the drug substance within 24 hours and is therefore suitable for once daily administration of the said drug substance.
      3. Exhibits linearity between the strength of the drug formulation and the total mass of the formulation, by proportional increase of the amounts of the drug substance and the excipients in the formulation.
      4. Is possible to be divided in smaller doses, without affecting the release of the drug substance.

      The invention provides a sustained release capsule formulation containing an appropriate number of functional complex mini tablets comprising of:

      1. A functional core comprising the active ingredient, especially the water-soluble drug Venlafaxine HCl and appropriate excipients.
      2. A functional coating layer or film that reduces the initial surface of the core that is available for the release of the water-soluble drug Venlafaxine HCl, reducing the burst phenomenon.
    • 本发明提供一种缓释组合物, 1.通过使用部分或完全被功能性涂层或膜涂覆的功能性核心,在含有水溶性药物文拉法辛HCl的持续释放系统中发生最初增加的药物递送(称为爆发现象)。 2.在24小时内提供药物,因此适用于每日一次给药所述药物。 3.通过药物物质和制剂中赋形剂的量的比例增加,显示药物制剂的强度与制剂的总质量之间的线性关系。 4.可能以较小剂量分割,而不影响药物释放。 本发明提供了含有适量数量的功能性复合微型片剂的缓释胶囊制剂,其包含:1.功能性核心,其包含活性成分,特别是水溶性药物文拉法辛HCl和适当的赋形剂。 2.一种功能性涂层或薄膜,可减少核心的初始表面,可用于释放水溶性药物文拉法辛HCl,减少爆发现象。