公开(公告)号：EP2072042A1

公开(公告)日：2009-06-24

申请号：EP07150359.3

申请日：2007-12-21

申请人： Lek Pharmaceuticals D.D.

发明人： Grahek, Rok ,  Resman, Aleksander ,  Batarda, Andrej ,  Crnugelj, Martin

IPC分类号： A61K9/18 ,  A61K31/122 ,  A61K31/397

CPC分类号： A61K31/122 ,  A61K9/143 ,  A61K31/397

摘要： The present invention discloses a combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support,
wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide, wherein said API is a compound having both, at least one hydrophobic structural moiety causing the API to have low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to said solid support involving polar or ionic or hydrogen bonding, wherein the hydrophilic groups of the API are independently equal or different and comprise at least one of the group consisting of OH- and halogen-groups;
wherein said API is bound to said solid support by adsorption, and wherein a major proportion of said API is in the amorphous state.
The present invention also discloses a pharmaceutical preparation comprising such a combination preparation as well as a method for producing such a combination preparation.

摘要翻译： 本发明光盘松散的组合制剂，其包含活性药物成分（API）和药学可接受的固体载体的，worin所述固体支持物是在水不溶性颗粒形式，并且包括选自硅酸，氢氧化铝和氢氧化钛，worin中选择的材料 所述API是具有两者的化合物，至少一个疏水结构部分使API在水中具有或在wässrige溶液的溶解度低，并且布置以形成多个分子间相互作用于所述固体支持涉及极性或离子键或氢键的多个亲水性基团 ，worin API的亲水基团是unabhängig相等或不同的，包括选自由OH-和卤素 - 基团中的至少一者; worin所述API通过吸附作用结合于所述固体载体，以及worin说API的主要部分处于非晶状态。 因此，本发明盘松动的药物制剂，其包含寻求的组合制剂以及用于制造寻求组合制剂的方法。