发明申请
US20100305087A1 ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY
审中-公开
活性药物成分在固体支持,无定形和改善溶解度
- 专利标题: ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY
- 专利标题(中): 活性药物成分在固体支持,无定形和改善溶解度
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申请号: US12809576申请日: 2008-12-18
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公开(公告)号: US20100305087A1公开(公告)日: 2010-12-02
- 发明人: Rok Grahek , Aleksander Resman , Andrej Bastarda , Martin Crnugelj
- 申请人: Rok Grahek , Aleksander Resman , Andrej Bastarda , Martin Crnugelj
- 申请人地址: SI Ljubljana
- 专利权人: Lek Pharmaceuticals d.d.
- 当前专利权人: Lek Pharmaceuticals d.d.
- 当前专利权人地址: SI Ljubljana
- 优先权: EP07150359.3 20071221
- 国际申请: PCT/EP2008/067875 WO 20081218
- 主分类号: A61K31/397
- IPC分类号: A61K31/397 ; A61K31/122
摘要:
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 is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed.
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