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公开(公告)号：EP1003487B1
公开(公告)日：2005-11-30
申请号：EP98932706.9
申请日：1998-07-13
IPC分类号： A61K9/50 , A61K9/16 , A61K9/20 , A61K31/415 , A61K31/44 , A61K31/435
CPC分类号： A61K9/1652 , A61K9/2095 , A61K9/5073
摘要： There is disclosed a method for stabilizing active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, by means of anhydrous granulation of active substances and dried pharmaceutically acceptable auxiliary substances for the preparation of pellet cores or granules. All pharamceutically acceptable auxiliary substances employed are dried before use so that their weight loss at drying is less than 1.0 % of the total weight of the pharmaceutically acceptable auxiliary substance, preferably less than 0.5 % Organic solvents used in process of anhydrous granulation should contain less than 0.2 % of water. A novel pharmaceutical formulation with controlled release of active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, is disclosed as well.
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2.发明授权
公开(公告)号：EP0827397B1
公开(公告)日：2001-09-05
申请号：EP96915292.5
申请日：1996-05-17
IPC分类号： A61K9/22
CPC分类号： A61K9/2077 , A61K9/2846 , A61K9/2866 , A61K9/2886
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3.发明公开
公开(公告)号：EP1003487A1
公开(公告)日：2000-05-31
申请号：EP98932706.9
申请日：1998-07-13
IPC分类号： A61K9/50 , A61K9/16 , A61K9/20 , A61K31/415 , A61K31/44 , A61K31/435
CPC分类号： A61K9/1652 , A61K9/2095 , A61K9/5073
摘要： There is disclosed a method for stabilizing active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, by means of anhydrous granulation of active substances and dried pharmaceutically acceptable auxiliary substances for the preparation of pellet cores or granules. All pharamceutically acceptable auxiliary substances employed are dried before use so that their weight loss at drying is less than 1.0 % of the total weight of the pharmaceutically acceptable auxiliary substance, preferably less than 0.5 % Organic solvents used in process of anhydrous granulation should contain less than 0.2 % of water. A novel pharmaceutical formulation with controlled release of active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, is disclosed as well.
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4.发明公开
公开(公告)号：EP0827397A2
公开(公告)日：1998-03-11
申请号：EP96915292.0
申请日：1996-05-17
CPC分类号： A61K9/2077 , A61K9/2846 , A61K9/2866 , A61K9/2886
摘要： Described is a novel three-phase pharmaceutical form with constant and controlled release of an amorphous active ingredient stabilized with polymers for a single daily peroral application, which is especially suitable for active ingredients existing in amorphous form or in one or more polymorphous forms, which exhibit poor solubility in crystal form depending on the polymorphous form, particle size and the specific surface area of the active ingredient. The active ingredient can be used in its amorphous or any polymorphous form, which in the process of the preparation of the three-phase pharmaceutical form according to the invention is converted into the amorphous form. The three-phase pharmaceutical form with constant and controlled release of an amorphous active ingredient for a single daily peroral application contains a core consisting of a first and a second phase and a coating representing the third phase. In the first phase the three-phase pharmaceutical form contains an amorphous active ingredient, the water-soluble polymer polyvinylpyrrolidone and a cellulose ether as carriers of the amorphous active ingredient and simultaneously as inhibitors of its crystallization, a surfactant that improves the solubility of the active ingredient and promotes the absorption of the amorphous active ingredient from gastrointestinal tract, in the second phase it contains a cellulose ether and a mixture of mono-, di- and triglycerides as sustained release agents and the third phase is represented by a poorly soluble or gastro-resistant film coating, which in the first few hours after the application controls the release of the active ingredient and can consist of an ester of hydroxypropylmethylcellulose with phthalic anhydride or of a copolymerizate based on methacrylic acid and ethyl acrylate. Described is also a process for the preparation of this pharmaceutical form.
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