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SOLID ORALLY ADMINISTERABLE PHARMACEUTICAL DOSAGE FORMS WITH RAPID ACTIVE PRINCIPLE RELEASE
专利权人:
发明人:
벤케, 클라우스
申请号:
KR1020087010702
公开号:
KR1014453980000B1
申请日:
2006.09.21
申请国别(地区):
KR
年份:
2014
代理人:
摘要:
Solid, orally administrable pharmaceutical drug delivery system (A) comprises 5-chloro-N ({(5S)- 2-oxo-3-[4-(3-oxo-4-morpholinyl)- phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide (I) with a fast release of the active substance, where the active substance (I) is in amorphous form and 80% of the active substance (I) is released within less than 2 hours, according to United State Pharmacopeial drug release procedure with apparatus 2 (Paddle). Independent claims are included for: (1) a method for the preparation of (A) comprising preparing the active substance (I) containing a mixture by a melt process, mixing the obtained mixture in powder form with further auxiliary materials and subsequently filling the mixture as sachet or capsules, or after mixing with tableting additives, preferably by direct tableting and press-molding to tablets, which is subsequently polished; (2) a mutli-particulate pharmaceutical drug delivery system; (3) a pharmaceutical drug delivery system comprising the multi-particulate pharmaceutical drug delivery system; (4) a method for the preparation of multi-particulate pharmaceutical drug delivery system comprising preparing active substance (I) with an extrudate by melt extrusion process and cutting the obtained mixture; and (5) a method for prophylaxis, secondary prophylaxis and/or treatment of thromboembolic diseases comprising administering (A). ACTIVITY : Thrombolytic; Cardiant; Antianginal; Vasotropic; Cerebroprotective; Anticoagulant. MECHANISM OF ACTION : Factor Xa inhibitor.본 발명은, 무정형 및/또는 열역학상 준안정성 결정 변형의 5-클로로-N-({(5S)-2-옥소-3-[4-(3-옥소-4-모르폴리닐)페닐]-1,3-옥사졸리딘-5-일}메틸)-2-티오펜카르복스아미드를 포함하고 활성 성분을 신속 방출하는 고형 경구 투여용 제약 투여 형태, 및 이의 제조 방법, 및 의약으로서의 이의 용도, 장애의 예방, 2차 예방 및/또는 치료에 있어서의 이의 용도, 및 장애의 예방, 2차 예방 및/또는 치료를 위한 의약 제조에 있어서의 이의 용도에 관한 것이다.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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