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1. 发明申请

WO2005020876A3 PHARMACEUTICAL COMPOSITION, METHOD OF MANUFACTURING AND THERAPEUTIC USE THEREOF 审中-公开
公开(公告)号：WO2005020876A3
公开(公告)日：2005-03-10
申请号：PCT/CZ2004/000053
申请日：2004-08-31
申请人： PLIVA-LACHEMA A.S. , ZALUDEK, Borek , BOLESLAV, Jan , KYSILKA, Vladimir , VERNER, Jiri , BRZOBOHATA, Hana , MATEJKOVA, Bozena , KAKRDA, Milan
发明人： ZALUDEK, Borek , BOLESLAV, Jan , KYSILKA, Vladimir , VERNER, Jiri , BRZOBOHATA, Hana , MATEJKOVA, Bozena , KAKRDA, Milan
IPC分类号： A61K9/19
摘要： The invention relates to a pharmaceutical composition prepared by freeze-drying in vacuo, containing oxaliplatin as the active component and a pharmaceutically acceptable carrier, wherein the carrier is at least one alcoholic sugar of non-animal origin, the weight ratio of oxaliplatin to the alcoholic sugar of non-animal origin or alcoholic sugars of non-animal origin being 1:3 to 1:7. The invention also relates to the method of manufacturing of said composition and to the use of this composition in the treatment of tumors sensitive to oxaliplatin.

2. 发明申请

WO2006034661A1 A METHOD FOR PRODUCING ORAL SOLID DOSAGE FORM AND ORAL SOLID DOSAGE FORM PREPARED THEREBY 审中-公开
标题翻译：一种制备口服固体剂型和口服固体剂型的方法
公开(公告)号：WO2006034661A1
公开(公告)日：2006-04-06
申请号：PCT/CZ2005/000073
申请日：2005-09-30
申请人： PLIVA-LACHEMA a.s. , FRANC, Ales , ZALUDEC, Borek , NOVOTNY, Zdenek , BRZOBOHATA, Hana , PETROVICOVA, Anna , STEJSKAL, Leos
发明人： FRANC, Ales , ZALUDEC, Borek , NOVOTNY, Zdenek , BRZOBOHATA, Hana , PETROVICOVA, Anna , STEJSKAL, Leos
IPC分类号： A61K9/20 , A61K31/138 , A61P5/32
CPC分类号： A61K31/138 , A61K9/2009 , A61K9/2054
摘要： The invention relates to a method for producing an oral solid dosage form capable of instantaneous release of the active substance which is a sparingly water-soluble antiestrogen, particularly tamoxifen citrate, characterized in that the antiestrogen is pre-mixed with a water-insoluble and/or alcohol-insoluble filler and optionally with at least one further pharmaceutically acceptable excipient, 80 % of particles of the filler or its mixture with at least one further pharmaceutically acceptable excipient being smaller than 355 micrometers and at most 10 % of these particles being smaller than 40 micrometers, whereupon the triturate obtained is mixed with a water-insoluble and/or alcohol-insoluble filler and with a water-soluble and/or alcohol-soluble binder and optionally with at least one further pharmaceutical excipient, 80 % of particles of the mixture of the filler and binder and optionally of at least one further pharmaceutically acceptable excipient being smaller than 355 micrometers and at most 10 % of these particles being smaller than 40 micrometers, and the mixture obtained is granulated in the presence of water and/or alcohol which are used in an amount smaller than or equal to 8 % by weight, based on the total weight of the wet granulated mixture, whereupon the granulate obtained is dried. The invention also relates to the thus-obtained oral solid dosage form.
摘要翻译：本发明涉及一种能够即时释放活性物质的口服固体剂型的方法，该活性物质是微水溶性抗雌激素，特别是柠檬酸他莫昔芬，其特征在于将抗雌激素预先与水不溶性和/ 或醇不溶性填料和任选与至少一种其它药学上可接受的赋形剂，80％的填料或其混合物与至少一种其它药学上可接受的赋形剂的颗粒小于355微米，并且至少10％的这些颗粒小于所得到的研磨剂与水不溶性和/或醇不溶性填料和水溶性和/或醇可溶性粘合剂和任选与至少一种其它药物赋形剂混合，80％填料和粘合剂的混合物和任选的至少一种另外的药学上可接受的赋形剂小于355微米这些颗粒中至少10％小于40微米，所得混合物在水和/或醇的存在下造粒，其用量小于或等于8重量％，基于总和湿颗粒状混合物的重量，然后将获得的颗粒干燥。本发明还涉及由此获得的口服固体剂型。

3. 发明申请

WO2005020876A2 PHARMACEUTICAL COMPOSITION, METHOD OF MANUFACTURING AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：药物组合物，制造方法及其治疗方法
公开(公告)号：WO2005020876A2
公开(公告)日：2005-03-10
申请号：PCT/CZ2004000053
申请日：2004-08-31
申请人： PLIVA LACHEMA AS , ZALUDEK BOREK , BOLESLAV JAN , KYSILKA VLADIMIR , VERNER JIRI , BRZOBOHATA HANA , MATEJKOVA BOZENA , KAKRDA MILAN
发明人： ZALUDEK BOREK , BOLESLAV JAN , KYSILKA VLADIMIR , VERNER JIRI , BRZOBOHATA HANA , MATEJKOVA BOZENA , KAKRDA MILAN
IPC分类号： A61K9/00 , A61K9/19 , A61K31/555 , A61K33/24 , A61K47/00 , A61K47/26 , A61K
CPC分类号： A61K9/0019 , A61K9/19 , A61K31/555 , A61K47/26
摘要： The invention relates to a pharmaceutical composition prepared by freeze-drying in vacuo, containing oxaliplatin as the active component and a pharmaceutically acceptable carrier, wherein the carrier is at least one alcoholic sugar of non-animal origin, the weight ratio of oxaliplatin to the alcoholic sugar of non-animal origin or alcoholic sugars of non-animal origin being 1:3 to 1:7. The invention also relates to the method of manufacturing of said composition and to the use of this composition in the treatment of tumors sensitive to oxaliplatin.
摘要翻译：本发明涉及通过真空冷冻干燥制备的含奥沙利铂作为活性组分的药物组合物和药学上可接受的载体，其中载体是至少一种非动物来源的酒精糖，奥沙利铂与酒精的重量比非动物来源的糖或非动物来源的酒精为1：3至1：7。本发明还涉及所述组合物的制备方法以及该组合物在治疗对奥沙利铂敏感的肿瘤中的用途。

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