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1.发明申请公开(公告)号：US20110104288A1
公开(公告)日：2011-05-05
申请号：US12917904
申请日：2010-11-02
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K31/375
摘要： Coprocessed compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained by preparing aqueous slurries of microcrystalline cellulose and calcium phosphate and drying such slurries to produce particulate products. The coprocessed products exhibit improved compactibility, as compared to dry physical blends of the same components.
摘要翻译： 包含磷酸钙和微晶纤维素的共加工组合物可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 这样的组合物可以通过制备微晶纤维素和磷酸钙的水性浆料并干燥这样的浆料以产生颗粒产物来获得。 与相同组分的干物理混合物相比，共加工产品表现出改进的紧密性。
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2.发明授权公开(公告)号：US08329221B2
公开(公告)日：2012-12-11
申请号：US12917904
申请日：2010-11-02
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K31/375
摘要： Coprocessed compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained by preparing aqueous slurries of microcrystalline cellulose and calcium phosphate and drying such slurries to produce particulate products. The coprocessed products exhibit improved compactibility, as compared to dry physical blends of the same components.
摘要翻译： 包含磷酸钙和微晶纤维素的共加工组合物可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 这样的组合物可以通过制备微晶纤维素和磷酸钙的水性浆料并干燥这样的浆料以产生颗粒产物来获得。 与相同组分的干物理混合物相比，共加工产品表现出改进的紧密性。
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3.发明申请MICROCRYSTALLINE CELLULOSE AND CALCIUM CARBONATE COMPOSITIONS USEFUL AS RECOMPACTIBLE PHARMACEUTICAL EXCIPIENTS 有权微晶纤维素和碳酸钙组合物作为可回收的药物成分有用公开(公告)号：US20110151014A1
公开(公告)日：2011-06-23
申请号：US12962992
申请日：2010-12-08
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
IPC分类号： A61K9/14 , A61K47/38 , A61K31/341 , A61P43/00 , B02C17/00
CPC分类号： A61K31/341 , A61K9/2009 , A61K9/2054 , A61K9/2095
摘要： Coprocessed compositions containing microcrystalline cellulose and calcium carbonate, wherein the weight ratio of microcrystalline cellulose to calcium carbonate is relatively high, are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained, for example, by preparing aqueous slurries or wet masses of microcrystalline cellulose and calcium carbonate and drying such slurries or wet masses to produce particulate products. The coprocessed products exhibit improved recompactibility, as compared to coprocessed products having lower microcrystalline cellulose:calcium carbonate weight ratios or as compared to physical dry blends of the two excipients.
摘要翻译： 包含微晶纤维素和碳酸钙的共加工组合物，其中微晶纤维素与碳酸钙的重量比相对较高，可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 这样的组合物可以通过例如制备水性浆液或湿块微晶纤维素和碳酸钙并干燥这样的浆料或湿块以产生颗粒产物来获得。 与具有较低微晶纤维素的共加工产物：碳酸钙重量比或与两种赋形剂的物理干混合物相比，共加工产品显示出改善的再压缩性。
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4.发明授权公开(公告)号：US08632818B2
公开(公告)日：2014-01-21
申请号：US12917991
申请日：2010-11-02
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
CPC分类号： A61K31/375 , A61K9/2009 , A61K9/2054 , A61K47/02 , A61K47/38
摘要： Compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. The recompactibility performance of such compositions is improved through the use of calcium phosphate having a relatively small particle size, e.g., a median particle size of not more than about 20 microns or not more than about 10 microns.
摘要翻译： 含有磷酸钙和微晶纤维素的组合物可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 通过使用具有相对较小粒度的磷酸钙，例如不大于约20微米或不大于约10微米的中值粒度，可以改善这种组合物的可再现性能。
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5.发明授权Microcrystalline cellulose and calcium carbonate compositions useful as recompactible pharmaceutical excipients 有权可用作可再生药物赋形剂的微晶纤维素和碳酸钙组合物公开(公告)号：US08632819B2
公开(公告)日：2014-01-21
申请号：US12962992
申请日：2010-12-08
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
CPC分类号： A61K31/341 , A61K9/2009 , A61K9/2054 , A61K9/2095
摘要： Coprocessed compositions containing microcrystalline cellulose and calcium carbonate, wherein the weight ratio of microcrystalline cellulose to calcium carbonate is relatively high, are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained, for example, by preparing aqueous slurries or wet masses of microcrystalline cellulose and calcium carbonate and drying such slurries or wet masses to produce particulate products. The coprocessed products exhibit improved recompactibility, as compared to coprocessed products having lower microcrystalline cellulose:calcium carbonate weight ratios or as compared to physical dry blends of the two excipients.
摘要翻译： 包含微晶纤维素和碳酸钙的共加工组合物，其中微晶纤维素与碳酸钙的重量比相对较高，可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 这样的组合物可以通过例如制备水性浆液或湿块微晶纤维素和碳酸钙并干燥这样的浆料或湿块以产生颗粒产物来获得。 与具有较低微晶纤维素的共加工产物：碳酸钙重量比或与两种赋形剂的物理干混合物相比，共加工产品显示出改善的再压缩性。
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6.发明申请公开(公告)号：US20110104271A1
公开(公告)日：2011-05-05
申请号：US12917991
申请日：2010-11-02
申请人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
发明人： Gregory Thoorens , Bruno LeClercq , Thomas Ruszkay
IPC分类号： A61K9/00 , A61K31/375 , A61K9/20
CPC分类号： A61K31/375 , A61K9/2009 , A61K9/2054 , A61K47/02 , A61K47/38
摘要： Compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. The recompactibility performance of such compositions is improved through the use of calcium phosphate having a relatively small particle size, e.g., a median particle size of not more than about 20 microns or not more than about 10 microns.
摘要翻译： 含有磷酸钙和微晶纤维素的组合物可用作制备含有活性药物成分的固体剂型的赋形剂，特别是通过涉及多次压实步骤的方法制备的那些。 通过使用具有相对较小粒度的磷酸钙，例如不大于约20微米或不大于约10微米的中值粒度，可以改善这种组合物的可再现性能。
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公开(公告)号：US20110294904A1
公开(公告)日：2011-12-01
申请号：US13207022
申请日：2011-08-10
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K9/2018 , A61K9/2054
摘要： A method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting is disclosed. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate lubricated dry granulate and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa. A method for evaluating binders is also disclosed.
摘要翻译： 公开了通过压片后压片制备含微晶纤维素的片剂的方法。 通过压片将片剂制剂转化成干燥颗粒，干燥颗粒润滑干燥颗粒并压制成片剂。 片剂制剂包含至少一种活性物质，含微晶纤维素的物质和任选的其它药学上可接受的赋形剂。 含微晶纤维素的材料具有至少9MPa或至少9.5MPa的最大初级压实拉伸强度和至少5MPa，至少5.5MPa或至少6MPa的二次压实拉伸强度。 还公开了一种用于评估粘合剂的方法。
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公开(公告)号：US07998505B2
公开(公告)日：2011-08-16
申请号：US11925375
申请日：2007-10-26
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K9/2018 , A61K9/2054
摘要： A method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting is disclosed. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate is lubricated and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa. A method for evaluating binders is also disclosed.
摘要翻译： 公开了通过压片后压片制备含微晶纤维素的片剂的方法。 通过压片将片剂制剂转化成干燥颗粒，将干燥的颗粒润滑并压实成片剂。 片剂制剂包含至少一种活性物质，含微晶纤维素的物质和任选的其它药学上可接受的赋形剂。 含微晶纤维素的材料具有至少9MPa或至少9.5MPa的最大初级压实拉伸强度和至少5MPa，至少5.5MPa或至少6MPa的二次压实拉伸强度。 还公开了一种用于评估粘合剂的方法。
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公开(公告)号：US20080213360A1
公开(公告)日：2008-09-04
申请号：US11925375
申请日：2007-10-26
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K9/2018 , A61K9/2054
摘要： A method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting is disclosed. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate lubricated dry granulate and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa. A method for evaluating binders is also disclosed.
摘要翻译： 公开了通过压片后压片制备含微晶纤维素的片剂的方法。 通过压片将片剂制剂转化成干燥颗粒，干燥颗粒润滑干燥颗粒并压制成片剂。 片剂制剂包含至少一种活性物质，含微晶纤维素的物质和任选的其它药学上可接受的赋形剂。 含微晶纤维素的材料具有至少9MPa或至少9.5MPa的最大初级压实拉伸强度和至少5MPa，至少5.5MPa或至少6MPa的二次压实拉伸强度。 还公开了一种用于评估粘合剂的方法。
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