公开(公告)号：WO2011087629A2

公开(公告)日：2011-07-21

申请号：PCT/US2010/059403

申请日：2010-12-08

Applicant: FMC CORPORATION ,  THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

Inventor： THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

CPC classification number: A61K31/341 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2095

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2011056785A2

公开(公告)日：2011-05-12

申请号：PCT/US2010/055102

申请日：2010-11-02

Applicant: FMC CORPORATION ,  THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

Inventor： THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

IPC: A61K47/04 ,  A61K47/02 ,  A61K47/38 ,  A61K47/30 ,  A61K9/20 ,  A61K9/16

CPC classification number: A61K31/375 ,  A61K9/2009 ,  A61K9/2054 ,  A61K47/02 ,  A61K47/38

Abstract: 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.

Abstract translation: 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，例如中值粒度不超过约20微米或不超过约10微米，改善了这种组合物的重新赋型性能。

公开(公告)号：WO2013169977A3

公开(公告)日：2014-01-09

申请号：PCT/US2013040263

申请日：2013-05-09

Applicant: FMC CORP ,  SEWALL CHRISTOPHER J ,  BLAKEMORE WILLIAM R ,  LECLERCQ BRUNO

Inventor： SEWALL CHRISTOPHER J ,  BLAKEMORE WILLIAM R ,  LECLERCQ BRUNO

IPC: A61K36/02 ,  A61K9/20 ,  A61K9/22 ,  A61K31/731

CPC classification number: A61K9/205

Abstract: The present invention is directed to a controlled release solid dosage form comprising a controlled release modifier and an active ingredient comprising at least one of a pharmaceutical, veterinary, or nutraceutical active ingredient, wherein the controlled release modifier comprises lambda carrageenan from the taxonomic order Halymeniales. The present invention is also directed to ethanol resistant controlled release solid dosage forms and methods for reducing the ethanol sensitivity of an active ingredient in a controlled release solid dose form.

Abstract translation: 本发明涉及包含控制释放调节剂和包含药物，兽医或营养活性成分中的至少一种的活性成分的控释固体剂型，其中控制释放调节剂包含分子分类Halymeniales的λ角叉菜胶。 本发明还涉及乙酸耐量控释固体剂型以及用于以控制释放固体剂量形式降低活性成分的乙醇敏感性的方法。

公开(公告)号：WO2013169977A2

公开(公告)日：2013-11-14

申请号：PCT/US2013/040263

申请日：2013-05-09

Applicant: FMC CORPORATION ,  SEWALL, Christopher, J. ,  BLAKEMORE, William, R. ,  LECLERCQ, Bruno

Inventor： SEWALL, Christopher, J. ,  BLAKEMORE, William, R. ,  LECLERCQ, Bruno

CPC classification number: A61K9/205

Abstract: The present invention is directed to a controlled release solid dosage form comprising a controlled release modifier and an active ingredient comprising at least one of a pharmaceutical, veterinary, or nutraceutical active ingredient, wherein the controlled release modifier comprises lambda carrageenan from the taxonomic order Halymeniales. The present invention is also directed to ethanol resistant controlled release solid dosage forms and methods for reducing the ethanol sensitivity of an active ingredient in a controlled release solid dose form.

Abstract translation: 本发明涉及包含控制释放调节剂和包含药物，兽医或营养活性成分中的至少一种的活性成分的控释固体剂型，其中控制释放调节剂包含分子分类Halymeniales的λ角叉菜胶。 本发明还涉及乙酸耐量控释固体剂型以及用于以控制释放固体剂量形式降低活性成分的乙醇敏感性的方法。

公开(公告)号：WO2011056785A3

公开(公告)日：2011-09-29

申请号：PCT/US2010055102

申请日：2010-11-02

Applicant: FMC CORP ,  THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

Inventor： THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

IPC: A61K47/04 ,  A61K9/16 ,  A61K9/20 ,  A61K47/02 ,  A61K47/30 ,  A61K47/38

CPC classification number: A61K31/375 ,  A61K9/2009 ,  A61K9/2054 ,  A61K47/02 ,  A61K47/38

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2008057266A3

公开(公告)日：2008-11-13

申请号：PCT/US2007022684

申请日：2007-10-26

Applicant: FMC CORP ,  THOORENS GREGORY ,  LECLERCQ BRUNO ,  CARLIN BRIAN ,  RILEY PETER J ,  GARCIA MIGUEL ANGEL

Inventor： THOORENS GREGORY ,  LECLERCQ BRUNO ,  CARLIN BRIAN ,  RILEY PETER J ,  GARCIA MIGUEL ANGEL

IPC: A61K9/16

CPC classification number: A61K9/1623 ,  A61K9/1652 ,  A61K9/1682 ,  A61K9/2018 ,  A61K9/2054

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2008057266A2

公开(公告)日：2008-05-15

申请号：PCT/US2007/022684

申请日：2007-10-26

Applicant: FMC CORPORATION ,  THOORENS, Gregory ,  LECLERCQ, Bruno ,  CARLIN, Brian ,  RILEY, Peter, J. ,  GARCIA, Miguel, Angel

Inventor： THOORENS, Gregory ,  LECLERCQ, Bruno ,  CARLIN, Brian ,  RILEY, Peter, J. ,  GARCIA, Miguel, Angel

IPC: A61K9/16

CPC classification number: A61K9/1623 ,  A61K9/1652 ,  A61K9/1682 ,  A61K9/2018 ,  A61K9/2054

Abstract: 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.

Abstract translation: 公开了一种通过碾压和压片制备含微晶纤维素片剂的方法。 通过碾压将片剂制剂转化为干燥的颗粒，干燥的颗粒润滑干燥的颗粒并压制成片剂。 该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。 含微晶纤维素材料具有至少9MPa或至少9.5MPa的最大一次压缩抗拉强度和至少5MPa，至少5.5MPa或至少6MPa的二次压缩抗拉强度。

公开(公告)号：WO2011087629A3

公开(公告)日：2011-11-17

申请号：PCT/US2010059403

申请日：2010-12-08

Applicant: FMC CORP ,  THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

Inventor： THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

IPC: A61K47/38 ,  A61K9/14 ,  A61K9/16 ,  A61K9/20 ,  A61K47/06 ,  A61K47/30

CPC classification number: A61K31/341 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2095

Abstract: 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.

Abstract translation: 包含微晶纤维素和碳酸钙的共处理组合物（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含水浆料或湿微团纤维素和碳酸钙并干燥这些浆料或湿料以产生微粒产品而获得。 与具有较低微晶纤维素：碳酸钙重量比或与两种赋形剂的物理干共混物相比的共处理产品相比，共处理产品表现出改进的重新赋型性。

公开(公告)号：WO2011056775A3

公开(公告)日：2011-11-03

申请号：PCT/US2010055068

申请日：2010-11-02

Applicant: FMC CORP ,  THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

Inventor： THOORENS GREGORY ,  LECLERCQ BRUNO ,  RUSZKAY THOMAS

IPC: A61K47/04 ,  A61K9/16 ,  A61K9/20 ,  A61K47/02 ,  A61K47/30 ,  A61K47/38

CPC classification number: A61K9/2009 ,  A61K9/1611 ,  A61K9/1652 ,  A61K9/2054 ,  A61K31/375

Abstract: 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.

Abstract translation: 含有磷酸钙和微晶纤维素的共加工组合物可用作制备含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含水浆液并干燥这些浆液以产生颗粒状产品而获得。 与相同组分的干物理共混物相比，共处理产品表现出改进的成型性。

公开(公告)号：WO2011056775A2

公开(公告)日：2011-05-12

申请号：PCT/US2010/055068

申请日：2010-11-02

Applicant: FMC CORPORATION ,  THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

Inventor： THOORENS, Gregory ,  LECLERCQ, Bruno ,  RUSZKAY, Thomas

IPC: A61K47/04 ,  A61K47/02 ,  A61K47/38 ,  A61K47/30 ,  A61K9/20 ,  A61K9/16

CPC classification number: A61K9/2009 ,  A61K9/1611 ,  A61K9/1652 ,  A61K9/2054 ,  A61K31/375

Abstract: 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.

Abstract translation: 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。