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1. 发明授权

US06866867B2 Process for preparing a directly compressible solid dosage form containing microcrystalline cellulose 失效
标题翻译：制备含有微晶纤维素的直接可压缩固体剂型的方法
公开(公告)号：US06866867B2
公开(公告)日：2005-03-15
申请号：US10015538
申请日：2001-12-13
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter , Clifford M. Davidson
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter , Clifford M. Davidson
IPC分类号： A61K9/20 , A61K9/22 , A61K9/14 , A61K9/28
CPC分类号： A61K9/2054 , Y10S977/906
摘要： The present invention provides an improved process for the preparation of a agglomerated solid dosage form, comprising: (1) preparing an aqueous slurry of (a) microcrystalline cellulose; (b) a microcrystalline cellulose compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; (ii) inhibits interactions between adjacent cellulose surfaces, for example, via the creation of a hydrophobic boundary at cellulose surfaces; or (iii) accomplishes both (i) and (ii) above; and (c) an active agent; (2) thereafter drying the resultant aqueous slurry in a manner which inhibits quasi-hornification, thereby obtaining an agglomerated material which is directly compressible into a solid dosage form.
摘要翻译：本发明提供了制备凝聚固体剂型的改进方法，其包括：（1）制备（a）微晶纤维素的含水浆液; （b）微晶纤维素可压缩性增强剂，其（i）物理地限制相邻纤维素表面之间的界面的接近度; （ii）抑制相邻纤维素表面之间的相互作用，例如通过在纤维素表面上产生疏水性边界; 或（iii）完成上述（i）和（ii）和（c）活性剂; （2）然后以抑制准角质化的方式干燥所得的含水浆料，从而获得可直接压缩成固体剂型的凝聚材料。

2. 发明授权

US06395303B1 Process for preparing a directly compressible solid dosage form containing microcrystalline cellulose 失效
标题翻译：制备含有微晶纤维素的直接可压缩固体剂型的方法
公开(公告)号：US06395303B1
公开(公告)日：2002-05-28
申请号：US08868745
申请日：1997-06-04
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter , Clifford M. Davidson
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter , Clifford M. Davidson
IPC分类号： A61K914
CPC分类号： A61K9/2054 , Y10S977/906
摘要： The present invention provides an improved process for the preparation of a agglomerated solid dosage form, comprising preparing an aqueous slurry of microcrystalline cellulose and a microcrystalline cellulose compressibility augmenting agent and an active agent. The augmenting agent is capable of physically restricting the proximity of the interface between adjacent cellulose surfaces and/or inhibiting interactions between adjacent cellulose surfaces, for example, via the creation of a hydrophobic boundary at cellulose surfaces. The resulting aqueous slurry is dried in a manner which inhibits quasi-hornification, thereby obtaining an agglomerated material which is directly compressible into a solid dosage form.
摘要翻译：本发明提供了制备凝聚固体剂型的改进方法，包括制备微晶纤维素的水性浆液和微晶纤维素可压缩性增强剂和活性剂。增强剂能够物理地限制相邻纤维素表面之间的界面的接近和/或抑制相邻纤维素表面之间的相互作用，例如通过在纤维素表面上产生疏水性边界。将所得到的含水浆料以抑制准角质化的方式干燥，从而获得可直接压缩成固体剂型的凝聚材料。

3. 发明授权

US6106865A Pharmaceutical excipient having improved compressibility 失效
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US6106865A
公开(公告)日：2000-08-22
申请号：US37841
申请日：1998-03-10
申请人： John N. Staniforth , Edward A. Hunter , Bob E. Sherwood
发明人： John N. Staniforth , Edward A. Hunter , Bob E. Sherwood
IPC分类号： A61K9/20 , A61K47/04 , A61K9/14
CPC分类号： A61K9/2036 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2095 , Y10S977/906 , Y10S977/915
摘要： A composition, comprising (a) microcrystalline cellulose; and (b) a compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; or (ii) inhibits interactions between adjacent cellulose surfaces; or (iii) accomplishes both (i) and (ii) above, is disclosed. The composition is in the form of agglomerated particles of microcrystalline cellulose and the compressibility augmenting agent in intimate association with each other.
摘要翻译：一种组合物，其包含（a）微晶纤维素; 和（b）压缩性增强剂，其（i）物理地限制相邻纤维素表面之间的界面的接近度; 或（ii）抑制相邻纤维素表面之间的相互作用; 或（iii）完成上述（i）和（ii）所述。该组合物是微晶纤维素的附聚颗粒的形式和彼此紧密结合的可压缩性增强剂。

4. 发明授权

US5858412A Sustained release formulations utilizing pharmaceutical excipient having improved compressibility with modified microcrystalline 失效
标题翻译：使用具有改进的微晶具有改进的压缩性的药用赋形剂的持续释放制剂
公开(公告)号：US5858412A
公开(公告)日：1999-01-12
申请号：US982224
申请日：1997-12-17
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K20060101 , A61K9/20 , A61K9/22 , A61K47/04 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/30 , A61K47/38 , A61K47/42 , A61K9/14
CPC分类号： A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , A61K9/2095 , Y10S977/904 , Y10S977/906 , Y10S977/915
摘要： Sustained release formulations include an augmented microcrystalline cellulose, an active agent, and a sustained release carrier and methods for making same are disclosed.
摘要翻译：持续释放制剂包括增强的微晶纤维素，活性剂和缓释载体及其制备方法。

5. 发明授权

US06471994B1 Pharmaceutical excipient having improved compressibility 失效
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US06471994B1
公开(公告)日：2002-10-29
申请号：US09384130
申请日：1999-08-27
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A16K914
CPC分类号： A61K9/2013 , A61K9/2009 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , Y10S977/906
摘要： A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide. An extra low moisture excipient is provided which exhibits improved compressibility as compared to conventional microcrystalline cellulose, while providing a moisture content of from about 0.5 to 2.5% LOD, preferably between about 0.5 and about 1.8%, more preferably between 0.8 and 1.5%, and most preferably between about 0.8 and about 1.2 %.
摘要翻译：公开了具有改进的压缩性的微晶纤维素基赋形剂，无论是用于直接压片，干法制粒还是湿法制粒。赋形剂是微晶纤维素颗粒的聚集物和约0.1％至约20％的微晶纤维素重量的二氧化硅颗粒，其中微晶纤维素和二氧化硅彼此紧密结合。新型赋形剂中使用的二氧化硅具有约1纳米至约100微米的粒度。最优选地，二氧化硅是胶体二氧化硅的等级。提供了与常规微晶纤维素相比显示出改进的可压缩性的超低水分赋形剂，同时提供约0.5至2.5％的LOD，优选约0.5至约1.8％，更优选0.8至1.5％的水分含量，以及最优选在约0.8至约1.2％之间。

6. 发明授权

US5948438A Pharmaceutical formulations having improved disintegration and/or absorptivity 失效
标题翻译：具有改善的崩解和/或吸收性的药物制剂
公开(公告)号：US5948438A
公开(公告)日：1999-09-07
申请号：US868744
申请日：1997-06-04
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K9/20 , A61K9/14
CPC分类号： A61K9/2013 , A61K9/2009 , A61K9/2018 , A61K9/2036 , A61K9/2054 , Y10S977/801 , Y10S977/906 , Y10S977/915
摘要： An oral solid dosage form, comprising a compressed tablet including an excipient comprising (a) microcrystalline cellulose; and (b) a compressibility augmenting agent which (I) physically restricts the proximity of the interface between adjacent cellulose surfaces (e.g., silicon dioxide); or (ii) inhibits interactions between adjacent cellulose surfaces (e.g., sodium lauryl sulfate); or (iii) accomplishes both (i) and (ii) above; together with an active agent, is disclosed which provides improved disintegration and/or absorptivity to the oral solid dosage form when orally administered to human patients. The excipient comprises agglomerated particles of said microcrystalline cellulose and said compressibility augmenting agent in intimate association with each other.
摘要翻译：一种口服固体剂型，其包含压片，其包含赋形剂，所述赋形剂包含（a）微晶纤维素; （b）压缩性增强剂，其（I）物理地限制相邻的纤维素表面（例如二氧化硅）之间的界面的接近度; 或（ii）抑制相邻纤维素表面（例如月桂基硫酸钠）之间的相互作用; 或（iii）完成上述（i）和（ii）与活性剂一起被公开，其当口服施用于人类患者时提供口服固体剂型的改善的崩解和/或吸收性。赋形剂包括所述微晶纤维素的凝聚颗粒和所述压缩性增强剂彼此紧密结合。

7. 发明授权

US5741524A Sustained-release formulations utilizing pharmaceutical excipient having improved compressibility 失效
标题翻译：使用具有改善的压缩性的药物赋形剂的持续释放制剂
公开(公告)号：US5741524A
公开(公告)日：1998-04-21
申请号：US676654
申请日：1996-07-08
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K20060101 , A61K9/20 , A61K9/22 , A61K47/04 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/30 , A61K47/38 , A61K47/42 , A61K9/14
CPC分类号： A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , A61K9/2095 , Y10S977/904 , Y10S977/906 , Y10S977/915
摘要： Sustained release formulations include an augmented microcrystalline cellulose, an active agent, and a sustained release carrier and methods for making same are disclosed.
摘要翻译：持续释放制剂包括增强的微晶纤维素，活性剂和缓释载体及其制备方法。

8. 发明授权

US5725883A Pharmaceutical excipient having improved compressibility 失效
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US5725883A
公开(公告)日：1998-03-10
申请号：US486183
申请日：1995-06-07
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K9/20 , A61K9/26 , A61K47/02 , A61K47/04 , A61K47/38 , A61K9/14
CPC分类号： A61K9/2054 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2036 , A61K9/205 , Y10S977/727 , Y10S977/773 , Y10S977/775 , Y10S977/801 , Y10S977/89 , Y10S977/896 , Y10S977/904 , Y10S977/906 , Y10S977/915 , Y10T428/2982
摘要： A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and an effective amount of a surfactant, which, in preferred embodiments is an anionic surfactant present in amounts ranging from about 0.1% to about 0.5%, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and surfactant are in intimate association with each other. One preferred anionic surfactant utilized in the novel excipient is sodium lauryl sulfate.
摘要翻译：公开了具有改进的压缩性的微晶纤维素基赋形剂，无论是用于直接压片，干法制粒还是湿法制粒。赋形剂是微晶纤维素颗粒和有效量的表面活性剂的附聚物，其在优选的实施方案中是以微晶纤维素重量计约0.1％至约0.5％的量存在的阴离子表面活性剂，其中微晶纤维素和表面活性剂彼此紧密结合。在新型赋形剂中使用的一种优选的阴离子表面活性剂是月桂基硫酸钠。

9. 发明授权

US06936277B2 Pharmaceutical excipient having improved compressibility 失效
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US06936277B2
公开(公告)日：2005-08-30
申请号：US10145563
申请日：2002-05-14
申请人： John N. Staniforth , Edward A. Hunter , Bob E. Sherwood
发明人： John N. Staniforth , Edward A. Hunter , Bob E. Sherwood
IPC分类号： A61K9/20 , A61K9/14 , A61K9/50
CPC分类号： A61K9/2031 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , A61K9/2095
摘要： A method of preparing an excipient composition includes forming an aqueous slurry containing a mixture of microcrystalline cellulose in the form of a wet cake and a surfactant, said surfactant being present in an amount from about 0.1% to about 0.5% by weight of the wet-cake microcrystalline cellulose; and drying said slurry to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said surfactant. The excipient may be mixed with a therapeutically active agent to form a dosage form. The surfactant provides a hydrophobic boundary at cellulose surfaces, and improves absorptivity of the therapeutically active agent.
摘要翻译：制备赋形剂组合物的方法包括形成含有湿滤饼形式的微晶纤维素和表面活性剂的混合物的水性浆料，所述表面活性剂的存在量为湿润片剂重量的约0.1％至约0.5％蛋糕微晶纤维素; 并干燥所述浆料以获得包含多个与所述表面活性剂紧密结合的微晶纤维素附聚颗粒的赋形剂。赋形剂可以与治疗活性剂混合以形成剂型。表面活性剂在纤维素表面提供疏水性边界，并提高治疗活性剂的吸收性。

10. 发明授权

US06746693B2 Pharmaceutical excipient having improved compressibility 有权
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US06746693B2
公开(公告)日：2004-06-08
申请号：US10266518
申请日：2002-10-08
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K914
CPC分类号： A61K9/2013 , A61K9/2009 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , Y10S977/906
摘要： A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide. An extra low moisture excipient is provided which exhibits improved compressibility as compared to conventional microcrystalline cellulose, while providing a moisture content of of from about 0.5 to 2.5% LOD, preferably between about 0.5 and about 1.8%, more preferably between 0.8 and 1.5%, and most preferably between about 0.8 and about 1.2%.
摘要翻译：公开了具有改进的压缩性的微晶纤维素基赋形剂，无论是用于直接压片，干法制粒还是湿法制粒。赋形剂是微晶纤维素颗粒的聚集物和约0.1％至约20％的微晶纤维素重量的二氧化硅颗粒，其中微晶纤维素和二氧化硅彼此紧密结合。在新型赋形剂中使用的二氧化硅具有1纳米至约100微米的粒度。最优选地，二氧化硅是胶体二氧化硅的等级。提供了与常规微晶纤维素相比显示出改善的可压缩性的特别低的水分赋形剂，同时提供约0.5至2.5％LOD，优选约0.5至约1.8％，更优选0.8至1.5％的水分含量，最优选在约0.8至约1.2％之间。

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