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1. 发明申请

US20080118552A1 Finely Divided Composition Containing Poorly Water Soluble Substance 有权
标题翻译：含水不良物质的细分组合物
公开(公告)号：US20080118552A1
公开(公告)日：2008-05-22
申请号：US11795734
申请日：2006-01-27
申请人： Hiroshi Suzuki , Tomohiro Yoshinari , Naomi Nagaoka
发明人： Hiroshi Suzuki , Tomohiro Yoshinari , Naomi Nagaoka
IPC分类号： A61K9/48 , A61K9/20 , A61K47/30 , A61K9/28 , A61K9/14
CPC分类号： A61K9/146 , A23L33/10 , A61K9/145 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/405 , A61K31/422 , A61K31/4422 , A61K31/64
摘要： A composition containing a poorly water soluble substance of the present invention is a composition having a median diameter of not more than 1 μm, comprising (i) a poorly water soluble substance and (ii) polyvinylpyrrolidone or a vinylpyrrolidone-vinyl acetate copolymer, and preferably, a composition having a median diameter of not more than 1 μm, comprising (i) a poorly water soluble substance, (ii) polyvinylpyrrolidone or a vinylpyrrolidone-vinyl acetate copolymer and (iii) an auxiliary dispersion stabilizer. By employing such constitution, a poorly water soluble substance is sufficiently micronized and a composition containing a poorly water soluble substance showing good absorbability of the poorly water soluble substance can be provided.A composition containing a poorly water soluble substance of the present invention can be prepared into a solid dosage form for oral administration in various forms such as tablet, powder, granule, capsule and the like. Therefore, using a composition containing a poorly water soluble substance of the present invention, for example, pharmaceutical preparations in various dosage forms showing good absorbability of a drug, which is a poorly water soluble substance, can be realized.
摘要翻译：含有本发明的水溶性差的物质的组合物是中值粒径不大于1μm的组合物，其包含（i）水难溶性物质和（ii）聚乙烯吡咯烷酮或乙烯基吡咯烷酮 - 乙酸乙烯酯共聚物，优选（i）水难溶性物质，（ii）聚乙烯吡咯烷酮或乙烯基吡咯烷酮 - 乙酸乙烯酯共聚物的组合物，和（iii）辅助分散稳定剂。通过采用这种结构，水溶性差的物质被充分微粉化，并且可以提供含有水难溶性物质显示良好吸收性的难溶于水的物质的组合物。含有本发明的水溶性差的物质的组合物可以制成固体剂型，用于各种形式的口服给药，例如片剂，粉剂，颗粒剂，胶囊剂等。因此，使用含有本发明的水溶性差的物质的组合物，例如可以实现作为水难溶性物质的药物的吸收性良好的各种剂型的药物制剂。

2. 发明授权

US08623405B2 Finely divided composition containing poorly water soluble substance 有权
标题翻译：精细分散的组合物含有水溶性差的物质
公开(公告)号：US08623405B2
公开(公告)日：2014-01-07
申请号：US11795734
申请日：2006-01-27
申请人： Hiroshi Suzuki , Tomohiro Yoshinari , Naomi Nagaoka
发明人： Hiroshi Suzuki , Tomohiro Yoshinari , Naomi Nagaoka
IPC分类号： A61K9/48 , A61K9/20 , A61K47/30 , A61K9/28 , A61K9/14
CPC分类号： A61K9/146 , A23L33/10 , A61K9/145 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/405 , A61K31/422 , A61K31/4422 , A61K31/64
摘要： The disclosed method involves preparation of a composition containing a poorly water soluble substance. The composition has a median diameter of not more than 1 μm, and includes (i) a poorly water soluble substance, (ii) polyvinylpyrrolidone or a vinylpyrrolidone-vinyl acetate copolymer, and (iii) an auxiliary dispersion stabilizer. By employing such constitution, a poorly water soluble substance is sufficiently micronized and a composition containing a poorly water soluble substance showing good absorbability of the poorly water soluble substance can be provided.
摘要翻译：所公开的方法涉及制备含有水难溶性物质的组合物。该组合物的中值粒径不大于1um，并且包括（i）水难溶性物质，（ii）聚乙烯吡咯烷酮或乙烯基吡咯烷酮 - 乙酸乙烯酯共聚物，和（iii）辅助分散稳定剂。通过采用这种结构，水溶性差的物质被充分微粉化，并且可以提供含有水难溶性物质显示良好吸收性的难溶于水的物质的组合物。

3. 发明申请

US20090208584A1 Solid preparation 审中-公开
标题翻译：固体制剂
公开(公告)号：US20090208584A1
公开(公告)日：2009-08-20
申请号：US11921664
申请日：2006-06-09
申请人： Tomohiro Yoshinari , Yutaka Ebisawa , Hiroshi Suzuki
发明人： Tomohiro Yoshinari , Yutaka Ebisawa , Hiroshi Suzuki
IPC分类号： A61K9/14 , A61K47/38 , A61K31/538
CPC分类号： A61K9/2095 , A61K9/1623 , A61K9/1652 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K9/2866 , A61K31/536
摘要： The solid preparation of the present invention aims at providing a solid preparation superior in the stability during production and preservation even when a poorly water-soluble substance having a low melting point is contained in a large amount, and also superior in the disintegration property and release property of a poorly water-soluble substance having a low melting point, after oral administration, and is characterized by the following 1) to 3): 1) containing a poorly water-soluble substance having a low melting point, a saccharide, and a cellulose selected from a crystalline cellulose and a low-substituted hydroxypropylcellulose, 2) a saccharide/cellulose weight ratio exceeding 2, and 3) a cellulose content of not less than 5 wt %.
摘要翻译：本发明的固体制剂的目的在于提供即使在大量含有低熔点的难溶性水溶性物质的情况下，在制造和保存中的稳定性方面也优异的固体制剂，并且还具有优异的崩解性和脱模性口服后具有低熔点的水溶性差的物质的性质，其特征在于以下1）〜3）：1）含有低熔点的水难溶性物质，糖类和选自结晶纤维素和低取代羟丙基纤维素的纤维素，2）糖/纤维素重量比超过2，和3）纤维素含量不小于5重量％。

4. 发明授权

US08927011B2 Method for producing pharmaceutical tablet 有权
标题翻译：生产药片的方法
公开(公告)号：US08927011B2
公开(公告)日：2015-01-06
申请号：US12601158
申请日：2008-05-20
申请人： Hiroshi Suzuki , Tomohiro Yoshinari
发明人： Hiroshi Suzuki , Tomohiro Yoshinari
IPC分类号： A61K9/20 , A61K31/44 , A61K31/485 , A61K47/12
CPC分类号： A61K9/2013 , A61K9/2077 , A61K31/485 , A61K47/12
摘要： A process for advantageously producing tablets having an improved release property and an excellent stability to change with time is provided. The process is for producing tablets containing a morphinan compound represented by the Formula (I) below or pharmaceutically acceptable acid addition salt thereof and an acidic substance such as fumaric acid, maleic acid or adipic acid, and characterized in that the morphinan compound or a pharmaceutically acceptable acid addition salt thereof is granulated by wet granulation together with (an) excipient(s) prior to adding the acidic substance thereto.
摘要翻译：提供了一种有利地制备具有改善的释放性能和优异的随时间变化的稳定性的片剂的方法。该方法用于制备含有由下式（I）表示的吗啡喃化合物或其药学上可接受的酸加成盐和酸性物质如富马酸，马来酸或己二酸的片剂，其特征在于吗啡喃化合物或药学上可接受的盐在将酸性物质加入其中之前，其可接受的酸加成盐与（a）赋形剂一起通过湿法制粒造粒。

5. 发明申请

US20110045028A1 SUSTAINED RELEASE PREPARATION 审中-公开
标题翻译：持续发布准备
公开(公告)号：US20110045028A1
公开(公告)日：2011-02-24
申请号：US12516536
申请日：2007-11-29
申请人： Satoshi Iinuma , Yoshie Iinuma , Tomohiro Yoshinari , Tsuneaki Tottori
发明人： Satoshi Iinuma , Yoshie Iinuma , Tomohiro Yoshinari , Tsuneaki Tottori
IPC分类号： A61K31/513 , A61K9/00 , A61P7/02 , A61P9/10
CPC分类号： A61K31/506 , A61K9/2018 , A61K9/2054
摘要： Disclosed is a sustained-release preparation which is prepared by shaping a granule comprising a blood coagulation factor Xa inhibitor and a mixture of at least two hydrophilic polymers. Also disclosed is a pharmaceutical composition comprising a combination of the sustained-release preparation and an immediate release preparation comprising a blood coagulation factor Xa inhibitor. It becomes possible to provide a controlled release preparation comprising a blood coagulation factor Xa inhibitor for the prevention or treatment of thrombosis, which can control the activity of blood coagulation factor Xa for a long term and is excellent in convenience and compliance. It is also becomes possible to provide a method for producing the controlled release preparation.
摘要翻译：公开了一种缓释制剂，其通过使包含凝血因子Xa抑制剂和至少两种亲水性聚合物的混合物的颗粒成形而制备。还公开了包含缓释制剂和包含凝血因子Xa抑制剂的速释制剂的组合的药物组合物。可以提供一种控制释放制剂，其包含凝血因子Xa抑制剂，用于预防或治疗血栓形成，其可以长期控制凝血因子Xa的活性，并且方便性和顺应性优异。也可以提供一种制备控释制剂的方法。

6. 发明授权

US06235947B1 D-mannitol and its preparation 有权
标题翻译： D-甘露醇及其制备方法
公开(公告)号：US06235947B1
公开(公告)日：2001-05-22
申请号：US09155978
申请日：1998-10-23
申请人： Tomohiro Yoshinari , Fritz Schueckler , Norbert Poellinger , Shinji Maegata
发明人： Tomohiro Yoshinari , Fritz Schueckler , Norbert Poellinger , Shinji Maegata
IPC分类号： C07C3118
CPC分类号： C07C31/26 , C07C29/78
摘要： D-mannitol having a specific surface area of not less than about 1 m2/g is disclosed. The D-mannitol shows improved compressibility and is useful as an excipient.
摘要翻译：公开了比表面积不小于约1m 2 / g的D-甘露糖醇。 D-甘露醇显示出改进的可压缩性并且可用作赋形剂。

7. 发明申请

US20080031942A1 Solid Preparation 审中-公开
标题翻译：固体制剂
公开(公告)号：US20080031942A1
公开(公告)日：2008-02-07
申请号：US11667517
申请日：2005-12-02
申请人： Yoshihiro Uchiyama , Tomohiro Yoshinari , Makoto Fukuta
发明人： Yoshihiro Uchiyama , Tomohiro Yoshinari , Makoto Fukuta
IPC分类号： A61K9/20 , A61K31/21 , A61K33/04 , A61K33/20 , A61P43/00 , A61K33/42 , A61K9/00 , A61K9/14
CPC分类号： A61K9/2013 , A61K31/4178
摘要： A medical drug, in particular, solid preparations containing a medicinal ingredient with high tendency toward gelation, characterized by simultaneously containing a surface modifier and an acid or base. This characteristic realizes improvement to the disintegration easiness, production efficiency and stability of the solid preparations containing the above medicinal ingredient.
摘要翻译：医药，特别是包含具有高凝胶化倾向的药用成分的固体制剂，其特征在于同时含有表面改性剂和酸或碱。该特征实现了包含上述药物成分的固体制剂的崩解容易度，生产效率和稳定性的改善。

8. 发明授权

US5187133A Catalyst composition for hydrotreating of hydrocarbons and hydrotreating process using the same 失效
标题翻译：用于氢化烃的催化剂组合物及其加氢方法
公开(公告)号：US5187133A
公开(公告)日：1993-02-16
申请号：US670719
申请日：1991-03-18
申请人： Tomohiro Yoshinari , Kazushi Usui , Yasuo Yamamoto , Mitsuru Ohi
发明人： Tomohiro Yoshinari , Kazushi Usui , Yasuo Yamamoto , Mitsuru Ohi
IPC分类号： B01J23/88 , B01J29/076 , B01J29/16 , B01J29/26 , B01J29/48 , B01J29/58 , B01J29/64 , B01J29/69 , B01J35/10 , C10G45/08 , C10G45/12
CPC分类号： C10G45/12
摘要： A catalyst composition for the hydrotreatment of hydrocarbon oils is disclosed. The composition comprises at least one metal compound having hydrogenating activity belonging to a Group VIB or Group VIII carried on a carrier comprising 2-35% by weight of zeolite and 98-65% by weight of alumina or an alumina-containing substance, wherein, (A) said alumina or alumina-containing substance (1) has a mean pore diameter of 60-125 angstrom and (2) contains the pore volume of which the diameter falls within .+-.10 angstrom of the mean pore diameter of 70-98% of the total pore volume, (B) said zeolite (3) has a mean particle size of 6 .mu.m or smaller and (4) contains particles of which the diameter is 6 .mu.m or smaller of 70-98% of all zeolite particles. It has both high hydrodesulfurization and high cracking capabilities at the same time, and can selectively crack the heavy fractions which have once been hydrotreated, yielding lighter fractions.

9. 发明授权

US4981832A Catalyst composition for hydrogenation of heavy hydrocarbon oil and process for producing the catalyst 失效
标题翻译：用于重质烃油氢化的催化剂组合物和用于生产催化剂的方法
公开(公告)号：US4981832A
公开(公告)日：1991-01-01
申请号：US374805
申请日：1989-07-03
申请人： Kinya Tawara , Kazuyoshi Kudoh , Kazushi Usui , Tomohiro Yoshinari , Shigenori Nakashizu
发明人： Kinya Tawara , Kazuyoshi Kudoh , Kazushi Usui , Tomohiro Yoshinari , Shigenori Nakashizu
IPC分类号： B01J23/88 , B01J23/883 , B01J35/02 , B01J35/10 , C10G45/04 , C10G45/06 , C10G45/08
CPC分类号： B01J35/10 , B01J23/883 , C10G45/04 , B01J35/1042 , B01J35/1061 , B01J35/108
摘要： A catalyst composition for the hydrogenation of heavy hydrocarbon oil, where the catalyst composition comprises at least one active ingredient for hydrogenation supported on a porous alumina carrier and has the following characteristics: (1) the total volume of the pores therein is from 0.4 to 1.0 ml/g; (2) the mean pore diameter of pores having a pore diameter of from 5 to 400 .ANG. is from 60 to 140 .ANG.; (3) the volume of pores having a pore size within .+-.25% of the mean pore diameter of pores having a pore diameter of from 5 to 400 .ANG. is from 60 to 98% of the volume of pores having a pore diameter of from 5 to 400 .ANG.; (4) the volume of pores having a pore diameter of from 400 to 5000 .ANG. is from 2 to 9% of the total volume of the entire pores; (5) the ratio (mm.sup.2 /mm.sup.3) of the outer surface area of a molded catalyst powder to the volume thereof is from 4 to 8; and (6) all points in the interior of the molded catalyst particle are positioned within 0.05 to 0.6 mm from the outer surface thereof. A process for producing the catalyst composition is also disclosed. Further, a process for hydrogenating heavy hydrocarbon oil, which comprises contacting the heavy hydrocarbon oil with the catalyst composition in the presence of hydrogen is disclosed.
摘要翻译：一种用于重质烃油氢化的催化剂组合物，其中催化剂组合物包含至少一种负载在多孔氧化铝载体上的用于氢化的活性成分，并具有以下特征：（1）其中的孔的总体积为0.4-1.0 ml / g; （2）孔径为5至400埃的孔的平均孔径为60至140纳米; （3）孔径为孔径为5〜400的孔的平均孔径的+/- 25％以内的孔的体积为孔径为孔的体积的60〜98％从5到400 ANGSTROM; （4）孔径为400〜5000的孔的体积为整个孔的总体积的2〜9％（5）成型催化剂粉末的外表面积与其体积的比（mm2 / mm3）为4〜8; 和（6）模塑催化剂颗粒内部的所有点位于距其外表面0.05至0.6mm的范围内。还公开了一种制备催化剂组合物的方法。此外，公开了一种用于氢化重质烃油的方法，其包括在氢气存在下使重质烃油与催化剂组合物接触。

10. 发明申请

US20080234343A1 Preparation with Elevated Content 审中-公开
标题翻译：高含量制备
公开(公告)号：US20080234343A1
公开(公告)日：2008-09-25
申请号：US10592829
申请日：2005-03-23
申请人： Tomohiro Yoshinari
发明人： Tomohiro Yoshinari
IPC分类号： A61K31/4178
CPC分类号： A61K47/14 , A61K9/1075 , A61K9/4858 , A61K47/44 , C07D403/12
摘要： A composition for oral use, which contains a drug compound (in particular, a hardly water soluble or water-insoluble drug compound) in an elevated amount and is excellent in the absorbability of the drug compound via the digestive tract, is produced by dispersing the drug compound in an oily base and a surfactant in an amount exceeding the solubility thereof in the mixture of the oily base with the surfactant under heating, adding a polar solvent which serves as a poor solvent for the drug compound to the thus obtained dispersion, and heating the mixture to give a transparent liquid composition. Further, the obtained composition is encapsulated to give a capsule preparation.
摘要翻译：含有药物化合物（特别是难溶于水或不溶于水的药物化合物）的口服用组合物通过将消化道吸收药物的吸收性优异的方法分散，在油性基质中的药物化合物和表面活性剂的量超过其在油基与表面活性剂的混合物中的溶解度，加入作为药物化合物的不良溶剂的极性溶剂加入到如此得到的分散体中，以及加热混合物得到透明的液体组合物。此外，将所得组合物包封以得到胶囊制剂。

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