公开(公告)号：US20070275074A1

公开(公告)日：2007-11-29

申请号：US11711965

申请日：2007-02-27

申请人： Per Holm ,  Anders Burr ,  Michiel Elema ,  Birgitte Mollgaard ,  Jannie Holm ,  Kirsten Schultz

发明人： Per Holm ,  Anders Burr ,  Michiel Elema ,  Birgitte Mollgaard ,  Jannie Holm ,  Kirsten Schultz

IPC分类号： A61K9/14 ,  A61K47/06 ,  A61K47/26 ,  A61K47/46

CPC分类号： A61K9/1682 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2031 ,  B01J2/006 ,  B01J2/02 ,  Y10T428/24868 ,  Y10T428/24901 ,  Y10T428/29 ,  Y10T428/2982 ,  Y10T428/2991 ,  Y10T428/2998

摘要： A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

摘要翻译： 通过受控的团聚法制备颗粒材料的方法，即能够控制粒度增长的方法。 该方法特别适用于制备含有水溶性相对较低和/或经受化学分解的治疗和/或预防活性物质的药物组合物。 该方法包括：将包含载体的第一组合物喷雾在第二组合物上，第二组合物的熔点为约5℃或更高，其存在于液体形式的第一组合物中，第二组合物包含固体形式的材料，第二组合物 组合物具有最高温度对应于载体和/或载体组合物的熔点的温度，以及ii）混合或其它手段对其上喷涂第一组合物的第二组合物进行机械加工以获得颗粒材料。

公开(公告)号：US20050008706A1

公开(公告)日：2005-01-13

申请号：US10482558

申请日：2002-07-05

申请人： Per Holm ,  Anders Buur ,  Michiel Elema ,  Birgitte Mollgaard ,  Jannie Holm ,  Kirsten Schultz

发明人： Per Holm ,  Anders Buur ,  Michiel Elema ,  Birgitte Mollgaard ,  Jannie Holm ,  Kirsten Schultz

IPC分类号： A61K9/14 ,  A61K9/10 ,  A61K9/16 ,  A61K9/20 ,  A61K9/48 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61K47/44 ,  B01J2/00 ,  B01J2/02 ,  B29B9/00

CPC分类号： A61K9/1682 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2031 ,  B01J2/006 ,  B01J2/02 ,  Y10T428/24868 ,  Y10T428/24901 ,  Y10T428/29 ,  Y10T428/2982 ,  Y10T428/2991 ,  Y10T428/2998

摘要： A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

摘要翻译： 通过受控的团聚法制备颗粒材料的方法，即能够控制粒度增长的方法。 该方法特别适用于制备含有水溶性相对较低和/或经受化学分解的治疗和/或预防活性物质的药物组合物。 该方法包括：将包含载体的第一组合物喷雾在第二组合物上，第二组合物的熔点为约5℃或更高，其存在于液体形式的第一组合物中，第二组合物包含固体形式的材料，第二组合物 组合物具有最高温度对应于载体和/或载体组合物的熔点的温度，以及ii）混合或其它手段对其上喷涂第一组合物的第二组合物进行机械加工以获得颗粒材料。

公开(公告)号：US20050130228A1

公开(公告)日：2005-06-16

申请号：US10965662

申请日：2004-10-14

申请人： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Holm ,  Kim Andersen

发明人： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Holm ,  Kim Andersen

IPC分类号： C07B61/00 ,  B01J19/00 ,  C07B63/00 ,  C07C211/27 ,  C07C211/35 ,  C07C217/60 ,  C07K1/04 ,  C08L101/00 ,  C40B60/14 ,  G01N33/53 ,  G01N33/543

CPC分类号： C07K1/042 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  B01J2219/0072 ,  C07B2200/11 ,  C40B60/14

摘要： A dosing form for a polymer support for organic chemical synthesis in a solvent medium comprising a fixed weight amount of beads of a polymer containing functional groups, which polymer is insoluble in the solvent for the intended synthesis, is provided as compressed tablets of essentially equal weight and composition wherein the polymer beads are essentially intact and are released as such when the tablets are disintegrated in said solvent. Use of the dosing form is made in conventional synthesis, in parallel synthesis, in split and mix synthesis and/or combinatorial chemistry. In a method for producing the dosing form, beads of a polymer having functional gropusgroups is compressed into tablets after pre-treatment with an aprotic organic solvent. groups are compressed into tablets after pre-treatment with an aprotic organic solvent.

摘要翻译： 提供用于溶剂介质中有机化学合成的聚合物载体的剂型，其包含固定重量的含有官能团的聚合物珠，该聚合物不溶于用于预期合成的溶剂中，作为基本相等重量的压片 和组合物，其中当片剂在所述溶剂中崩解时，聚合物珠基本上是完整的并且如此释放。 在分批和混合合成和/或组合化学中，在常规合成，并行合成中使用配料形式。 在制备给药形式的方法中，具有功能性组蛋白的聚合物的珠粒在用非质子有机溶剂预处理后被压缩成片剂。 在用非质子有机溶剂预处理后，将组压缩成片剂。

公开(公告)号：US08535799B2

公开(公告)日：2013-09-17

申请号：US11711965

申请日：2007-02-27

申请人： Anders Burr ,  Michiel Ringkjøbing-Elema ,  Jannie Egeskov Holm ,  Per Holm ,  Birgitte Møllgaard ,  Kirsten Schultz

发明人： Anders Burr ,  Michiel Ringkjøbing-Elema ,  Jannie Egeskov Holm ,  Per Holm ,  Birgitte Møllgaard ,  Kirsten Schultz

IPC分类号： A61K47/02 ,  A61K9/10 ,  B01J2/00

CPC分类号： A61K9/1682 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2031 ,  B01J2/006 ,  B01J2/02 ,  Y10T428/24868 ,  Y10T428/24901 ,  Y10T428/29 ,  Y10T428/2982 ,  Y10T428/2991 ,  Y10T428/2998

摘要： A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

摘要翻译： 通过受控的团聚法制备颗粒材料的方法，即能够控制粒度增长的方法。 该方法特别适用于制备含有水溶性相对较低和/或经受化学分解的治疗和/或预防活性物质的药物组合物。 该方法包括：将包含载体的第一组合物喷雾在第二组合物上，第二组合物的熔点为约5℃或更高，其存在于液体形式的第一组合物中，第二组合物包含固体形式的材料，第二组合物 组合物具有最高温度对应于载体和/或载体组合物的熔点的温度，以及ii）混合或其它手段对其上喷涂第一组合物的第二组合物进行机械加工以获得颗粒材料。

公开(公告)号：US20060093668A1

公开(公告)日：2006-05-04

申请号：US11305682

申请日：2005-12-16

申请人： Michiel Elema ,  Per Holm

发明人： Michiel Elema ,  Per Holm

IPC分类号： A61K9/20

CPC分类号： A61K9/1694

摘要： Solid modified release dosage forms, prepared from melt granulated compositions comprising (A) one or more hydrophilic cellulose ether polymers, (B) a hydrophilic melt binder, and (C) a therapeutically active ingredient.

公开(公告)号：US07217431B2

公开(公告)日：2007-05-15

申请号：US10482558

申请日：2002-07-05

申请人： Per Holm ,  Anders Buur ,  Michiel Onne Elema ,  Birgitte Møllgaard ,  Jannie Egeskov Holm ,  Kirsten Schultz

发明人： Per Holm ,  Anders Buur ,  Michiel Onne Elema ,  Birgitte Møllgaard ,  Jannie Egeskov Holm ,  Kirsten Schultz

IPC分类号： A61K9/19 ,  A61K9/20

CPC分类号： A61K9/1682 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2031 ,  B01J2/006 ,  B01J2/02 ,  Y10T428/24868 ,  Y10T428/24901 ,  Y10T428/29 ,  Y10T428/2982 ,  Y10T428/2991 ,  Y10T428/2998

摘要： A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

公开(公告)号：US08664239B2

公开(公告)日：2014-03-04

申请号：US13167420

申请日：2011-06-23

申请人： Robert D. Gordon ,  Per Holm ,  Anne-Marie Lademann ,  Tomas Norling

发明人： Robert D. Gordon ,  Per Holm ,  Anne-Marie Lademann ,  Tomas Norling

IPC分类号： A61K31/44 ,  A61K31/436

CPC分类号： A61K31/436 ,  A61K9/0053 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/284 ,  A61K9/2846 ,  A61K9/4891 ,  A61K47/10 ,  Y10S514/885

摘要： An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.

公开(公告)号：US08591946B2

公开(公告)日：2013-11-26

申请号：US10569862

申请日：2004-08-30

申请人： Per Holm

发明人： Per Holm

IPC分类号： A61K9/14

CPC分类号： A61K9/0053 ,  A61K9/10 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2095 ,  A61K9/2846 ,  A61K9/2893 ,  A61K31/00 ,  A61K31/436 ,  A61K31/439 ,  A61K31/4745 ,  Y10S514/885

摘要： A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

公开(公告)号：US20100323008A1

公开(公告)日：2010-12-23

申请号：US12642563

申请日：2009-12-18

申请人： Per Holm ,  Tomas Norling

发明人： Per Holm ,  Tomas Norling

IPC分类号： A61K9/32 ,  A61K31/216 ,  A61P3/00

CPC分类号： A61K9/20 ,  A61K9/2013 ,  A61K9/2018 ,  A61K31/192 ,  A61K31/195 ,  A61K31/216 ,  A61K31/22 ,  A61K31/40 ,  A61K45/06 ,  A61K2300/00

摘要： The invention provides stable, solid dosage forms and pharmaceutical compositions in particulate form comprising a fibrate, for example fenofibrate, dissolved in an non-aqueous vehicle in order to ensure improved bioavailability of the active ingredient upon oral administration relative to known fibrate formulations.

摘要翻译： 本发明提供稳定的固体剂型和药物组合物，其包含溶解在非水载体中的贝特类，例如非诺贝特，以确保相对于已知的贝特类制剂口服给药时活性成分的生物利用度得到改善。

公开(公告)号：US07772273B2

公开(公告)日：2010-08-10

申请号：US11673270

申请日：2007-02-09

申请人： Per Holm

发明人： Per Holm

IPC分类号： A01N43/36

CPC分类号： A61K9/209 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2846 ,  A61K9/2866 ,  A61K31/138 ,  A61K31/40 ,  A61K31/401 ,  A61K2300/00

摘要： A stable pharmaceutical composition for oral administration comprising atorvastatin and an amount of a pharmaceutically acceptable organic alkalizing compound capable of establishing a microenvironment for atorvastatin having a pH of at least about 5, for example 2-amino-2-(hydroxymethyl)-1,3-propanediol (trometamol).

摘要翻译： 一种用于口服给药的稳定药物组合物，其包含阿托伐他汀和一定量的药学上可接受的有机碱化化合物，其能够建立pH至少约为5的阿托伐他汀的微环境，例如2-氨基-2-（羟甲基） - 丙二醇（氨丁三醇）。