公开(公告)号：US20030138847A1

公开(公告)日：2003-07-24

申请号：US10245839

申请日：2002-09-16

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

IPC: G01N033/53 ,  C08G063/91 ,  G01N033/543 ,  C08G063/48

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

Abstract: 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.

Abstract translation: 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基团预处理后被压缩成片剂，在用非质子有机溶剂预处理后被压缩成片剂。

公开(公告)号：US20030138376A1

公开(公告)日：2003-07-24

申请号：US10245836

申请日：2002-09-16

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

IPC: A61K049/00 ,  G01N033/543

CPC classification number: C07K1/023 ,  B01J4/02 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  C07K1/04 ,  C07K1/1077 ,  C40B60/14

Abstract: A dosing form for at least one solid reagent for use in conventional organic and inorganic synthesis, in parallel synthesis, and in split and mix synthesis in combinatorial chemistry is provided as compressed tablets each containing the same predetermined amount of said at least one reagent embedded in a polymer matrix comprising beads of a polymer insoluble in the solvents for the intended synthesis, which tablets are capable of disintegrating in said solvent for release of the at least one reagent and disperse the matrix as polymer beads into the solvent. The polymer beads forming the matrix and the reagents of the dosing form can easily be removed by filtration in order to separate these from a formed soluble product. In a method for producing the dosing form, beads of one or more polymers are mixed with the reagents and compressed into tablets after pre-treatment with an aprotic organic solvent.

Abstract translation: 提供用于常规有机和无机合成，并行合成和组合化学中的分离和混合合成中的至少一种固体试剂的给药形式，其为包含相同预定量的所述至少一种试剂 聚合物基质，其包含不溶于用于预期合成的溶剂中的聚合物的珠粒，该片剂能够在所述溶剂中分解以释放至少一种试剂并将基质作为聚合物珠分散到溶剂中。 形成基质的聚合物珠粒和剂型的试剂可以通过过滤容易地除去，以将它们与形成的可溶性产物分离。 在制备给药形式的方法中，将一种或多种聚合物的珠粒与试剂混合，并用非质子有机溶剂预处理后压制成片剂。

公开(公告)号：US20040058989A1

公开(公告)日：2004-03-25

申请号：US10619743

申请日：2003-07-01

Applicant: H. Lundbeck A/S

Inventor： Ken Liljegren ,  Per Holm

IPC: A61K031/343

CPC classification number: C07D307/87 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/1688 ,  A61K9/2054 ,  A61K31/343

Abstract: A solid unit dosage form comprising citalopram which is prepared by a process comprising a step wherein citalopram base or a pharmaceutically acceptable salt thereof and optionally pharmaceutically acceptable excipients is roller compacted.

Abstract translation: 包含西酞普兰的固体单位剂型，其通过包括以下步骤的方法制备，其中将西酞普兰碱或其药学上可接受的盐和任选的药学上可接受的赋形剂压实。

公开(公告)号：US20030232881A1

公开(公告)日：2003-12-18

申请号：US10310621

申请日：2002-12-05

Applicant: H. LUNDBECK A/S

Inventor： Ken Liljegren ,  Per Holm ,  Ole Nielsen ,  Sven Wagner

IPC: C07D307/87 ,  A61K031/343

CPC classification number: A61K9/2054 ,  A61K9/4866 ,  A61K31/343 ,  C07D307/87

Abstract: The invention is directed to methods of crystallizing pharmaceutically acceptable salts of citalopram, the resulting crystals, and pharmaceutical compositions comprising the crystals.

Abstract translation: 本发明涉及结晶西酞普兰的药学上可接受的盐，所得结晶和包含晶体的药物组合物的方法。

公开(公告)号：US20020160050A1

公开(公告)日：2002-10-31

申请号：US10106805

申请日：2002-03-25

Applicant: H. Lundbeck A/S

Inventor： Michiel Onne Elema ,  Per Holm

IPC: A61K009/16 ,  A61K009/50

CPC classification number: A61K9/1694

Abstract: 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.

Abstract translation: 由熔融粒状组合物制备的固体改性剂型，包含（A）一种或多种亲水性纤维素醚聚合物，（B）亲水性熔融粘合剂和（C）治疗活性成分。

公开(公告)号：US20030078442A1

公开(公告)日：2003-04-24

申请号：US10245824

申请日：2002-09-12

Applicant: H. Lundbeck A/S

Inventor： Hans Petersen ,  Klaus Peter Bogeso ,  Per Holm

IPC: C07D307/87

CPC classification number: C07D307/87

Abstract: The present invention relates to the crystalline base of the well known antidepressant drug citalopram,1-null3-(dimethylamino)propylnull-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.

Abstract translation: 本发明涉及众所周知的抗抑郁药物西酞普兰，1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，所述碱的制剂， 制备西酞普兰纯化盐的方法，例如使用碱的氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。