公开(公告)号：US5955104A

公开(公告)日：1999-09-21

申请号：US896629

申请日：1997-07-18

申请人： Helmut Momberger ,  Marc Raber ,  Dieter Kuhn ,  Wolfgang Schmid

发明人： Helmut Momberger ,  Marc Raber ,  Dieter Kuhn ,  Wolfgang Schmid

IPC分类号： A61P25/04 ,  A61K9/22 ,  A61K9/50 ,  A61K9/52 ,  A61K9/54 ,  A61K9/60 ,  A61K9/62 ,  A61K31/135 ,  A61K31/137 ,  A61P29/00

CPC分类号： A61K31/137 ,  A61K9/5078 ,  Y10S514/951

摘要： A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt. based on the active ingredient layer, the binder in the active ingredient layer is suitably a mixture of ethylcellulose and shellac, in a weight proportion suitably of from about 1:9 to about 9:1, the coating for retarding the release suitably contains from about 70% wt. to about 95% wt. based on the coating, of a substantially water-insoluble, pharmacologically inert, particulate material, and a binder; the pharmacologically inert, particulate material is suitably talcum, and the binder in the active ingredient layer is suitably identical to the binder in the coating.

摘要翻译： 一种多单位口服药物剂型，其在水溶性胶囊中或在片剂中压制的片剂中具有多个丸粒，其中每个丸粒包含（a）基本上惰性的核心，（b）惰性核心上的活性成分层， 并且包含（i）药理学活性的颗粒活性成分，（ii）非固定量的用于将活性成分粘附在惰性核上的粘合剂，以及任选地（iii）药学上可接受的惰性佐剂，例如胶体二氧化硅和（ c）活性成分层上的涂层，用于阻止活性成分从活性成分层原位释放到体液溶剂中，非粘合剂量的粘合剂适宜为约1重量％ 至约10重量％ 基于活性成分层，活性成分层中的粘合剂适当地为乙基纤维素和虫胶的混合物，其重量比适当地为约1:9至约9:1，用于延缓释放的涂层适当地含有约 70％wt 至约95重量％ 基于涂层，基本上不溶于水的，药理惰性的颗粒材料和粘合剂; 药理学惰性的颗粒材料适当地是滑石粉，并且活性成分层中的粘合剂适当地与涂层中的粘合剂相同。

公开(公告)号：US06436438B1

公开(公告)日：2002-08-20

申请号：US09349564

申请日：1999-07-08

申请人： Helmut Momberger ,  Marc Raber ,  Dieter Kuhn ,  Wolfgang Schmid

发明人： Helmut Momberger ,  Marc Raber ,  Dieter Kuhn ,  Wolfgang Schmid

IPC分类号： A61K922

CPC分类号： A61K31/137 ,  A61K9/5078 ,  Y10S514/951

摘要： A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt. based on the active ingredient layer, the binder in the active ingredient layer is suitably a mixture of ethylcellulose and shellac, in a weight proportion suitably of from about 1: about 9, to from about 9: about 1, the coating for retarding the release suitably contains from about 70% wt. to about 95% wt. based on the coating, of a substantially water-insoluble, pharmacologically inert, particulate material, and a binder; the pharmacologically inert, particulate material is suitably talcum, and the binder in the active ingredient layer is suitably identical to the binder in the coating.

摘要翻译： 一种多单位口服药物剂型，其在水溶性胶囊中或在片剂中压制的片剂中具有多个丸粒，其中每个丸粒包含（a）基本上惰性的核心，（b）惰性核心上的活性成分层， 并且包含（i）药理学活性的颗粒活性成分，（ii）非固定量的用于将活性成分粘附在惰性核上的粘合剂，以及任选地（iii）药学上可接受的惰性佐剂，例如胶体二氧化硅和（ c）活性成分层上的涂层，用于阻止活性成分从活性成分层原位释放到体液溶剂中，非粘合剂量的粘合剂适宜为约1重量％ 至约10重量％ 基于活性成分层，活性成分层中的粘合剂合适地是乙基纤维素和虫胶的混合物，其重量比适当地为约1：约9至约9：约1，用于延缓释放的涂层 合适地含有约70重量％ 至约95重量％ 基于涂层，基本上不溶于水的，药理惰性的颗粒材料和粘合剂; 药理学惰性的颗粒材料适当地是滑石粉，并且活性成分层中的粘合剂适当地与涂层中的粘合剂相同。

公开(公告)号：US06667058B1

公开(公告)日：2003-12-23

申请号：US08212578

申请日：1994-03-17

申请人： Joachim Goede ,  Helmut Hettche ,  Helmut Momberger ,  Jürgen Engel ,  Michael Lobisch

发明人： Joachim Goede ,  Helmut Hettche ,  Helmut Momberger ,  Jürgen Engel ,  Michael Lobisch

IPC分类号： A61K908

CPC分类号： A61K31/44 ,  A61K9/2077 ,  A61K9/209 ,  A61K9/5078 ,  A61K9/5084

摘要： Pharmaceutical dosage units containing flupirtine or a pharmaceutically acceptable salt of flupirtine with controlled release of active substance using a delayed-action or controlled-release component. There are 0.001 to 20 parts delayed-action component for each part by weight flupirtine (calculated as the base) and the release rate of flupirtine is between 5 and 300 mg per hour. In some cases, the dosage units may also contain a rapidly releasing component of flupirtine or of one of its salts. The dosage units reduce the sedative effect of flupirtine.

摘要翻译： 含有氟吡汀或氟吡汀药学上可接受的盐的药物剂量单位，其使用延迟作用或控制释放组分控制释放活性物质。 对于每份重量的氟吡汀（以碱为基准计），有0.001-20份延迟作用组分，氟吡汀的释放速率为5至300mg /小时。 在一些情况下，剂量单位还可以含有氟吡汀或其一种盐的快速释放组分。 剂量单位降低氟吡汀的镇静作用。

公开(公告)号：US06376550B1

公开(公告)日：2002-04-23

申请号：US09247204

申请日：1999-02-09

申请人： Marc Raber ,  Helmut Momberger

发明人： Marc Raber ,  Helmut Momberger

IPC分类号： A61K31133

CPC分类号： A61K31/135 ,  A61K45/06 ,  A61K2300/00

摘要： A method for treating migraine is disclosed in which a composition consisting essentially of pharmacologically effective amounts of both an antiemetic compound and tramadol is administered to a patient in need thereof.

摘要翻译： 公开了一种治疗偏头痛的方法，其中基本上由药理学有效量的止吐化合物和曲马多组成的组合物施用于有需要的患者。