公开(公告)号：US06599529B1

公开(公告)日：2003-07-29

申请号：US09508594

申请日：2000-07-17

申请人： Annette Skinhøj ,  Poul Bertelsen

发明人： Annette Skinhøj ,  Poul Bertelsen

IPC分类号： A61K954

CPC分类号： A61K9/2081 ,  A61K9/5084 ,  A61K31/542 ,  A61K45/06

摘要： An oral pharmaceutical modified release multiple-units composition for the administration of a therapeutically and/or prophylactically effective amount of a non-steroid anti-inflammatory drug substance to obtain both a relatively fast onset of the therapeutic effect and the maintenance of a therapeutically active plasma concentration for a relatively long period of time is disclosed.

摘要翻译： 一种用于施用治疗和/或预防有效量的非类固醇抗炎药物的口服药物改良释放多单元组合物，以获得治疗效果相对较快发作和维持治疗活性血浆 浓度相对较长的时间被公开。

公开(公告)号：US07070803B2

公开(公告)日：2006-07-04

申请号：US09823202

申请日：2001-03-29

申请人： Annette Skinhøj ,  Peder Mohr Olsen ,  Poul Bertelsen

发明人： Annette Skinhøj ,  Peder Mohr Olsen ,  Poul Bertelsen

IPC分类号： A61K9/16 ,  A61K9/22 ,  A61K9/52

CPC分类号： B82Y5/00 ,  A61K9/5078 ,  A61K31/137 ,  A61K31/165

摘要： Novel controlled release pharmaceutical compositions for oral use containing midodrine and/or its active metabolite desglymidodrine. The novel compositions are designed to release midodrine and/or desglymidodrine after oral intake in a manner which enables absorption to take place in the gastrointestinal tract so that a relatively fast peak plasma concentration of the active metabolite desglymidodrine is obtained followed by a prolonged and relatively constant plasma concentration of desglymidodrine.The novel compositions may be designed for administration once or twice daily, i.e. a therapeutically effective concentration of desglymidodrine is maintained for a period of at least 10-16 hours followed by a wash out period of about 8-12 hours in order to avoid the well-known midodrine related side effect with respect to supine hypertension. The therapeutically effective concentration of desglymidodrine is regarded as a plasma concentration of desglymidodrine of at least about 3 ng/ml. A composition is designed to release midodrine and/or desglymidodrine in at least the following consecutive steps: i) an initial relatively fast release of midodrine and/or desglymidodrine (in order to obtain a relatively fast onset of action), ii) a steady release or a slower release than in step 1 of midodrine and/or desglymidodrine (in order to maintain a plasma concentration of desglymidodrine which is prolonged and relatively constant), iii) a second rise in release of midodrine and/or desglymidodrine (in order to take advantage of absorption from the colon, i.e. such a second rise release is designed to take place when the composition (or the disintegrated parts of the composition) reaches the colon; normally this is regarded to take about 8 hours after oral intake, and iv) a decline in release rate corresponding to that essentially all midodrine and/or desglymidodrine have been released from the composition.Also disclosed is a method for treating orthostatic hypotension and/or urinary incontinence, the method comprising administration to a patient in need thereof of an effective amount of midodrine and/or desglymidodrine in a composition according to the invention.

公开(公告)号：US06761904B2

公开(公告)日：2004-07-13

申请号：US09823093

申请日：2001-03-29

申请人： Poul Bertelsen ,  Annette Skinhøj ,  Peder Mohr Olsen

发明人： Poul Bertelsen ,  Annette Skinhøj ,  Peder Mohr Olsen

IPC分类号： A61K920

CPC分类号： A61K9/0095 ,  A61K9/0031 ,  A61K9/0043 ,  A61K9/0056 ,  A61K9/0063 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/008 ,  A61K9/127 ,  A61K9/2072 ,  A61K9/209 ,  A61K9/2886 ,  A61K9/4808 ,  A61K9/5073 ,  A61K9/5078 ,  A61K31/137 ,  A61K31/165 ,  A61K47/18

摘要： The invention provides a novel pharmaceutical kit comprising a controlled release pharmaceutical compositions for oral use containing midodrine and/or its active metabolite desglymidodrine. The controlled release composition is designed to release midodrine and/or desglymidodrine after oral intake in a manner which enables absorption to take place in the gastrointestinal tract so that a relatively fast peak plasma concentration of the active metabolite desglymidodrine is obtained, followed by a prolonged and relatively constant plasma concentration of desglymidodrine. The invention also provides a method for treating orthostatic hypotension and/or urinary incontinence, the method comprising administration to a patient in need thereof of an effective amount of midodrine and/or desglymidodrine in a kit.

摘要翻译： 本发明提供了一种新颖的药物试剂盒，其包含含有米多君和/或其活性代谢物去糖质胞苷的用于口服的控释药物组合物。 控制释放组合物被设计为在口服摄入后以能够在胃肠道中进行吸收的方式释放midodrine和/或desglymidodrine，从而获得活性代谢物desglymidodrine的相对快速的峰值血浆浓度，随后延长和 相对恒定的血浆浓度的desglymidodrine。 本发明还提供了一种治疗体位性低血压和/或尿失禁的方法，所述方法包括向有需要的患者施用试剂盒中有效量的米多君和/或去糖质鼠。