公开(公告)号：US20050106241A1

公开(公告)日：2005-05-19

申请号：US10957947

申请日：2004-10-04

申请人： Francesca Brewer ,  Edward Johnson ,  Anthony Clarke

发明人： Francesca Brewer ,  Edward Johnson ,  Anthony Clarke

IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K31/136 ,  A61K31/137

CPC分类号： A61K9/0056 ,  A61K9/2095 ,  A61K31/136 ,  A61K31/137

摘要： The invention described herein provides a fast dispersing oral solid dosage form containing monoamine oxidase B inhibitor (MAO-B inhibitor) as the active ingredient, and method of treating disease therewith, such as Parkinson's disease. In one embodiment, the monoamine oxidase B inhibitor selegiline or its analogue can be the sole active ingredient in the composition administered. The dosage form composition is formulated to promote absorption through the buccal, sublingual, pharyngeal and/or esophageal mucous membrane tissue, such that at least 5% of the active ingredient is absorbed within one minute of placement in the oral cavity, as determined by a buccal absorption test. Monoamine oxidase B inhibitor compounds administered in accordance with the invention decrease the amount of undesirable metabolites associated with first pass effect of selegiline, for example, such as amphetamine and methamphetamine. The invention provides a number of other advantages over conventional orally administered tablet forms, including administration of monoamine oxidase B inhibitor compounds to patients that have difficulty swallowing.

摘要翻译： 本文描述的本发明提供了含有单胺氧化酶B抑制剂（MAO-B抑制剂）作为活性成分的快速分散口服固体剂型，以及用于治疗疾病如帕金森病的方法。 在一个实施方案中，单胺氧化酶B抑制剂司来吉兰或其类似物可以是所施用组合物中的唯一活性成分。 配制剂型组合物以促进通过颊，舌下，咽和/或食管粘膜组织的吸收，使得至少5％的活性成分在放置在口腔中的一分钟内被吸收，如通过 颊吸收试验。 根据本发明施用的单胺氧化酶B抑制剂化合物减少与司来吉兰（例如苯丙胺和甲基苯丙胺）的首次通过效应相关的不合需要的代谢物的量。 本发明提供了与常规口服给药的片剂形式相比的许多其它优点，包括向吞咽困难的患者施用单胺氧化酶B抑制剂化合物。