公开(公告)号：US06455526B1

公开(公告)日：2002-09-24

申请号：US09454555

申请日：1999-12-07

申请人： Rachel S. Kohn ,  Stephen J. Hanley ,  Stephen J. Comiskey

发明人： Rachel S. Kohn ,  Stephen J. Hanley ,  Stephen J. Comiskey

IPC分类号： A61K31495

CPC分类号： A61K31/50 ,  A61K9/1647 ,  A61K9/1694 ,  A61K31/495

摘要： A new class of biodegradable pharmaceutical compositions useful as sustained release medicamentous compositions, including methods of making and methods of using these compositions, are described and claimed. The method of making these compositions include the steps of: a) dry mixing of a pharmaceutically active molecule with a biodegradable polymer; b) melt extruding the mixture to form a solid solution of the active molecule in the polymer; and c) pulverizing the solid solution to form microparticles such that they can be formed into injectable formulations. Preferred embodiments include pharmaceutical compositions of polylactide-co-glycolide and (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol (active ingredient) and a method for its formation. These compositions release the active ingredient at a steady rate over a period of days to weeks. The active ingredient antagonizes the effects of serotonin at the 5HT2A receptor and are useful in treating various conditions such as, for example, psychoses including schizophrenia, obsessive compulsive disorder, sleep disorder, depression, anorexia, anxiety, drug addiction and bipolar disorders.

摘要翻译： 描述和要求保护的一类新的可生物降解的药物组合物，其用作缓释药物组合物，包括制备方法和使用这些组合物的方法。 制备这些组合物的方法包括以下步骤：a）将药物活性分子与可生物降解的聚合物干混; b）熔融挤出混合物以形成聚合物中活性分子的固溶体; 和c）粉碎固溶体以形成微粒，使得它们可以形成可注射制剂。 优选的实施方案包括聚丙交酯 - 共 - 乙交酯和（+） - α-（2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇（活性成分）的药物组合物和 其形成。 这些组合物在几天到数周的时间内以稳定的速率释放活性成分。 活性成分拮抗5-羟色胺在5HT2A受体上的作用，可用于治疗各种病症，例如精神病，包括精神分裂症，强迫症，睡眠障碍，抑郁症，厌食症，焦虑症，药物成瘾和双相性精神障碍。

公开(公告)号：US06946118B1

公开(公告)日：2005-09-20

申请号：US09661836

申请日：2000-09-14

申请人： James Ronald Lawter ,  Stephen J. Comiskey

发明人： James Ronald Lawter ,  Stephen J. Comiskey

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K31/65 ,  A61K47/36 ,  A61P1/00 ,  A61K9/14 ,  A61K7/16 ,  A61K9/10 ,  A61K9/20

CPC分类号： A61K31/65 ,  A61K9/006 ,  A61K9/0095 ,  A61K9/1652 ,  A61K9/1676 ,  A61K47/36 ,  Y10S514/901

摘要： Mucositis is treated and/or prevented by administrating to a patient a formulation comprising a tetracycline that is poorly absorbed from the gastro-intestinal tract. The tetracycline may be in the form of a pharmaceutically acceptable salt or a base. The formulations may optionally also contain an antifungal agent to prevent fungal overgrowth due to reduction in the normal oral flora by the tetracycline. Such compositions have the advantage of treating the entire gastro-intestinal tract since the active ingredient is not removed from the tract via absorption. Further, such compositions minimize systemic exposure and accompanying side effects.

摘要翻译： 通过向患者施用包含从胃肠道吸收不良的四环素的制剂来治疗和/或预防粘膜炎。 四环素可以是药学上可接受的盐或碱的形式。 制剂还可任选地含有抗真菌剂，以防止由四环素引起的正常口腔菌群减少引起的真菌过度生长。 这样的组合物具有治疗整个胃肠道的优点，因为活性成分不通过吸收从道路中除去。 此外，这样的组合物使全身暴露和伴随的副作用最小化。

公开(公告)号：US06893665B2

公开(公告)日：2005-05-17

申请号：US10007197

申请日：2001-12-04

申请人： James Ronald Lawter ,  Stephen J. Comiskey

发明人： James Ronald Lawter ,  Stephen J. Comiskey

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K31/65 ,  A61K47/36 ,  A61P1/00 ,  A61K7/16 ,  A61K9/127 ,  A61K9/20

CPC分类号： A61K31/65 ,  A61K9/006 ,  A61K9/0095 ,  A61K9/1652 ,  A61K9/1676 ,  A61K47/36 ,  Y10S514/901

摘要： Mucositis is treated and/or prevented by administrating to a patient a formulation comprising a tetracycline that is poorly absorbed from the gastro-intestinal tract. The tetracycline may be in the form of a pharmaceutically acceptable salt or a base. The formulations may optionally also contain an antifungal agent to prevent fungal overgrowth due to reduction in the normal oral flora by the tetracycline. Such compositions have the advantage of treating the entire gastro-intestinal tract since the active ingredient is not removed from the tract via absorption. Further, such compositions minimize systemic exposure and accompanying side effects.

公开(公告)号：US06683067B2

公开(公告)日：2004-01-27

申请号：US09815762

申请日：2001-03-23

申请人： James Ronald Lawter ,  Stephen J. Comiskey

发明人： James Ronald Lawter ,  Stephen J. Comiskey

IPC分类号： A61K3105

CPC分类号： A61K31/65 ,  A61K9/006 ,  A61K9/0095 ,  A61K9/1652 ,  A61K9/1676 ,  A61K47/36 ,  Y10S514/901

摘要： Mucositis is treated and/or prevented by administrating to a patient a formulation comprising a tetracycline that is poorly absorbed from the gastro-intestinal tract. The tetracycline may be in the form of a pharmaceutically acceptable salt or a base. The formulations may optionally also contain an antifungal agent to prevent fungal overgrowth due to reduction in the normal oral flora by the tetracycline. Such compositions have the advantage of treating the entire gastro-intestinal tract since the active ingredient is not removed from the tract via absorption. Further, such compositions minimize systemic exposure and accompanying side effects.

摘要翻译： 通过向患者施用包含从胃肠道吸收不良的四环素的制剂来治疗和/或预防粘膜炎。 四环素可以是药学上可接受的盐或碱的形式。 制剂还可任选地含有抗真菌剂，以防止由四环素引起的正常口腔菌群减少引起的真菌过度生长。 这样的组合物具有治疗整个胃肠道的优点，因为活性成分不通过吸收从道路中除去。 此外，这样的组合物使全身暴露和伴随的副作用最小化。