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1.发明申请Pharmaceutical presentation form for oral administration of a poorly soluble active compound, process for its preparation and kit 审中-公开用于口服不溶性活性化合物的药物呈递形式，其制备方法和试剂盒公开(公告)号：US20060040991A1
公开(公告)日：2006-02-23
申请号：US11169407
申请日：2005-06-29
申请人： Berthold Roessler
发明人： Berthold Roessler
IPC分类号： A61K31/4439
CPC分类号： A61K31/4439
摘要： The invention relates to a pharmaceutical presentation form for the oral administration of indibulin in the form of an aqueous drink solution, and a method for its preparation.
摘要翻译： 本发明涉及以饮料水溶液的形式口服靛蓝的药物呈递形式及其制备方法。
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2.发明授权公开(公告)号：US07884071B2
公开(公告)日：2011-02-08
申请号：US10529203
申请日：2003-09-26
申请人： Horst Bauer , Thomas Reissmann , Peter Romeis , Berthold Roessler
发明人： Horst Bauer , Thomas Reissmann , Peter Romeis , Berthold Roessler
IPC分类号： A61K38/22 , C07K14/575 , C07K14/59
CPC分类号： A61K9/06 , A61K9/0019 , A61K9/0024 , A61K9/19 , A61K47/02 , A61K47/12 , A61K47/26
摘要： The invention relates to pharmaceutical administration forms with sustained release comprising at least one pharmacologically active peptide. The invention also relates to a method for the production thereof, a kit comprising a lyophilised peptide and an aqueous solution of an inorganic salt or acetic acid salt and the use of an aqueous solution of an inorganic or acetic acid salt for producing a pharmaceutical administration form which releases peptides in a continuous manner over a long period of time.
摘要翻译： 本发明涉及具有持续释放的药物施用形式，其包含至少一种药理学活性肽。 本发明还涉及其制备方法，包含冻干肽和无机盐或乙酸盐的水溶液的试剂盒，以及使用无机或乙酸盐的水溶液来制备药物给药形式 其在长时间内以连续的方式释放肽。
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3.发明申请TROFOSFAMIDE-CONTAINING FILM-COATED TABLETS AND METHOD FOR THE PRODUCTION THEREOF 审中-公开含有呋喃并菲的薄膜包衣片及其生产方法公开(公告)号：US20090117186A1
公开(公告)日：2009-05-07
申请号：US11816391
申请日：2006-02-10
申请人： Berthold Roessler
发明人： Berthold Roessler
CPC分类号： A61K9/2866 , A61K9/2846 , A61K31/675
摘要： The invention at hand concerns trofosfamide containing film-coated tablets for oral application and a procedure for their production.
摘要翻译： 本发明涉及用于口服应用的含有片剂的膜包衣片剂及其制备方法。
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4.发明申请公开(公告)号：US20050282731A1
公开(公告)日：2005-12-22
申请号：US10529203
申请日：2003-09-26
申请人： Horst Bauer , Thomas Reissmann , Peter Romeis , Berthold Roessler
发明人： Horst Bauer , Thomas Reissmann , Peter Romeis , Berthold Roessler
IPC分类号： A61K38/09 , A61K9/00 , A61K9/06 , A61K9/19 , A61K38/22 , A61K47/02 , A61K47/12 , A61K47/26 , C07K7/23
CPC分类号： A61K9/06 , A61K9/0019 , A61K9/0024 , A61K9/19 , A61K47/02 , A61K47/12 , A61K47/26
摘要： The invention relates to pharmaceutical administration forms with sustained release comprising at least one pharmacologically active peptide. The invention also relates to a method for the production thereof, a kit comprising a lyophilised peptide and an aqueous solution of an inorganic salt or acetic acid salt and the use of an aqueous solution of an inorganic or acetic acid salt for producing a pharmaceutical administration form which releases peptides in a continuous manner over a long period of time.
摘要翻译： 本发明涉及具有持续释放的药物施用形式，其包含至少一种药理学活性肽。 本发明还涉及其制备方法，包含冻干肽和无机盐或乙酸盐的水溶液的试剂盒，以及使用无机或乙酸盐的水溶液来制备药物给药形式 其在长时间内以连续的方式释放肽。
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5.发明申请Pharmaceutical formulation of the tubulin inhibitor indibulin for oral administration with improved pharmacokinetic properties, and process for the manufacture thereof 审中-公开用于口服给药的微管蛋白抑制剂靛蓝的药物制剂具有改善的药代动力学性质，及其制备方法公开(公告)号：US20060280787A1
公开(公告)日：2006-12-14
申请号：US11151459
申请日：2005-06-14
CPC分类号： A61K9/1623 , A61K9/1652 , A61K31/4439 , Y02A50/465
摘要： The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 μm for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.
摘要翻译： 本发明涉及用于口服不溶性且因此难以生物利用的微管阻聚剂靛红纤维素的药物制剂及其制备方法。 特别地，提供了用于口服给药的靛蓝纤维素的药物制剂，其包含含有至少99％体积的颗粒，至少一种亲水性表面活性剂和至少一种亲水性表面活性剂的粒径小于20μm的微粉化靛蓝的颗粒 封装赋形剂。 本发明还公开了用靛蓝蛋白治疗过度增殖性疾病，恶性肿瘤和肿瘤的方法。
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6.发明申请公开(公告)号：US20050124589A1
公开(公告)日：2005-06-09
申请号：US10952027
申请日：2004-09-28
申请人： Berthold Roessler
发明人： Berthold Roessler
IPC分类号： A61K9/08 , A61K9/19 , A61K31/185 , A61K31/66 , A61K31/675 , A61K45/06 , A61K47/20 , A61K47/26 , A61P35/00
CPC分类号： A61K31/66 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/185 , A61K31/675 , A61K45/06 , A61K47/20 , A61K47/26 , A61K2300/00
摘要： The invention concerns the use of mercaptoethane sulfonate-sodium (Mesna) to increase the solubility of Ifosfamide in storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical preparations, storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical Ifosfamide preparations for parenteral administration as well as a process for their production.
摘要翻译： 本发明涉及巯基磺酸磺酸钠（Mesna）在储存稳定，浓缩和/或高度浓缩（过饱和的）水性药物制剂中的溶解度，储存稳定，浓缩和/或高度浓缩 过饱和）水性药物用于肠胃外给药的异环磷酰胺制剂以及其制备方法。
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公开(公告)号：US08093230B2
公开(公告)日：2012-01-10
申请号：US10952027
申请日：2004-09-28
申请人： Berthold Roessler
发明人： Berthold Roessler
IPC分类号： A61K31/665
CPC分类号： A61K31/66 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/185 , A61K31/675 , A61K45/06 , A61K47/20 , A61K47/26 , A61K2300/00
摘要： The invention concerns the use of mercaptoethane sulfonate-sodium (Mesna) to increase the solubility of Ifosfamide in storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical preparations, storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical Ifosfamide preparations for parenteral administration as well as a process for their production.
摘要翻译： 本发明涉及巯基磺酸磺酸钠（Mesna）在储存稳定，浓缩和/或高度浓缩（过饱和的）水性药物制剂中的溶解度，储存稳定，浓缩和/或高度浓缩 过饱和）水性药物用于肠胃外给药的异环磷酰胺制剂以及其制备方法。
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公开(公告)号：US20060110462A1
公开(公告)日：2006-05-25
申请号：US11266518
申请日：2005-11-03
申请人： Pavlos Papadopoulos , Gerhard Raab , Mark Doty , James Kipp , Berthold Roessler
发明人： Pavlos Papadopoulos , Gerhard Raab , Mark Doty , James Kipp , Berthold Roessler
IPC分类号： A61K31/4439 , A61K9/14
CPC分类号： C07D401/12 , A61K9/0019 , A61K9/0095 , A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/5123 , A61K9/5146 , A61K31/404 , A61K31/4439 , Y10T428/2982
摘要： The present invention is directed to novel pharmaceutical compositions comprising nano- and micro-particulate formulations of poorly water soluble tubulin inhibitors of the indole chemical class, preferably N-substituted indol-3-glyoxyamides, and more preferably N-(Pyridin-4-yl)-[1-(4-chlorobenzyl)-indol-3-yl]glyoxylic acid amide (D-24851), also known as “Indibulin,” and methods of making and using such compositions for the treatment of anti-tumor agent resistant cancers and other diseases.
摘要翻译： 本发明涉及新的药物组合物，其包含吲哚化学类的水难溶性微管蛋白抑制剂的纳米微粒和微粒制剂，优选N-取代的吲哚-3-乙酰氧基酰胺，更优选N-（吡啶-4-基 ） - 也称为“靛敏蛋白”的[1-（4-氯苄基） - 吲哚-3-基]乙醛酸酰胺（D-24851），以及制备和使用这些组合物用于治疗抗肿瘤药物抗性的方法 癌症等疾病。
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