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1. 发明公开

EP2429498A4 NEW ORAL FORMULATIONS FOR TETRAPYRROLE DERIVATIVES 审中-公开
标题翻译： NEUE ORALE FORMULIERUNGENFÜRTETRAPYRROL-DERIVATE
公开(公告)号：EP2429498A4
公开(公告)日：2013-02-06
申请号：EP10772566
申请日：2010-04-28
申请人： CERAMOPTEC GMBH , BIOLITEC RES GMBH
发明人： GRAEFE SUSANNA , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , GERHARD WIELAND , WIEHE ARNO , FAHR ALBERT
IPC分类号： A61K9/16 , A61K9/127 , A61K9/20 , A61K31/122 , A61K31/409 , A61K31/495 , A61P31/04 , A61P35/00
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了光动力治疗（PDT）和抗微生物光动力治疗（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于粘膜粘附和通过胃肠粘膜吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，Alpha-Feto蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，口服制剂使用合适的表面活性剂/增溶剂稳定，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在施用PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为在哺乳动物体内没有可以代谢Temoporfin或类似光敏剂的已知的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

2. 发明公开

EP2424536A4 NOVEL PHOTOSENSITIZER FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：新生儿维生素A
公开(公告)号：EP2424536A4
公开(公告)日：2012-10-31
申请号：EP10772569
申请日：2010-04-28
申请人： CERAMOPTEC GMBH , BIOLITEC RES GMBH
发明人： FARMER GERARD , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , WIELAND GERHARD , WIEHE ARNO , GRAEFE SUSANNA
IPC分类号： A61K31/498 , A61K31/122 , A61K31/40 , A61P31/04 , A61P35/00
CPC分类号： A61K31/122 , A61K31/40 , A61K31/498 , A61K41/0071
摘要： The present invention provides novel drug formulations for oral administration for diverse medical applications including anticancer, antimetastatic, antibacterial, antifungal, antiprotozoic, antiviral, antiprionic and PDT treatments for diagnostic and therapeutic purposes. In a preferred embodiment the oral drug formulation comprises a photosensitizer and suitable excipients and may be administered in multiple doses over an extended period of time with exposure to activating radiation occurring generally between individual doses or in a light-independent manner. In another preferred embodiment PDT methods for treating hyperplasia and neoplasia, for localizing hyperplasic and neoplasic tissues and pathogen bacteria by fluorescence, for treating infections caused by pathogen bacteria in complex body fluids and for fat reduction, skin disorders and vascular diseases are provided.
摘要翻译：本发明提供用于口服给药以用于多种医学应用的新型药物制剂，包括用于诊断和治疗目的的抗癌，抗转移，抗细菌，抗真菌，抗原生动脉，抗病毒，止痒和PDT治疗。在优选的实施方案中，口服药物制剂包含光敏剂和合适的赋形剂，并且可以在长时间内以多个剂量施用，其中暴露于通常在单独剂量之间或以不依赖光的方式发生的活化辐射。在另一个优选实施方案中，提供了用于治疗增生和瘤形成的PDT方法，用于通过荧光定位增生和新生组织和病原体细菌，用于治疗复杂体液中由病原体细菌引起的感染和用于减脂，皮肤病和血管疾病。

3. 发明公开

EP1660041A4 NON-POLAR PHOTOSENSITIZER FORMULATIONS FOR PHOTODYNAMIC THERAPY 有权转让
标题翻译：不是两极的光敏剂制剂的光动力疗法
公开(公告)号：EP1660041A4
公开(公告)日：2010-01-27
申请号：EP04776989
申请日：2004-06-23
申请人： CERAMOPTEC GMBH
发明人： ALBRECHT VOLKER , FAHR ALFRED , SCHEGLMANN DIETRICH , GRAEFE SUSANNA , NEUBERGER WOLFGANG
IPC分类号： A61K9/127 , A61K41/00
CPC分类号： A61K41/0071 , A61K9/127

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