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    • 1. 发明授权
    • Oral formulations for tetrapyrrole derivatives
    • 四吡咯衍生物的口服制剂
    • US08815931B2
    • 2014-08-26
    • US12768244
    • 2010-04-27
    • Susanna GräfeNikolay NifantievAlbrecht VolkerWolfgang NeubergerGerhard WielandDietrich ScheglmannAlfred FahrArno Wiehe
    • Susanna GräfeNikolay NifantievAlbrecht VolkerWolfgang NeubergerGerhard WielandDietrich ScheglmannAlfred FahrArno Wiehe
    • A61K31/40A61K9/127A61K31/498A61K9/00A61K31/409
    • A61K31/409A61K9/0065A61K9/127A61K9/1271A61K31/498
    • 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.
    • 提出了在光动力治疗(PDT)和抗微生物光动力疗法(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通过胃肠粘膜进行粘膜粘附和吸收。 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,α-铁蛋白(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,使用合适的表面活性剂/增溶剂稳定口服制剂,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。 配制药物可以在给予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,因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 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. 发明申请
    • Oral Formulations for Tetrapyrrole Derivatives
    • 四吡咯衍生物的口服制剂
    • US20100273803A1
    • 2010-10-28
    • US12768244
    • 2010-04-27
    • Susanna GräfeNikolay NifantievAlbrecht VolkerWolfgang NeubergerGerhard WielandDietrich ScheglmannAlfred FahrArno Wiehe
    • Susanna GräfeNikolay NifantievAlbrecht VolkerWolfgang NeubergerGerhard WielandDietrich ScheglmannAlfred FahrArno Wiehe
    • A61K31/498C07D241/46A61K31/409C07D487/22A61P35/00A61P31/00A61K8/49A61Q19/00A61Q9/00
    • A61K31/409A61K9/0065A61K9/127A61K9/1271A61K31/498
    • 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.
    • 提出了在光动力治疗(PDT)和抗微生物光动力疗法(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通过胃肠粘膜进行粘膜粘附和吸收。 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,α-铁蛋白(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,使用合适的表面活性剂/增溶剂稳定口服制剂,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。 配制药物可以在给予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,因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 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。
    • 5. 发明授权
    • Liposomal formulations of hydrophobic photosensitizer for photodynamic therapy
    • 用于光动力疗法的疏水性光敏剂的脂质体制剂
    • US07354599B2
    • 2008-04-08
    • US11298729
    • 2005-12-09
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GräfeWolfgang Neuberger
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GräfeWolfgang Neuberger
    • A61K9/127
    • A61K41/0071A61K9/127
    • Pharmaceutical liposomal formulations are described for photodynamic therapy comprising a, hydrophobic porphyrin photosensitizer, a monosaccharide and one or more synthetic phospholipids, which are stable in storage especially through freeze-drying process. The liposomal formulations provide therapeutically effective amounts of the photosensitizer for intravenous administration. In particular derivatives of chlorins and bacteriochlorins, such as temoporfin, are, hydrophobic photosensitizers whose efficacy and safety are enhanced by such liposomal formulations. The formulation can be efficiently freeze-dried preserving the size of the liposomal vehicles, and the content of a therapeutically effective amount of the photosensitizer, due to the selection of phospholipids and monosaccharides. The invention also relates to liposome compositions formed upon reconstitution with an aqueous vehicle. The freeze-dried formulation upon reconstitution with a suitable aqueous vehicle forms liposomes that are useful for intravenous administration.
    • 描述了用于光动力学治疗的药物脂质体制剂,其包括疏水性卟啉光敏剂,单糖和一种或多种合成磷脂,其特别通过冷冻干燥方法在储存中稳定。 脂质体制剂提供治疗有效量的用于静脉内给药的光敏剂。 特别是二氢卟酚和细菌二氢卟酚的衍生物,如temoporfin,是通过这种脂质体制剂增强其功效和安全性的疏水性光敏剂。 由于磷脂和单糖的选择,制剂可以有效地冷冻干燥,保持脂质体载体的大小和治疗有效量的光敏剂的含量。 本发明还涉及在用水性载体重建时形成的脂质体组合物。 用合适的水性载体重建后的冷冻干燥制剂形成可用于静脉内给药的脂质体。
    • 6. 发明申请
    • Hydrophobic photosensitizer formulations for photodynamic therapy
    • 用于光动力疗法的疏水性光敏剂配方
    • US20060159740A1
    • 2006-07-20
    • US11384767
    • 2006-03-20
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • A61K31/409A61K31/555A61K9/127
    • A61K41/0071A61K9/127
    • Pharmaceutical liposomal formulations for photodynamic therapy are presented, which are stable in storage as liquid formulations, comprise a hydrophobic photosensitizer and one or more synthetic phospholipids. The liposomal formulations provide therapeutically effective amounts of the photosensitizer for intravenous administration. The formed liposomes contain the hydrophobic photosensitizer within the lipid bilayer membrane. In the present formulation the size of the liposomal vehicles and their content of a therapeutically effective amount of the photosensitizing agent remain unchanged over storage times of a year or more, thus making the liquid formulations commercially viable. Being stable in the liquid state also makes them easy to store, and easier to use for doctors and patients. They can be prepared in a ‘factory setting’ delivered to practitioners in a liquid state and be available for use in PDT related treatments as called for by the practitioners' patient needs.
    • 提出了用于光动力学治疗的药物脂质体制剂,其作为液体制剂在储存中稳定,包含疏水性光敏剂和一种或多种合成磷脂。 脂质体制剂提供治疗有效量的用于静脉内给药的光敏剂。 形成的脂质体在脂质双层膜内含有疏水性光敏剂。 在本发明的制剂中,脂质体载体的大小及其治疗有效量的光敏剂的含量在一年以上的保存时间内保持不变,从而使液体制剂在商业上可行。 在液体状态下稳定也使得它们易于储存,并且更容易用于医生和患者。 他们可以在“工厂设置”下准备就绪,以液体状态送达医生,并可根据医生的病人需要进行PDT相关治疗。
    • 7. 发明申请
    • Non-polar photosensitizer formulations for photodynamic therapy
    • 用于光动力疗法的非极性光敏剂配方
    • US20050048109A1
    • 2005-03-03
    • US10648168
    • 2003-08-26
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • A61K9/127A61K41/00
    • A61K41/0071A61K9/127
    • A pharmaceutical liposomal formulation for photodynamic therapy comprising a non-polar porphyrin photosensitizer and one or more phospholipids, which are stable in storage without requiring freeze-drying is described. The liposomal formulation provides therapeutically effective amounts of the photosensitizer for intravenous administration. The phospholipids may be modified by pegylation, i.e. they contain poly ethylene glycol as an integral part of the phospholipids. The formed liposomes contain the non-polar photosensitizer within the membrane and are useful for the combined targeting of a non-polar photosensitizer and a second polar substance. When a formulation includes the presence of monosaccharides or polyalcohols, it can be efficiently freeze-dried preserving the size of the liposomal vehicles and the content of a therapeutically effective amount of the photosensitizing agent. The invention also relates to the liposome composition formed upon reconstitution with an aqueous vehicle. The freeze-dried formulation upon reconstitution with a suitable aqueous vehicle forms liposomes that are also useful for intravenous administration.
    • 描述了一种用于光动力疗法的药物脂质体制剂,其包含非极性卟啉光敏剂和一种或多种在不需要冷冻干燥的情况下在储存中稳定的磷脂。 脂质体制剂提供治疗有效量的用于静脉内施用的光敏剂。 可以通过聚乙二醇化来改变磷脂,即它们含有聚乙二醇作为磷脂的组成部分。 形成的脂质体在膜内含有非极性光敏剂,并且可用于非极性光敏剂和第二极性物质的组合靶向。 当制剂包含单糖或多元醇的存在时,可有效地冷冻干燥保存脂质体载体的大小和治疗有效量的光敏剂的含量。 本发明还涉及在与水性载体重建时形成的脂质体组合物。 用合适的水性载体重构后的冷冻干燥制剂形成也可用于静脉内施用的脂质体。
    • 8. 发明申请
    • Liposomal formulations of hydrophobic photosensitizer for photodynamic therapy
    • 用于光动力疗法的疏水性光敏剂的脂质体制剂
    • US20060088584A1
    • 2006-04-27
    • US11298729
    • 2005-12-09
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • Volker AlbrechtAlfred FahrDietrich ScheglmannSusanna GrafeWolfgang Neuberger
    • A61K9/127A61K31/70A61K31/409
    • A61K41/0071A61K9/127
    • Pharmaceutical liposomal formulations are described for photodynamic therapy comprising a, hydrophobic porphyrin photosensitizer, a monosaccharide and one or more synthetic phospholipids, which are stable in storage especially through freeze-drying process. The liposomal formulations provide therapeutically effective amounts of the photosensitizer for intravenous administration. In particular derivatives of chlorins and bacteriochlorins, such as temoporfin, are, hydrophobic photosensitizers whose efficacy and safety are enhanced by such liposomal formulations. The formulation can be efficiently freeze-dried preserving the size of the liposomal vehicles, and the content of a therapeutically effective amount of the photosensitizer, due to the selection of phospholipids and monosaccharides. The invention also relates to liposome compositions formed upon reconstitution with an aqueous vehicle. The freeze-dried formulation upon reconstitution with a suitable aqueous vehicle forms liposomes that are useful for intravenous administration.
    • 描述了用于光动力学治疗的药物脂质体制剂,其包括疏水性卟啉光敏剂,单糖和一种或多种合成磷脂,其特别通过冷冻干燥方法在储存中稳定。 脂质体制剂提供治疗有效量的用于静脉内给药的光敏剂。 特别是二氢卟酚和细菌二氢卟酚的衍生物,如temoporfin,是通过这种脂质体制剂增强其功效和安全性的疏水性光敏剂。 由于磷脂和单糖的选择,制剂可以有效地冷冻干燥,保持脂质体载体的大小和治疗有效量的光敏剂的含量。 本发明还涉及在用水性载体重建时形成的脂质体组合物。 用合适的水性载体重建后的冷冻干燥制剂形成可用于静脉内给药的脂质体。