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公开(公告)号：US20080113015A1
公开(公告)日：2008-05-15
申请号：US11569514
申请日：2005-05-24
IPC分类号： A61K9/127 , A61K38/16 , A61K31/715 , A61P43/00
CPC分类号： A61K9/1271
摘要： The present invention relates to liposomes for drug delivery, wherein a liposome includes molecules of at least one desired drug distributed within an aqueous phase in the interior of the liposome and wherein the liposome further includes molecules of the same or of another drug attached to either or both sides of the liposomal membrane. More specifically, the invention relates to liposomes, wherein at least a part of the molecules of a desired drug bear a functional group that is reactive with a functional group present in at least one lipid fraction, and wherein the drug is covalently linked to the membrane lipids by chemical bonding, e.g. by ester bonding of a hydroxyl group of a lipid molecule and an acidic residue of the drug. In a preferred embodiment, the desired drug is a glycoprotein such as erythropoietin. The invention further relates to a method of manufacture of said liposomes and to pharmaceutical compositions containing them.
摘要翻译： 本发明涉及用于药物递送的脂质体，其中脂质体包括分布在脂质体内部的水相内的至少一种所需药物的分子，并且其中所述脂质体还包括与所述脂质体或其它药物相连接的分子， 脂质体膜两侧。 更具体地，本发明涉及脂质体，其中所需药物的至少一部分分子具有与存在于至少一种脂质部分中的官能团反应的官能团，并且其中所述药物与膜共价连接 脂质通过化学键合，例如 通过脂质分子的羟基和药物的酸性残基的酯键合。 在优选的实施方案中，所需药物是糖蛋白，例如红细胞生成素。 本发明还涉及制备所述脂质体的方法和含有它们的药物组合物。
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2.发明申请LIPOSOMAL COMPOSITION COMPRISING AN ACTIVE INGREDIENT FOR RELAXING SMOOTH MUSCLE, THE PRODUCTION OF THIS COMPOSITION AND THE THERAPEUTIC USE THEREOF 有权包含用于放松平滑肌肉的活性成分的脂质组合物，该组合物的生产及其治疗用途公开(公告)号：US20090324698A1
公开(公告)日：2009-12-31
申请号：US11577488
申请日：2005-10-14
IPC分类号： A61K9/127 , A61P15/00 , A61K31/519 , A61K31/4985
CPC分类号： A61K9/127 , A61K9/0034 , A61K9/06 , A61K9/1277 , A61K9/1278
摘要： The invention relates to a pharmaceutical composition made from an active ingredient included in liposomes for topical application, whereby the liposomes have an aqueous medium in the interior thereof and contain at least one active ingredient therein which exerts a direct or indirect relaxing effect on smooth musculature and is preferably selected from the group of prostaglandins, adenylate cyclases, cAMP, AMP, ATP, NO-synthetases, nitrogen monoxide (NO), NO compounds, nitrates, guanylate cyclases, cGMP, GMP, GTP and phosphodiesterases, in particular, Sildenafil. The invention further relates to a method for production of said composition, optionally, in sterile form and the use of the liposomes supporting the active ingredient in various galenic forms for external application in the genital region, for prophylaxis and/or therapy of sexual disorders in men or women and/or for increase of sexual sensitivity.
摘要翻译： 本发明涉及由用于局部应用的脂质体中包含的活性成分制成的药物组合物，其中所述脂质体在其内部具有水性介质并且含有其中的至少一种活性成分，其对平滑肌肉组织施加直接或间接的缓解作用， 优选选自前列腺素，腺苷酸环化酶，cAMP，AMP，ATP，NO-合成酶，一氧化氮（NO），NO化合物，硝酸盐，鸟苷酸环化酶，cGMP，GMP，GTP和磷酸二酯酶，特别是西地那非。 本发明进一步涉及用于生产所述组合物的方法，任选地以无菌形式，以及使用支持活性成分的各种盖仑样形式的外源性生物区域用于预防和/或治疗性障碍的用途 男性或女性和/或增加性敏感性。
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3.发明授权Liposomal composition comprising an active ingredient for relaxing smooth muscle, the production of this composition and the therapeutic use thereof 有权包含用于松弛平滑肌的活性成分的脂质体组合物，该组合物的制备及其治疗用途公开(公告)号：US08524274B2
公开(公告)日：2013-09-03
申请号：US11577488
申请日：2005-10-14
CPC分类号： A61K9/127 , A61K9/0034 , A61K9/06 , A61K9/1277 , A61K9/1278
摘要： The invention relates to a pharmaceutical composition made from an active ingredient included in liposomes for topical application, whereby the liposomes have an aqueous medium in the interior thereof and contain at least one active ingredient therein which exerts a direct or indirect relaxing effect on smooth musculature and is preferably selected from the group of prostaglandins, adenylate cyclases, cAMP, AMP, ATP, NO-synthetases, nitrogen monoxide (NO), NO compounds, nitrates, guanylate cyclases, cGMP, GMP, GTP and phosphodiesterases, in particular, Sildenafil. The invention further relates to a method for production of said composition, optionally, in sterile form and the use of the liposomes supporting the active ingredient in various galenic forms for external application in the genital region, for prophylaxis and/or therapy of sexual disorders in men or women and/or for increase of sexual sensitivity.
摘要翻译： 本发明涉及由用于局部应用的脂质体中包含的活性成分制成的药物组合物，其中所述脂质体在其内部具有水性介质并且含有其中的至少一种活性成分，其对平滑肌肉组织施加直接或间接的缓解作用， 优选选自前列腺素，腺苷酸环化酶，cAMP，AMP，ATP，NO-合成酶，一氧化氮（NO），NO化合物，硝酸盐，鸟苷酸环化酶，cGMP，GMP，GTP和磷酸二酯酶，特别是西地那非。 本发明进一步涉及用于生产所述组合物的方法，任选地以无菌形式，以及使用支持活性成分的各种盖仑样形式的外源性生物区域用于预防和/或治疗性障碍的用途 男性或女性和/或增加性敏感性。
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公开(公告)号：US06843942B2
公开(公告)日：2005-01-18
申请号：US10415414
申请日：2001-10-31
CPC分类号： A61K9/1277 , B01J13/02 , Y10T428/2984
摘要： The invention relates to a device for producing lipid vesicles, which is equipped with a line (1) for transporting a polar liquid phase, with a line (2) for transporting an organic liquid phase containing lipids, with a collecting receptacle (7) for accommodating produced lipid vesicles, and with means for conveying the liquid phases through lines (1) and (2). At at least one location, the outer side of line (1) forms a common contact surface with line (2) inside of which a common opening (3) is provided that permits the flow of liquid and joins the inside of line (2) to the inside of line (1). Lines (1) and (2) do not contain agitating or dispersing aids in the area of the opening (3). The invention also relates to a method for the careful production of lipid vesicles, wherein the lipid phase is sprayed under pressure perpendicular to the direction of flow of the polar phase and into the same, whereupon lipid vesicles having a narrow size distribution form spontaneously and without the action of mechanical agitating or dispersing aids.
摘要翻译： 本发明涉及一种用于生产脂质囊泡的装置，其装备有用于输送极性液相的管线（1）和用于输送含有脂质的有机液相的管线（2），其中收集容器（7）用于 容纳产生的脂质囊泡，以及用于通过管线（1）和（2）输送液相的装置。 在至少一个位置处，管线（1）的外侧与管线（2）形成共同的接触表面，内部具有允许液体流动并连接管线（2）内部的公共开口（3） 到线（1）的内部。 线（1）和（2）在开口（3）的区域不包含搅拌或分散助剂。 本发明还涉及一种仔细生产脂质囊泡的方法，其中脂质相在垂直于极性相流动方向的压力下喷雾并进入脂质囊泡，由此自发地形成具有窄尺寸分布的脂质囊泡 机械搅拌或分散助剂的作用。
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5.发明授权Liposomal recombinant human superoxide-dismutase for the treatment of peyronie's disease 有权脂质体重组人超氧化物歧化酶用于治疗白喉病公开(公告)号：US06312720B1
公开(公告)日：2001-11-06
申请号：US09327174
申请日：1999-06-07
IPC分类号： A61K9133
CPC分类号： A61K9/0019 , A23L5/25 , A61K8/14 , A61K8/66 , A61K9/0014 , A61K9/127 , A61K38/446 , A61K47/36 , A61K2800/52 , A61Q17/00 , A61Q19/00 , A61Q19/004
摘要： Superoxide dismutase (SOD), preferably rhSOD, is used in liposomes, optionally mixed with hyaluronic acid and/or at least one physiologically acceptable carrier, and other optional additives, to prepare a pharmaceutical composition useful against increased concentrations of superoxide radicals and/or the damage caused thereby. The compositions are administered topically, preferably as gels or ointments, to prevent and/or heal human fibrotic tissue degeneration diseases, in particular induratio penis plastica (Peyronie's Disease).
摘要翻译： 超氧化物歧化酶（SOD），优选rhSOD，用于脂质体，任选地与透明质酸和/或至少一种生理学上可接受的载体和其它任选的添加剂混合，以制备可用于增加浓度超氧自由基和/或 造成的损害。 组合物局部给药，优选用凝胶或软膏，以预防和/或愈合人纤维化组织变性疾病，特别是阴茎勃氏塑型（Peyronie's disease）。
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公开(公告)号：US5942245A
公开(公告)日：1999-08-24
申请号：US836185
申请日：1997-05-05
IPC分类号： A23L5/20 , A61K8/14 , A61K8/66 , A61K9/00 , A61K9/127 , A61K9/133 , A61K38/44 , A61K47/36 , A61Q17/00 , A61Q19/00 , C12N9/02
CPC分类号： A61K9/0019 , A23L5/25 , A61K38/446 , A61K8/14 , A61K8/66 , A61K9/0014 , A61K9/127 , A61Q19/00 , A61K2800/52 , A61K47/36 , A61Q17/00 , A61Q19/004
摘要： Superoxide dismutase (SOD), preferably rhSOD, is used in liposomes, optionally mixed with hyaluronic acid and/or at least one physiologically acceptable carrier, and other optional additives, to prepare a pharmaceutical composition useful against increased concentrations of superoxide radicals and/or the damage caused thereby. These compositions can be administered topically, orally and/or parenterally to prevent and/or heal burns, skin lesions due to radiation, inflammations, rheumatic and arthritic diseases, bronchitis, ARDS, emphysema, allergic oedemas and other inflammatory process, possibly trigged by microbial infections. They may also be used in the cosmetic treatment of furuncles, acne and the like. They may also be used to improve the preservability of organic, preferably biogenic, materials, in particular organ transplants and liquids with organic components, as well as foodstuffs.
摘要翻译： PCT No.PCT / EP95 / 04352 Sec。 371日期1997年7月1日 102（e）日期1997年7月1日PCT提交1995年11月6日PCT公布。 WO96 / 14083 PCT出版物 日期1996年5月17日超氧化物歧化酶（SOD），优选rhSOD，用于脂质体，任选地与透明质酸和/或至少一种生理学上可接受的载体和其它任选的添加剂混合，以制备可用于增加超氧化物自由基浓度的药物组合物 和/或由此造成的损害。 这些组合物可以局部，口服和/或肠胃外给药以预防和/或愈合灼伤，由辐射引起的皮肤损伤，炎症，风湿性关节炎疾病，支气管炎，ARDS，肺气肿，过敏性水肿和其他可能由微生物触发的炎性过程 感染。 它们也可用于治疗fur，痤疮等的美容治疗。 它们也可用于改善有机，优选生物源的材料，特别是具有有机组分的器官移植物和液体以及食品的保存性。
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7.发明申请公开(公告)号：US20080031935A1
公开(公告)日：2008-02-07
申请号：US11578191
申请日：2005-04-21
申请人： Angelika Bodenteich , Josef Bockmann , Werner Frantsits , Eberhard Pirich , Andreas Wagner , Karola Vorauer-Uhl
发明人： Angelika Bodenteich , Josef Bockmann , Werner Frantsits , Eberhard Pirich , Andreas Wagner , Karola Vorauer-Uhl
IPC分类号： A61K9/127 , A61K31/27 , A61K31/407 , A61K31/435 , A61P25/00 , A61K31/4353 , A61K31/55 , A61K31/661
CPC分类号： A61K9/127
摘要： The invention relates to a pharmaceutical composition based on an active ingredient that is enclosed in liposomes for topical, transdermal application. The interior of said liposomes comprises an acidic, aqueous medium containing at least one cholinesterase inhibitor, preferably from the group containing donepezil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phenserine, tolserine, cymserine, thiatolserine, thiacymserine, neostigmine, huperzine, tacrine, metrifonate and dichlorvos, or an enantiomer or derivative of at least one of said compounds. In addition, the invention relates to a method for producing said composition, optionally in a sterile form and also to the use of the liposomes charged with the active ingredient in various galenic formulations for topical, transdermal application with a depot effect in the epidermis, for the prophylaxis and/or treatment of cutaneous neuropathic pain or the loss of cutaneous sensory function as a result of neuropathy.
摘要翻译： 本发明涉及一种基于活性成分的药物组合物，其被包封在用于局部，经皮施用的脂质体中。 所述脂质体的内部包含含有至少一种胆碱酯酶抑制剂的酸性水性培养基，优选来自含有多奈哌齐，利凡斯的明，加兰他敏，毒扁豆碱，庚基苯非司明，苯丝氨酸，丝氨酸，胞嘧磺酸，硫蛋白丝氨酸，硫柳汞，新斯的明，石杉碱，他克林， 和二氯葡聚糖，或至少一种所述化合物的对映异构体或衍生物。 此外，本发明涉及任选地以无菌形式生产所述组合物的方法，还涉及在各种盖仑制剂中装载活性成分的脂质体用于在表皮中具有贮库作用的局部，经皮施用的用途， 预防和/或治疗皮肤神经性疼痛或神经病变导致皮肤感觉功能丧失。
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