-
1.发明授权Liposomes comprising aminoglycoside phosphates and methods of production and use 失效包含氨基糖苷磷酸酯的脂质体及其生产和使用方法
公开(公告)号：US5409704A
公开(公告)日：1995-04-25
申请号：US59192
申请日：1993-05-06
IPC分类号： A61K9/127 , A61K47/48 , C07H15/226 , A61K9/133
CPC分类号： A61K31/70 , A61K9/127 , A61K9/1271 , A61K9/1277 , A61K9/1278 , C07H15/226 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10T428/2984
摘要： Aminoglycosides, analogs and derivatives thereof, in the form of phosphate salts are described as well as the process for making and utilizing same. Aminoglycoside phosphate liposomes and nonguanadino aminoglycoside phosphate liposomes, their preparation and use, are particularly described.
摘要翻译： 描述磷酸盐形式的氨基糖苷类，其类似物和衍生物以及其制备和利用方法。 氨基糖苷磷酸酯脂质体和非瓜氨酰氨基糖苷磷酸脂质体，其制备和用途，具体描述。
-
公开(公告)号：US4975282A
公开(公告)日：1990-12-04
申请号：US122613
申请日：1987-11-17
CPC分类号： A61K9/1278 , A61K9/1271 , A61K9/1277
摘要： A multilamellar vesicle dispersed in an aqueous phase comprising an aqueous medium, a lipid concentration of at least about 50 mg/ml and a trapping efficiency of at least about 40 percent. The vesicle can be prepared by dispersing the lipid in an aqueous phase to form a multilamellar vesicle, rapidly freezing the multilamellar vesicle to obtain a frozen lipid-aqueous medium mixture, and warming the mixture to obtain a frozen and thawed multilamellar vesicle dispersed in an aqueous phase.
摘要翻译： 分散在包含水性介质的水相中的多层囊泡，至少约50mg / ml的脂质浓度和至少约40％的捕获效率。 可以通过将脂质分散在水相中以形成多层囊泡，快速冷冻多层囊泡以获得冷冻的脂质 - 水性介质混合物，并加热混合物以获得分散在水溶液中的冷冻和解冻的多层囊泡， 相。
-
公开(公告)号：US5837279A
公开(公告)日：1998-11-17
申请号：US450831
申请日：1995-05-25
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译： 通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。 优选地，保护性糖存在于脂质体膜的内表面和外表面。 在脱水之前冻干脂质体制剂是任选的。 或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在 补液。 可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。
-
公开(公告)号：US5922350A
公开(公告)日：1999-07-13
申请号：US876938
申请日：1997-06-16
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译： 通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。 优选地，保护性糖存在于脂质体膜的内表面和外表面。 在脱水之前冻干脂质体制剂是任选的。 或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在 补液。 可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。
-
公开(公告)号：US5578320A
公开(公告)日：1996-11-26
申请号：US22819
申请日：1993-02-24
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译： 通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。 优选地，保护性糖存在于脂质体膜的内表面和外表面。 在脱水之前冻干脂质体制剂是任选的。 或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在 补液。 可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。
-
公开(公告)号：US4880635A
公开(公告)日：1989-11-14
申请号：US759419
申请日：1985-07-26
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译： 通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。 优选地，保护性糖存在于脂质体膜的内表面和外表面。 在脱水之前冻干脂质体制剂是任选的。 或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在 补液。 可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。
-
公开(公告)号：US5736155A
公开(公告)日：1998-04-07
申请号：US461212
申请日：1995-06-05
CPC分类号： A61K9/1278 , A61K9/1271 , A61K9/1277
摘要： Methods for encapsulating ionizable antineoplastic agents in liposomes using transmembrane potentials are provided. Trapping efficiencies approaching 100% and rapid loading are readily achieved. Dehydration protocols which allow liposomes to be conveniently used in the administration of antineoplastic agents in a clinical setting are also provided. In accordance with other aspects of the invention, transmembrane potentials are used to reduce the rate of release of ionizable drugs from liposomes.
摘要翻译： 提供了使用跨膜电位将可电离抗肿瘤剂包封在脂质体中的方法。 捕获效率接近100％，快速加载容易实现。 还提供允许脂质体在临床环境中方便地用于施用抗肿瘤剂的脱水方案。 根据本发明的其他方面，使用跨膜电位来降低可离子化药物从脂质体释放的速率。
-
8.发明授权Methods of treatment using high drug-lipid formulations of liposomal-antineoplastic agents 失效使用脂质体 - 抗肿瘤药物的高药物 - 脂质制剂的治疗方法
公开(公告)号：US5744158A
公开(公告)日：1998-04-28
申请号：US450830
申请日：1995-05-25
申请人： Lawrence D. Mayer , Marcel B. Bally , Pieter R. Cullis , Richard S. Ginsberg , George N. Mitilenes
发明人： Lawrence D. Mayer , Marcel B. Bally , Pieter R. Cullis , Richard S. Ginsberg , George N. Mitilenes
CPC分类号： A61K9/1278 , A61K9/127 , Y10S436/826 , Y10S436/829 , Y10S514/908 , Y10T428/2984
摘要： A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.
摘要翻译： 提供了在脂质体中包封抗肿瘤剂的方法，优选具有高的药物：脂质比。 脂质体可以通过使用跨膜离子梯度，优选跨膜pH梯度的活性机制加载药物的方法制备。 使用这种技术，捕获效率接近100％，脂质体可以在使用前立即加载药物，消除与脂质体中药物滞留有关的稳定性问题。 药物：使用的脂质比例比传统脂质体制剂高约3-80倍，并且药物从脂质体的释放速率降低。 还公开了一种在脂质体制剂中测定游离抗肿瘤剂的测定方法。
-
公开(公告)号：US5595756A
公开(公告)日：1997-01-21
申请号：US172140
申请日：1993-12-22
IPC分类号： A61K9/127
CPC分类号： A61K9/1272
摘要： Liposomal compositions encapsulating bioactive agents and having improved circulation longevity of the agents are disclosed. Such liposomes combine a low pH of the solution in which a bioactive agent is entrapped and a sugar-modified lipid or an amine-bearing lipid, the combination of which enhances the retention of the encapsulated bioactive agent and thereby promotes circulation longevity. The present invention also discloses methods of making and using such compositions.
摘要翻译： 公开了封装生物活性剂并具有改善的试剂的循环寿命的脂质体组合物。 这种脂质体结合生物活性剂被捕获的溶液的低pH值和糖修饰的脂质或含胺脂质，其组合增强了包封的生物活性剂的保留，从而促进循环寿命。 本发明还公开了制备和使用这些组合物的方法。
-
公开(公告)号：US6083530A
公开(公告)日：2000-07-04
申请号：US84526
申请日：1998-05-26
申请人： Lawrence D. Mayer , Marcel B. Bally , Pieter R. Cullis , Richard S. Ginsberg , George N. Mitilenes
发明人： Lawrence D. Mayer , Marcel B. Bally , Pieter R. Cullis , Richard S. Ginsberg , George N. Mitilenes
CPC分类号： A61K9/1278 , A61K9/127 , Y10S436/826 , Y10S436/829 , Y10S514/908 , Y10T428/2984
摘要： A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.
摘要翻译： 提供了在脂质体中包封抗肿瘤剂的方法，优选具有高的药物：脂质比。 脂质体可以通过使用跨膜离子梯度，优选跨膜pH梯度的活性机制加载药物的方法制备。 使用这种技术，捕获效率接近100％，脂质体可以在使用前立即加载药物，消除与脂质体中药物滞留有关的稳定性问题。 药物：使用的脂质比例比传统脂质体制剂高约3-80倍，并且药物从脂质体的释放速率降低。 还公开了一种在脂质体制剂中测定游离抗肿瘤剂的测定方法。
-
-
-
-
-
-
-
-
-
搜索结果
60 条记录 (耗时 0.032 秒)
