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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。
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公开(公告)号：US5766624A
公开(公告)日：1998-06-16
申请号：US449598
申请日：1995-05-24
申请人： Andrew S. Janoff , Walter Perkins , Imran Ahmad
发明人： Andrew S. Janoff , Walter Perkins , Imran Ahmad
摘要： Defensins are microbicidal, tumoricidal cytotoxic protein components of animal host defense systems. They can be entrapped in liposomes containing release-inhibiting lipid such that the defensins are neutralized, and their release from the liposomes is inhibited; however, the defensins remain effective when exposed to endocytosed material in endocytic vesicles. Liposomal defensin formulations are administered to animals for the treatment or prevention of microbial infections, for the treatment of cancers and for the treatment of disorders characterized by a deficiency of protein-mediated cytotoxic activity in cytoplasmic granules.
摘要翻译： 防卫素是动物宿主防御系统的杀菌，杀肿瘤细胞毒性蛋白质成分。 它们可以被包裹在含有释放抑制脂质的脂质体中，使得防御素被中和，并且它们从脂质体的释放被抑制; 然而，防御素在暴露于内吞囊泡中的内吞物质时仍然有效。 向动物施用脂质体防御素制剂用于治疗或预防微生物感染，用于治疗癌症和用于治疗以细胞质颗粒中蛋白质介导的细胞毒活性缺乏为特征的病症。
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公开(公告)号：US5415867A
公开(公告)日：1995-05-16
申请号：US105764
申请日：1993-08-11
申请人： Sharma R. Minchey , Christine E. Swenson , Andrew S. Janoff , Lawrence Boni , Kathy A. Stewart , Walter Perkins
发明人： Sharma R. Minchey , Christine E. Swenson , Andrew S. Janoff , Lawrence Boni , Kathy A. Stewart , Walter Perkins
IPC分类号： A61K9/127 , A61K31/545 , A61K49/04
CPC分类号： A61K49/0466 , A61K31/545 , A61K47/48053 , A61K9/127
摘要： High ratio active agent:lipid complexes, their preparation and use are disclosed. Particular reference is made to cephalosporin:lipid complex and iodinated contrast agent:lipid complex. Use of high ratio cephalosporin:lipid complex in bacterial prophylaxis, and particularly bacteremia prophylaxis, including a method of preventing bacterial infection in an animal over an extended period comprising the step of administering to said animal a high ratio cephalosporin:lipid complex is further disclosed as is the use of high ratio iodinated contrast agent:lipid complex in X-ray applications.
摘要翻译： 高比例的活性剂：脂质复合物，其制备和用途被公开。 特别提到头孢菌素：脂质复合物和碘化造影剂：脂质复合物。 在细菌预防中使用高比例头孢菌素：脂质复合物，特别是菌血症预防，包括在长时间内预防动物细菌感染的方法，包括向所述动物施用高比例头孢菌素：脂质复合物的步骤进一步公开为 是使用高比例碘化造影剂：X射线应用中的脂质复合物。
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公开(公告)号：US5154930A
公开(公告)日：1992-10-13
申请号：US160141
申请日：1988-02-25
申请人： Mircea C. Popescu , Paul A. Tremblay , Andrew S. Janoff , Marc J. Ostro , Elaine Chan , Alan Weiner
发明人： Mircea C. Popescu , Paul A. Tremblay , Andrew S. Janoff , Marc J. Ostro , Elaine Chan , Alan Weiner
CPC分类号： B82Y5/00 , A61K47/10 , A61K47/24 , A61K9/0019 , A61K9/1277 , A61K9/4858 , Y10S436/829 , Y10S514/885 , Y10S514/937 , Y10T428/2984
摘要： A pharmacological agent-lipid solution preparation comprising a lipophilic pharmacological agent, a desalted charged lipid and an aqueous-miscible lipid solvent such that upon introduction into an aqueous medium a suspension of lipid aggregates associated with the pharmacological agent are formed, and methods of manufacture and use.
摘要翻译： 一种药理学试剂 - 脂溶液制剂，其包含亲脂性药理学试剂，脱盐的带电脂质和水溶性脂溶性溶剂，使得在引入水性介质中形成与药理学试剂相关的脂质聚集体的悬浮液时， 使用。
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公开(公告)号：US4891208A
公开(公告)日：1990-01-02
申请号：US773429
申请日：1985-09-10
申请人： Andrew S. Janoff , Mircea C. Popescu , Alan L. Weiner , Lois E. Bolscak , Paul A. Tremblay , Christine E. Swenson
发明人： Andrew S. Janoff , Mircea C. Popescu , Alan L. Weiner , Lois E. Bolscak , Paul A. Tremblay , Christine E. Swenson
IPC分类号： A61K38/00 , A23K20060101 , A23K1/00 , A61K20060101 , A61K9/00 , A61K9/02 , A61K9/06 , A61K9/10 , A61K9/107 , A61K9/127 , A61K9/52 , A61K31/00 , A61K31/415 , A61K38/22 , A61K39/00 , A61K39/395 , A61K47/00 , A61K47/28 , A61K49/00 , A61K51/00 , A61P31/04 , B01J20060101 , B01J13/00 , B01J13/02
CPC分类号： A61K9/1271 , A61K9/1272 , A61K2039/55555 , Y10S436/829 , Y10S514/885 , Y10S514/887 , Y10S514/967 , Y10T428/2984
摘要： Steroidal liposomes comprising a bioactive agent and method for their administration are disclosed, the bilayers of said steroidal liposomes comprising a salt form of a carboxylic acid derivative of a sterol, a salt form of a polycarboxylic acid derivative of a sterol, a salt form of a hydroxy carboxylic acid derivative of a sterol, a salt form of an amino acid derivative of a sterol or a salt form of a poly (amino acid) derivative of a sterol; or a salt form of an organic acid derivative of cholesterol, a vitamin D, a phytosterol, or a steroidal hormone.
摘要翻译： 公开了包含生物活性剂和其给药方法的类固醇脂质体，所述甾族脂质体的双层包含固醇的羧酸衍生物的盐形式，固醇的多元羧酸衍生物的盐形式， 固醇的羟基羧酸衍生物，固醇的氨基酸衍生物的盐形式或固醇的聚（氨基酸）衍生物的盐形式; 或胆固醇，维生素D，植物甾醇或类固醇激素的有机酸衍生物的盐形式。
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公开(公告)号：US4666831A
公开(公告)日：1987-05-19
申请号：US702555
申请日：1985-02-19
IPC分类号： G01N33/86 , G01N33/92 , G01N33/53 , G01N33/571
CPC分类号： G01N33/92 , G01N33/86 , G01N2405/04 , Y10S436/811 , Y10S436/825 , Y10T436/25125
摘要： Improved lipid-dependent diagnostic assays are provided wherein the test sample to be assayed is pre-incubated with one or more phospholipids having a hexagonal (H.sub.II) organization or with lipidic particles. The pre-incubation results in reduced false positives due to anti-phospholipid antibodies, such as, lupus anticoagulants, which may be present in the test sample, without changing the overall character, including the normal baseline, of the assay. Suprisingly, in accordance with the invention, it has been found that only hexagonal phospholipids and lipidic particles can be used, and, in particular, lamellar (bilayer) phospholipids cannot be used. An assay for diagnosing systemic lupus erythematosus (SLE) is also provided.
摘要翻译： 提供改进的脂质依赖性诊断测定法，其中待测试的测试样品与一种或多种具有六方（HII）组织或脂质颗粒的磷脂预孵育。 预孵育导致由于抗磷脂抗体（例如可能存在于测试样品中的狼疮抗凝剂）而导致的假阳性减少，而不改变测定的总体特征，包括正常基线。 令人惊奇的是，根据本发明，已经发现只能使用六方磷脂和脂质颗粒，特别是不能使用层状（双层）磷脂。 还提供了用于诊断系统性红斑狼疮（SLE）的测定法。
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公开(公告)号：US4522803A
公开(公告)日：1985-06-11
申请号：US476496
申请日：1983-03-24
CPC分类号： A61K9/127 , Y10S436/829 , Y10T428/2984
摘要： A new and substantially improved type of lipid vesicle, called stable plurilamellar vesicles (SPLVs), are described, as well as the process for making the same. SPLVs are stable during storage and can be used in vivo for the sustained release of compounds and in the treatment of disease.
摘要翻译： 描述了称为稳定的多层囊泡（SPLV）的新的和显着改进的脂质囊泡型，以及其制备方法。 SPLV在储存期间是稳定的，并且可以在体内用于化合物的持续释放和疾病的治疗。
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公开(公告)号：US5616334A
公开(公告)日：1997-04-01
申请号：US430699
申请日：1995-04-28
申请人： Andrew S. Janoff , Lawrence Boni , Thomas D. Madden , Pieter R. Cullis , Robert P. Lenk , John J. Kearns , Anthony G. Durning , Robert Klimchak , Joel Portnoff
发明人： Andrew S. Janoff , Lawrence Boni , Thomas D. Madden , Pieter R. Cullis , Robert P. Lenk , John J. Kearns , Anthony G. Durning , Robert Klimchak , Joel Portnoff
IPC分类号： A61K9/127 , A61K9/16 , A01N25/32 , A01N57/26 , A61K31/685
CPC分类号： A61K9/127 , A61K31/7048 , A61K47/48053 , A61K9/1277 , A61K9/1617 , G03B2227/325 , Y10T428/2984
摘要： Methods and compositions are described for nonliposomal lipid complexes in association with toxic hydrophobic drugs such as the polyene antibiotic amphotericin B. Lipid compositions are preferably a combination of the phospholipids dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidylglycerol (DMPG) in about a 7:3 mole ratio. The lipid complexes contain a bioactive agent, and may be made by a number of procedures, at high drug:lipid ratios. These compositions of high drug:lipid complexes (HDLCs) may be administered to mammals such as humans for the treatment of infections, with substantially equivalent or greater efficacy and reduced drug toxicities as compared to the drugs in their free form. Also disclosed is a novel liposome-loading procedure, which may also be used in the formation of the HDLCs.
摘要翻译： 描述了与毒性疏水性药物如多烯抗生素两性霉素B相关的非脂质体脂质复合物的方法和组合物。脂质组合物优选以约7:3摩尔比组合磷脂二肉豆蔻酰磷脂酰胆碱（DMPC）和二肉豆蔻酰磷脂酰甘油（DMPG）。 脂质复合物含有生物活性剂，并且可以以高药物：脂质比例通过多种方法制备。 与其游离形式的药物相比，高药物：脂质复合物（HDLC）的这些组合物可以施用于哺乳动物例如人以治疗感染，具有基本相同或更大的功效和降低的药物毒性。 还公开了一种新的脂质体加载程序，其也可用于HDLC的形成。
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公开(公告)号：US5614214A
公开(公告)日：1997-03-25
申请号：US247053
申请日：1994-05-20
CPC分类号： A61K9/1271 , Y10T428/2984
摘要： Provided herein is a method of administering a liposome composition to an animal, the method involving adminstering to the animal a liposome composition containing an adverse physiological reaction-reducing effective amount of a liposome which has, in addition to a bioactive agent, a lipid bilayer containing a lipid and a surface agent-modified molecule. An adverse physiological reaction which may be experienced by the animal upon administration of a liposome composition is reduced by way of the presence of the surface agent-modified molecule in the liposome's lipid bilayer.
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20.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。
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