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公开(公告)号：US06770290B1
公开(公告)日：2004-08-03
申请号：US07600154
申请日：1990-10-19
IPC分类号： A61K9127
CPC分类号： A61K9/1277 , A61K31/7048 , A61K47/544 , B82Y5/00
摘要： A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble complex is hydrated, the final pH of the hydrating aqueous buffer is carefully controlled. The Amphotericin B liposomes formed have markedly reduced toxicity.
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公开(公告)号：US5965156A
公开(公告)日：1999-10-12
申请号：US469251
申请日：1995-06-06
IPC分类号： A61K47/14 , A61K9/10 , A61K9/127 , A61K31/00 , A61K31/685 , A61K31/70 , A61K47/00 , A61P31/00 , A61P31/04 , C07H1/00
CPC分类号： A61K9/1277 , A61K31/7048 , A61K47/48053 , B82Y5/00
摘要： A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble complex is hydrated, the final pH of the hydrating aqueous buffer is carefully controlled. The Amphotericin B liposomes formed have markedly reduced toxicity.
摘要翻译： 公开了一种用于将二亲性药物溶解在少量有机溶剂中用于改进的脂质体的新型组合物和方法。 磷脂酰甘油在少量有机溶剂中酸化。 然后将悬浮在有机溶剂中的两亲性药物如两性霉素B加入酸化的磷脂酰甘油中，并在磷脂酰甘油和两亲性药物之间形成可溶性复合物。 当掺入可溶性复合物的脂质体组合物水合时，仔细控制水合水性缓冲液的最终pH。 形成的两性霉素B脂质体毒性明显降低。
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3.发明授权Liposomal cyclosporin formulations as agents for immunosuppression and multiple drug resistant indications 失效脂质体环孢菌素制剂作为免疫抑制剂和多种耐药性适应症
公开(公告)号：US5656287A
公开(公告)日：1997-08-12
申请号：US472635
申请日：1995-06-07
申请人： Jill Adler-Moore , Su-Ming Chiang
发明人： Jill Adler-Moore , Su-Ming Chiang
摘要： An improved liposomal cyclosporin therapeutic formulation, comprising phosphatidylcholine, cholesterol, dimyristoylphosphatidylglycerol and a cyclosporin in a mole ratios of about 21:0.5:3:1 to 21:1.5:3:1 and 24:0.5:3:1 to about 24:1.5:3:1. The formulations are useful as immunosuppressive agents and enhancers of antineoplastic agents in drug resistant cancer cells.
摘要翻译： 一种改进的脂质体环孢菌素治疗制剂，其包含摩尔比为约21:0.5:3:1至21:1.5:3:1和24:0.5:3:1至约24:1.5的磷脂酰胆碱，胆固醇，二肉豆蔻酰磷脂酰甘油和环孢菌素 ：3：1。 该制剂作为药物抗性癌细胞中抗肿瘤剂的免疫抑制剂和增强剂是有用的。
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公开(公告)号：US5756120A
公开(公告)日：1998-05-26
申请号：US468497
申请日：1995-06-06
CPC分类号： A61K31/7036 , A61K9/127
摘要： A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided where the hydration temperature is significantly below the transition temperature of the formulation. A method for the treatment of drug susceptible and drug resistant bacteria.
摘要翻译： 包含中性脂质，带负电荷的脂质和固醇的脂质体氨基糖苷制剂。 该制剂含有平均粒度低于100nm的单层囊泡。 提供了含有氨基糖苷类的脂质体的方法，其中水合温度明显低于制剂的转变温度。 一种治疗药物易感和耐药细菌的方法。
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公开(公告)号：US5958449A
公开(公告)日：1999-09-28
申请号：US82633
申请日：1998-05-21
CPC分类号： A61K31/7036 , A61K9/127 , A61K9/1272
摘要： A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipid and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided. A method is also provide for the treatment of drug susceptible and drug resistant bacteria.
摘要翻译： 包含中性脂质，带负电荷的脂质和甾醇的脂质体氨基糖苷制剂。 该制剂含有平均粒度低于100nm的单层囊泡。 提供了制备含有氨基糖苷类的脂质体的方法。 还提供了用于治疗药物易感和耐药细菌的方法。
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公开(公告)号：US06221388B1
公开(公告)日：2001-04-24
申请号：US09407798
申请日：1999-09-28
IPC分类号： A61K9127
CPC分类号： A61K31/7036 , A61K9/127 , A61K9/1272
摘要： A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is also provided. A method is also provided for the treatment of drug susceptible and drug resistant bacteria.
摘要翻译： 包含中性脂质，带负电荷的脂质和固醇的脂质体氨基糖苷制剂。 该制剂含有平均粒度低于100nm的单层囊泡。 还提供了制备含有氨基糖苷类的脂质体的方法。 还提供了用于治疗药物易感和耐药细菌的方法。
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公开(公告)号：US5759571A
公开(公告)日：1998-06-02
申请号：US84218
申请日：1993-06-23
CPC分类号： A61K31/7036 , A61K9/127
摘要： A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided where the hydration temperature is significantly below the transition temperature of the formulation. A method for the treatment of drug susceptible and drug resistant bacteria.
摘要翻译： PCT No.PCT / US93 / 04501 Sec。 371日期：1993年6月23日 102（e）1993年6月23日日期PCT 1993年5月11日提交的脂质体氨基糖苷制剂，其包含中性脂质，带负电荷的脂质和固醇。 该制剂含有平均粒度低于100nm的单层囊泡。 提供了含有氨基糖苷类的脂质体的方法，其中水合温度明显低于制剂的转变温度。 一种治疗药物易感和耐药细菌的方法。
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公开(公告)号：US06740335B1
公开(公告)日：2004-05-25
申请号：US09486309
申请日：2000-02-24
IPC分类号： A61K9127
CPC分类号： A61K31/4745 , A61K9/127 , A61K9/1278 , A61K31/496
摘要： Liposomal encapsulated camptothecin formulations are provided. The liposomes have improved pharmacokinetics, enhanced efficacy as anti-tumor agents and provide an increased therapeutic index as compared to the free drug and topotecan. The formulations include liposomes comprising at least one phospholipid and a camptothecin or analog thereof.
摘要翻译： 提供了脂质体包封的喜树碱制剂。 与游离药物和拓扑替康相比，脂质体具有改善的药代动力学，增强作为抗肿瘤剂的功效并提供增加的治疗指数。 制剂包括包含至少一种磷脂和喜树碱或其类似物的脂质体。
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公开(公告)号：US20050238705A1
公开(公告)日：2005-10-27
申请号：US11035755
申请日：2005-01-14
申请人： Ning Hu , Gerard Jensen , Stephanie Yang , Su-Ming Chiang
发明人： Ning Hu , Gerard Jensen , Stephanie Yang , Su-Ming Chiang
CPC分类号： A61K9/127 , A61K9/0019
摘要： The invention provides lipid-based dispersion comprising comprising, a) phosphatidyl choline; b) an anionic phospholipid; optionally c) up to 1% cholesterol by weight of total lipids; and optionally d) a therapeutic agent; wherein the mean particle size measured by dynamic light scattering is less than 100 nm. The invention also provides pharmaceutical compositions comprising such a dispersion as well as methods of producing a therapeutic effect in a mammal comprising administering an effective amount of such a dispersion.
摘要翻译： 本发明提供基于脂质的分散体，其包含：a）磷脂酰胆碱; b）阴离子磷脂; 任选地c）总脂质重量高达1％的胆固醇; 和任选地d）治疗剂; 其中通过动态光散射测量的平均粒度小于100nm。 本发明还提供包含这种分散体的药物组合物以及在哺乳动物中产生治疗效果的方法，包括施用有效量的这种分散体。
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公开(公告)号：US5683714A
公开(公告)日：1997-11-04
申请号：US417487
申请日：1995-04-05
摘要： An improved liposomal cyclosporin therapeutic formulation, comprising phosphatidylcholine, phosphatidylglycerol and a cyclosporin in a mole ratio of from 25:3:1 to 17:3:1 is described. The formulation includes unilamellar vesicles having reduced toxicity. The formulation is used as an immunosuppressive agent and is an enhancer of the efficacy of antineoplasties for drug resistant cancer cells. A method is also provided for inhibiting the growth of cancer cells.
摘要翻译： 描述了一种改进的脂质体环孢菌素治疗制剂，其包含摩尔比为25:3:1至17:3:1的磷脂酰胆碱，磷脂酰甘油和环孢菌素。 该制剂包括具有降低的毒性的单层囊泡。 该制剂用作免疫抑制剂，并且是用于抗药性癌细胞的抗肿瘤功效的增强剂。 还提供了抑制癌细胞生长的方法。
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