Amphotericin B liposome preparation

    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

    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.

    Amphotericin B liposome preparation
    2.
    发明授权
    Amphotericin B liposome preparation 失效
    两性霉素B脂质体制剂

    公开(公告)号:US5965156A

    公开(公告)日:1999-10-12

    申请号:US469251

    申请日:1995-06-06

    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。

    Treatment of systemic fungal infections with phospholipid particles
encapsulating polyene antibiotics
    3.
    发明授权
    Treatment of systemic fungal infections with phospholipid particles encapsulating polyene antibiotics 失效
    用包封多烯抗生素的磷脂颗粒治疗全身真菌感染

    公开(公告)号:US5874104A

    公开(公告)日:1999-02-23

    申请号:US467864

    申请日:1995-06-06

    摘要: Formulations consisting of phospholipid small unilamellar particles encapsulating polyene antifungal antibiotics and methods for using such compositions to treat systemic fungal infections are described. In a preferred embodiment, the particles are in the form of vesicles which comprise a polyene antifungal antibiotic, preferably amphotericin B and/or nystatin, egg phosphatidylcholine and cholesterol, preferably in the molar ratio of about 0.2 (AMB):2(PL):1(CHOL). These vesicles may also have an amine modified surface. The vesicles are suspended in a low isonic strength saccharide/tris solution at a pH of from about 6.0 to about 8.0 and may be administered to deliver the antifungal antibiotic to treat systemic fungal infections.

    摘要翻译: 描述由包含多烯抗真菌抗生素的磷脂小单层颗粒组成的制剂以及使用这些组合物治疗全身性真菌感染的方法。 在优选的实施方案中,颗粒是囊泡形式,其包含多烯抗真菌抗生素,优选两性霉素B和/或制霉菌素,卵磷脂酰胆碱和胆固醇,优选摩尔比为约0.2(AMB):2(PL): 1(CHOL)。 这些囊泡也可以具有胺改性的表面。 将囊泡悬浮在pH为约6.0至约8.0的低等强度糖/ tris溶液中,并且可以施用以输送抗真菌抗生素以治疗全身性真菌感染。

    Preparation small unilamellar vesicles including polyene antifungal
antibiotics
    4.
    发明授权
    Preparation small unilamellar vesicles including polyene antifungal antibiotics 失效
    制备小单层囊泡,包括多烯抗真菌抗生素

    公开(公告)号:US5043107A

    公开(公告)日:1991-08-27

    申请号:US427732

    申请日:1989-10-27

    IPC分类号: A61K9/127 A61K9/133

    摘要: Formulations consisting of phospholipid small unilamellar particles encapsulating polyene antifungal antibiotics and methods for using such compositions to treat systemic fungal infections are described. In a preferred embodiment, the particles are in the form of vesicles which comprise a polyene antifungal antibiotic, preferably amphotericin B and/or nystatin, egg phosphatidylcholine and cholesterol, preferably in the molar ratio of about 0.2 (AMB):2(PL):1(CHOL). These vesicles may also have an amine modified surface. The vesicles are suspended in a low ionic strength saccharide/tris solution at a pH of from about 6.0 to about 8.0 and may be administered to deliver the anti-fungal antibiotic to treat systemic fungal infections.

    摘要翻译: 描述由包含多烯抗真菌抗生素的磷脂小单层颗粒组成的制剂以及使用这些组合物治疗全身性真菌感染的方法。 在优选的实施方案中,颗粒是囊泡形式,其包含多烯抗真菌抗生素,优选两性霉素B和/或制霉菌素,卵磷脂酰胆碱和胆固醇,优选摩尔比为约0.2(AMB):2(PL): 1(CHOL)。 这些囊泡也可以具有胺改性的表面。 将囊泡悬浮在约6.0至约8.0的pH下的低离子强度的糖/三溶液中,并且可以施用以递送抗真菌抗生素以治疗全身性真菌感染。

    Liposomal cyclosporin formulations as agents for immunosuppression and
multiple drug resistant indications
    5.
    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

    IPC分类号: A61K9/127 A61K38/13

    CPC分类号: A61K38/13 A61K9/127

    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。

    LIPOSOMAL FORMULATIONS
    6.
    发明申请
    LIPOSOMAL FORMULATIONS 审中-公开
    药物制剂

    公开(公告)号:US20140287022A1

    公开(公告)日:2014-09-25

    申请号:US14113707

    申请日:2012-04-25

    摘要: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise liposomes formed from dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol; and an antigenic polypeptide comprising a first polypeptide sequence, and a second polypeptide sequence heterologous the first polypeptide sequence which comprises a transmembrane sequence from a membrane protein, said transmembrane sequence having a number of residues sufficient to cross a lipid bilayer, at least nine contiguous residues of which are predicted to form an alpha helix having a hydrophobicity score of about 0.7 or greater.

    摘要翻译: 本发明涉及脂质体疫苗组合物,其制备方法及其用于刺激动物免疫应答的方法。 这些组合物包含由二肉豆蔻酰磷脂酰胆碱(“DMPC”)形成的脂质体; 二肉豆蔻酰磷脂酰甘油(“DMPG”)或二肉豆蔻酰基三甲基铵丙烷(“DMTAP”)或DMPC和DMTAP两者; 和至少一种甾醇; 和包含第一多肽序列的抗原多肽和第二多肽序列,所述第一多肽序列包含来自膜蛋白的跨膜序列,所述跨膜序列具有足以穿过脂质双层的残基数,至少9个连续残基 预测其形成疏水性评分为约0.7或更高的α螺旋。