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    • 1. 发明申请
    • Platinum Aggregates and Process for Producing the Same
    • 白金聚集体及其生产方法
    • US20080187578A1
    • 2008-08-07
    • US12027752
    • 2008-02-07
    • Jin K. LeeBrian S. MillerFangjun WuLawrence T. BoniVladimir Malinin
    • Jin K. LeeBrian S. MillerFangjun WuLawrence T. BoniVladimir Malinin
    • A61K9/127A61K33/24A61K31/28
    • A61K9/127A61K9/0078A61K9/1277A61K31/28A61K33/24A61K47/544A61K47/554
    • One aspect of the disclosure relates to a new form of lipid-complexed active platinum compound, which allows for high concentrations of platinum compound in the composition. For example, the concentration of cisplatin in the composition is higher at room temperature, e.g., about greater than 1.2 mg/mL, compared to 1 mg/mL in aqueous solution. In one embodiment, the present invention is directed to a composition comprising a lipid-complexed active platinum compound, wherein the complex has a lipid to drug (L/D) ratio of less than about 1 by weight, e.g. about 0.10 to 1, wherein the lipid-complexed active platinum compound comprises at least one lipid and at least one active platinum compound. In other embodiments, wherein lipid-complexed active platinum compound has an average volume-weighted diameter of about 0.5 to about 20 microns. In still other embodiments, the composition further comprises a liposome. The liposome may comprise at least one lipid, and may further comprise at least one active platinum compound. The disclosure also relates to a pharmaceutical formulation comprising a lipid complexed active platinum compound and a pharmaceutically acceptable carrier or diluent. The pharmaceutical formulation may be formulated for inhalation or injection.
    • 本公开的一个方面涉及脂质复合的活性铂化合物的新形式,其允许组合物中高浓度的铂化合物。 例如,与1mg / mL的水溶液相比,组合物中顺铂的浓度在室温较高,例如大于1.2mg / mL。 在一个实施方案中,本发明涉及包含脂质复合的活性铂化合物的组合物,其中所述复合物具有小于约1重量比的脂质与药物(L / D)比例,例如。 约0.10至1,其中所述脂质复合的活性铂化合物包含至少一种脂质和至少一种活性铂化合物。 在其它实施方案中,其中脂质配合的活性铂化合物的平均体积加权直径为约0.5至约20微米。 在其它实施方案中,组合物还包含脂质体。 脂质体可以包含至少一种脂质,并且还可以包含至少一种活性铂化合物。 本公开还涉及包含脂质复合的活性铂化合物和药学上可接受的载体或稀释剂的药物制剂。 药物制剂可以配制用于吸入或注射。
    • 2. 发明授权
    • Platinum aggregates and process for producing the same
    • 铂集合体及其生产方法
    • US09186322B2
    • 2015-11-17
    • US12027752
    • 2008-02-07
    • Jin K. LeeBrian S. MillerFangjun WuLawrence T. BoniVladimir Malinin
    • Jin K. LeeBrian S. MillerFangjun WuLawrence T. BoniVladimir Malinin
    • A61K9/127A61K9/00A61K31/28A61K33/24A61K47/48
    • A61K9/127A61K9/0078A61K9/1277A61K31/28A61K33/24A61K47/544A61K47/554
    • One aspect of the disclosure relates to a new form of lipid-complexed active platinum compound, which allows for high concentrations of platinum compound in the composition. For example, the concentration of cisplatin in the composition is higher at room temperature, e.g., about greater than 1.2 mg/mL, compared to 1 mg/mL in aqueous solution. In one embodiment, the present invention is directed to a composition comprising a lipid-complexed active platinum compound, wherein the complex has a lipid to drug (L/D) ratio of less than about 1 by weight, e.g. about 0.10 to 1, wherein the lipid-complexed active platinum compound comprises at least one lipid and at least one active platinum compound. In other embodiments, wherein lipid-complexed active platinum compound has an average volume-weighted diameter of about 0.5 to about 20 microns. In still other embodiments, the composition further comprises a liposome. The liposome may comprise at least one lipid, and may further comprise at least one active platinum compound. The disclosure also relates to a pharmaceutical formulation comprising a lipid complexed active platinum compound and a pharmaceutically acceptable carrier or diluent. The pharmaceutical formulation may be formulated for inhalation or injection.
    • 本公开的一个方面涉及脂质复合的活性铂化合物的新形式,其允许组合物中高浓度的铂化合物。 例如,与1mg / mL的水溶液相比,组合物中顺铂的浓度在室温较高,例如大于1.2mg / mL。 在一个实施方案中,本发明涉及包含脂质复合的活性铂化合物的组合物,其中所述复合物具有小于约1重量比的脂质与药物(L / D)比例,例如。 约0.10至1,其中所述脂质复合的活性铂化合物包含至少一种脂质和至少一种活性铂化合物。 在其它实施方案中,其中脂质配合的活性铂化合物的平均体积加权直径为约0.5至约20微米。 在其它实施方案中,组合物还包含脂质体。 脂质体可以包含至少一种脂质,并且还可以包含至少一种活性铂化合物。 本公开还涉及包含脂质复合的活性铂化合物和药学上可接受的载体或稀释剂的药物制剂。 药物制剂可以配制用于吸入或注射。
    • 6. 发明授权
    • Sustained release of antiinfectives
    • 持续释放抗感染药
    • US07718189B2
    • 2010-05-18
    • US11185448
    • 2005-07-19
    • Lawrence T. BoniBrian S. MillerVladimir MalininXingong Li
    • Lawrence T. BoniBrian S. MillerVladimir MalininXingong Li
    • A61K9/127
    • A61K47/28A61K9/0078A61K9/127A61K9/1277A61K31/407A61K31/4709A61K31/496A61K31/545A61K31/7036A61K31/704A61K45/06Y02A50/473
    • Provided are lipid antiinfective formulations substantially free of anionic lipids with a lipid to antiinfective ratio is about 1:1 to about 4:1, and a mean average diameter of less than about 1 μm. Also provided is a method of preparing a lipid antiinfective formulation comprising an infusion process. Also provided are lipid antiinfective formulations wherein the lipid to drug ratio is about 1:1 or less, about 0.75:1 or less, or about 0.50:1 or less prepared by an in line fusion process. The present invention also relates to a method of treating a patient with a pulmonary infection comprising administering to the patient a therapeutically effective amount of a lipid antiinfective formulation of the present invention. The present invention also relates to a method of treating a patient for cystic fibrosis comprising administering to the patient a therapeutically effective amount of a lipid antiinfective formulation of the present invention.
    • 提供基本上不含阴离子脂质的脂质抗感染制剂,其脂质与抗感染比为约1:1至约4:1,平均平均直径小于约1μm。 还提供了制备包含输注方法的脂质抗感染制剂的方法。 还提供了脂质抗感染制剂,其中通过在线融合方法制备的脂质与药物的比例为约1:1或更低,约0.75:1或更低,或约0.50:1或更低。 本发明还涉及治疗患有肺部感染的患者的方法,其包括向患者施用治疗有效量的本发明的抗脂质抗感染药物。 本发明还涉及一种治疗患者囊性纤维化的方法,其包括向患者施用治疗有效量的本发明的抗脂质抗感染制剂。