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    AZOLE PHARMACEUTICAL FORMULATIONS FOR PARENTERAL ADMINISTRATION AND METHODS FOR PREPARING AND USING THE SAME AS TREATMENT OF DISEASES SENSITIVE TO AZOLE COMPOUNDS
    1.
    发明申请
    AZOLE PHARMACEUTICAL FORMULATIONS FOR PARENTERAL ADMINISTRATION AND METHODS FOR PREPARING AND USING THE SAME AS TREATMENT OF DISEASES SENSITIVE TO AZOLE COMPOUNDS 审中-公开
    用于住院管理的AZOLE药物制剂及其制备和使用该方法用于治疗对AZOLE化合物敏感的疾病

    公开(公告)号：US20140031366A1

    公开(公告)日：2014-01-30

    申请号：US13994152

    申请日：2011-12-16

    申请人： Borje S. Andersson ,  Jeffrey Tarrand ,  Benigno C. Valdez

    发明人： Borje S. Andersson ,  Jeffrey Tarrand ,  Benigno C. Valdez

    IPC分类号： A61K31/496 ,  A61K9/00

    CPC分类号： A61K31/496 ,  A61K9/0019 ,  A61K9/0053 ,  A61K47/10

    摘要： A parenteral azole composition comprises a first solvent, made of benzyl alcohol and/or an acidified alcohol such as ethanol, and a lipophilic component such as PEG400, and the azole, or triazole, such as itraconazole or posaconazole dissolved in this first composite solvent vehicle that is essentially free of surfactants, particularly non-ionic surfactants, and has low levels of water, preferably less than 5% water. The composition may be further diluted with an infusion fluid, such as normal saline or 5% or 10% dextrose in water, before infusion into an immunocompromized mammal, preferably a human. The composition is useful for the treatment and suppression of infections caused by microbes such as yeast and molds that are sensitive to azoles, but it may be extended to dissolve other pharmaceutically active agents that can be used to treat other types of infectious diseases or other ailments, such as malignant and autoimmune diseases.

    摘要翻译： 肠胃外唑类组合物包含由苄醇和/或酸化醇如乙醇制成的第一溶剂和溶于该第一复合溶剂载体中的亲脂性组分如PEG400，唑类或三唑如伊曲康唑或泊沙康唑 其基本上不含表面活性剂，特别是非离子表面活性剂，并且具有低水平的水，优选小于5％的水。 在输注到免疫受损的哺乳动物，优选人中之前，组合物可以用输注液（例如生理盐水或5％或10％葡萄糖水溶液）进一步稀释。 该组合物可用于治疗和抑制由诸如对唑类敏感的酵母和霉菌等微生物引起的感染，但可延长其溶解其他可用于治疗其他类型感染性疾病或其它疾病的药物活性剂 ，如恶性和自身免疫性疾病。

    Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same
    2.
    发明授权
    Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same 有权
    亲脂性药剂的肠胃外制剂及其制备和使用方法

    公开(公告)号：US09364433B2

    公开(公告)日：2016-06-14

    申请号：US13452033

    申请日：2012-04-20

    申请人： Borje S. Andersson ,  Benigno C. Valdez ,  Jeffrey Tarrand

    发明人： Borje S. Andersson ,  Benigno C. Valdez ,  Jeffrey Tarrand

    IPC分类号： A61K47/10 ,  A61K31/255 ,  A61K31/496 ,  A61K9/00 ,  A61K9/107

    CPC分类号： A61K31/496 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/1075 ,  A61K31/255 ,  A61K47/02 ,  A61K47/10 ,  A61K47/26

    摘要： There may be provided compositions of lipophilic pharmaceutical agents with improved solubility and stability. For example, there may be provided a non-aqueous composition that comprises a lipophilic pharmaceutical agent, and an amphiphilic polymeric solvent such as PEG400 but essentially free of organic solvents and non-solubilized particles. The composition may be further diluted with a desired aqueous diluent such as an infusion fluid for parenteral administration to a subject such as a human. The compositions may be useful for the treatment for diseases or conditions that are sensitive to lipophilic agents, such as infectious diseases, malignant or autoimmune diseases.

    摘要翻译： 可以提供具有改善的溶解度和稳定性的亲脂性药剂的组合物。 例如，可以提供包含亲脂性药剂和两亲性聚合物溶剂如PEG400但基本上不含有机溶剂和未溶解颗粒的非水性组合物。 组合物可以用所需的水性稀释剂如用于胃肠外给药的输注液进一步稀释至受试者例如人。 组合物可用于治疗对亲脂性试剂如感染性疾病，恶性或自身免疫性疾病敏感的疾病或病症。

    Large animal model of invasive pulmonary aspergillosis in an immunocompromised host
    6.
    发明授权
    Large animal model of invasive pulmonary aspergillosis in an immunocompromised host 失效
    免疫受损宿主侵袭性肺曲霉病的大动物模型

    公开(公告)号：US06444872B1

    公开(公告)日：2002-09-03

    申请号：US09642397

    申请日：2000-08-18

    申请人： Borje S. Andersson ,  Taraneh K. Sadeghi ,  Douglas M. Cromeens ,  Jeffrey J. Tarrand

    发明人： Borje S. Andersson ,  Taraneh K. Sadeghi ,  Douglas M. Cromeens ,  Jeffrey J. Tarrand

    IPC分类号： A01K6700

    CPC分类号： A61K49/0004 ,  A01K67/027 ,  C12Q1/025

    摘要： A model of systemic mold/Aspergillus infection in a profoundly immunocompromised host has been established in the beagle dog. The beagle was rendered immunosuppressed using a combination of total body irradiation and daily steroids, which provided a window of time where the mold could be successfully inoculated through a bronchoscope. This created a localized infection in one lung lobe, which subsequently spread diffusely throughout the lung parenchyma, and uniformly resulted in the animal's death. The invention contemplates the further study of the pathophysiology of opportunistic mold infections in vivo and also provides examples for the development of new antifungal agents and more effective combinations of agents. Finally, the invention contemplates the development of technology for the early detection of systemic mold infections. The inventors envision, that the use of the model should help save patients from clinical trials of antifungal drugs that may be effective in vitro without living up to the expectations in a clinical setting.

    摘要翻译： 在比格犬中已经建立了一个深度免疫受损宿主的全身霉菌/曲霉菌感染模型。 使用全身照射和日常类固醇的组合使小猎犬进行免疫抑制，这提供了通过支气管镜成功接种霉菌的时间窗口。 这在一个肺叶中产生局部感染，其随后在整个肺实质中扩散扩散，并且均匀地导致动物的死亡。 本发明考虑进一步研究体内机会性霉菌感染的病理生理学，还提供了开发新的抗真菌剂和更有效的药剂组合的实例。 最后，本发明考虑了用于早期检测全身性霉菌感染的技术的发展。 本发明人设想，该模型的使用应该有助于挽救来自抗真菌药物的临床试验的患者，所述抗真菌药物在体外可能是有效的，而不能达到临床环境中的预期。

    Pharmacologically acceptable solvent vehicles
    8.
    发明授权
    Pharmacologically acceptable solvent vehicles 失效
    药理学上可接受的溶剂车

    公开(公告)号：US07153838B2

    公开(公告)日：2006-12-26

    申请号：US09415890

    申请日：1999-10-08

    申请人： Borje S. Andersson ,  Elias J. Anaissie

    发明人： Borje S. Andersson ,  Elias J. Anaissie

    IPC分类号： A61K31/7008 ,  A61K9/07 ,  A61K25/02

    CPC分类号： A61K47/18 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/107 ,  A61K9/19 ,  Y10S514/937 ,  Y10S514/938 ,  Y10S514/943 ,  Y10S514/97 ,  Y10S514/974

    摘要： An antifungal composition suitable for parenteral administration to a mammal includes an amount of pimaricin or an antifungal derivative thereof that is effective to inhibit the growth of a fungal infection in a mammal; a pharmaceutically acceptable dipolar aprotic solvent; and a pharmaceutically acceptable aqueous secondary solvent. The composition can be used in methods of preventing or treating a systemic fungal infection in a mammal. The composition can be prepared by dissolving pimaricin or an antifungal derivative thereof in the pharmaceutically acceptable dipolar aprotic solvent; adding to the solution a pharmaceutically acceptable aqueous secondary solvent; and in a preferred method, by subsequently lypohilizing the composition, whereby a dry, shelf-stable composition is produced. This dry composition can be reconstituted into an aqueous solution suitable for parenteral administration.

    摘要翻译： 适合于向哺乳动物肠胃外给药的抗真菌组合物包括一定量的有效抑制哺乳动物真菌感染生长的派马林或其抗真菌衍生物; 药学上可接受的偶极非质子溶剂; 和药学上可接受的水性二级溶剂。 该组合物可用于预防或治疗哺乳动物全身真菌感染的方法。 该组合物可以通过将派马林或其抗真菌衍生物溶解在药学上可接受的偶极非质子溶剂中来制备; 向该溶液中加入药学上可接受的水性二级溶剂; 并且在优选的方法中，通过随后将组合物洗脱，由此产生干燥的，稳定的组合物。 该干组合物可以重构成适合肠胃外给药的水溶液。