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    • 3. 发明申请
    • LIPOSOMES FOR PULMONARY APPLICATION
    • 用于肺部应用的脂质体
    • WO2011000835A3
    • 2011-03-03
    • PCT/EP2010059216
    • 2010-06-29
    • UNIV GIESSEN JUSTUS LIEBIGGESSLER TOBIASSCHMEHL THOMASRIEGER MONIKA
    • GESSLER TOBIASSCHMEHL THOMASRIEGER MONIKA
    • A61K9/00A61K9/127
    • A61K9/127A61K9/0078
    • The invention relates to liposomes for pulmonary application, advantageously comprising at least one first and at least one second phospholipid, cholesterol, and at least one active substance and/or colorant, wherein the first phospholipid is a phosphatidylcholine, preferably DSPC, and the second phospholipid is a phosphatidylcholine or an ethanolamine, preferably selected from the group DMPC, DPPC, DPPE. It is thereby advantageous if the first and the second phospholipid are present at a molar ratio of 0.5:1 to 10:1, preferably at a ratio of 6:1 to 2:1, in particular preferably at a ratio of 3:1. It is further advantageous if the molar ratio between phospholipids and cholesterol is between 10:1 and 1:1, preferably between 6:1 and 3:1, in particular preferably 4:1. The second phospholipid is further preferably DMPC or DPPE, in particular preferably DPPE. The size of the liposomes is advantageously between 0.05 µm and 5 µm, preferably between 0.2 µm and 2.0 µm, and the median aerodynamic mass diameter of aerosol particles comprising the liposomes is between 1 µm and 6 µm, preferably between 1.5 µm and 5 µm, in particular preferably between 2 µm and 4.5 µm. It is further in particular advantageous if the liposomes comprise an atomization stability of greater than 50%, preferably greater than 75%, in particular preferably greater than 80%, and if the transition temperature is greater than 37 °C, preferably greater than 45 °C, in particular preferably greater than 50 °C.
    • 为有利地包含至少一个第一和至少一个第二磷脂和胆固醇和至少一种活性物质和/或染料,其中所述第一磷脂是磷脂酰胆碱,优选DSPC,和第二磷脂肺施用本发明的脂质体是磷脂酰胆碱或乙醇胺 优选选自DMPC,DPPC,DPPE。 有利的是,当第一和在0.5:1的摩尔比的第二磷脂:1〜10:1,优选在6:1的比例为2:1,更优选为3:1的比例存在 , 也有利的是,如果磷脂和胆固醇10之间的摩尔比:1和1:1之间,优选在6:1和3:1,更优选4:1。 应进一步理解,第二种磷脂优选为DMPC或DPPE,更优选为DPPE。 有利地,脂质体的大小为0.05微米和5微米之间,优选在0.2微米和2.0微米和含脂质体是1微米和6微米之间的气溶胶颗粒的质量中值空气动力学直径之间,优选为1.5微米之间 和5μm,更优选在2μm和4.5μm之间。 这也是特别有利的,如果超过50%,优选超过75%,特别优选80%以上的脂质体雾化稳定性,并且当转变温度超过37℃,优选大于45℃,更优选 超过50℃
    • 4. 发明申请
    • COMPOSITE MATERIALS LOADED WITH THERAPEUTIC AND DIAGNOSTIC AGENTS COMPRISING POLYMER NANOPARTICLES AND POLYMER FIBERS
    • 药物和诊断负载的复合材料综合聚合物纳米微粒以及聚合物纤维
    • WO2010106063A3
    • 2011-09-29
    • PCT/EP2010053381
    • 2010-03-16
    • UNIV GIESSEN JUSTUS LIEBIGUNIV MARBURG PHILIPPSTRANSMIT GMBHSCHMEHL THOMASNGUYEN JULIANEBECK-BROICHSITTER MORITZGESSLER TOBIASKISSEL THOMASTHIEME MARCEL
    • SCHMEHL THOMASNGUYEN JULIANEBECK-BROICHSITTER MORITZGESSLER TOBIASKISSEL THOMASTHIEME MARCEL
    • A61K9/51A61K9/70
    • A61K9/5153A61K9/70
    • The invention relates to composite materials comprising polymer nanofibers and polymer nanoparticles, wherein at least one of the two polymer materials is loaded with a substance selected from therapeutic and diagnostic agents. Fibers and nanoparticles can comprise identical or different polymers; the polymer materials are, however, biocompatible in every case. Therapeutic and diagnostic agents can be hydrophilic or lipophilic and the two polymer materials likewise. The at least one polymer material and the substance with which said material is loaded are either both hydrophilic or both lipophilic. The polymer nanoparticles of the composite materials have a diameter of 10 nm to 600 nm. The polymer fibers have diameters of 10 nm to 50 µm and lengths of 1 µm to several meters. The invention further relates to a method for producing said composite materials. Polymer nanoparticles can be produced in different ways, such as through controlled precipitation of a polymer solution that optionally comprises a loading substance. The nanoparticles are then mixed with another polymer and a loading substance as applicable, depending on whether particles, fibers or both are to be loaded with substance. The processing of this solution into composites comprising polymer fibers polymer nanoparticles can occur by means of electrospinning, melt spinning, extruding or template process. Composite materials according to the invention are suitable for the production of pharmaceuticals that release therapeutically or diagnostically effective substances slowly and in a controlled manner.
    • 本发明提供了包含制备的聚合物纳米纤维和纳米颗粒的聚合物复合材料,其特征在于,在治疗和诊断中加载的物质中选择的两种聚合物材料中的至少一种。 纤维和纳米颗粒可以由相同或不同的聚合物; 然而,聚合材料是在每种情况下生物相容的。 治疗和诊断由此可以是亲水性或亲脂性,以及两种聚合物材料为好。 所述至少一种聚合物材料和与它加载的物质,无论是二者均为亲水或亲脂。 复合材料的聚合物纳米颗粒的直径为10nm至600nm的。 所述聚合物纤维具有从10纳米至50微米的直径和1微米长度可达几米。 本发明提供了一种制备所述复合材料的进一步处理。 聚合物纳米颗粒可以以各种方式通过聚合物溶液的控制的沉淀来制备,例如,任选地含有负载物质。 随后,将纳米颗粒与另一种聚合物混合,并且如果必要的话,装载物质,根据不同的颗粒,纤维,或两者是否将被装载的物质。 这种解决方案的处理,以复合材料,其包括聚合物纤维的聚合物纳米颗粒可以,例如,静电纺丝,熔融纺丝,挤出或通过装置发生模板。 根据本发明的复合材料是适合于释放治疗或诊断活性物质缓慢和受控的药物中的用途。