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    • 9. 发明申请
    • UNILAMELLAR LIPOSOMAL PREPARATIONS WITH HIGH ACTIVE SUBSTANCE CONTENT
    • 单层脂质体具有高主动型筹备工作
    • WO1996005808A1
    • 1996-02-29
    • PCT/DE1995001162
    • 1995-08-18
    • MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZINBRANDL, MartinBACHMANN, DieterRESZKA, RegineDRECHSLER, Markus
    • MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN
    • A61K09/133
    • A61K9/1277Y10T428/2984
    • The liposomal preparation proposed is suitable for use in pharmaceutics and medicine, in particular as a carrier for drugs, vaccines, diagnostic agents and vectors. Its production and use are also disclosed. The liposomes in the preparation proposed are exclusively, or to by far the greater part, unilamellar liposomes of small to medium size, preferably 10 t0 300 nm in diameter, with a closely packed vesicular structure. A high proportion, preferably at least 20 %, of the active substance is included in the preparation in encapsulated form. The preparation can be used directly as a depot of the encapsulated substance, or after stepwise dilution by addition of an aqueous solution. The preparation is produced by mixing a lipid or lipids, water and the active substance to be incorporated, and subsequently removing the solvents by evaporation and dispersal in water, followed by single or multiple high-pressure homogenization (at the most 50 times) at a pressure between 50 and 1600 bar (5-160 MPa) and, optionally, freeze/thaw treatment. The preparation is then converted into a free-flowing dispersion which is extruded through filters with a pore size of 0.1 to 1 mu m.
    • 本发明涉及脂质体制剂,它们的制备和它们的用途来。 应用领域医药及医药,特别是作为药物,疫苗,诊断试剂和载体载波系统中使用。 本发明的脂质体制剂从到中型,优选为100〜300nm的直径,具有多孔结构的致密堆积的小的单层脂质体完全或主要组成。 它包含高比例的,优选至少20%,以包封形式的活性成分。 该制剂可以直接作为包封的物质的贮库或通过加入水性介质的逐步稀释来施加。 制剂的通过蒸发和分散在水中的一种或更多次(最大50malige)高压均质化混合脂质(一个或多个),水和einzuschliessendem活性成分,随后去除溶剂,用50和1600巴之间的压力的制备(5-160兆帕 )和随后的冷冻,必要/融处理,转化成通过具有0.1至1微米的孔尺寸的过滤器自由流动的分散体和挤出。