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    • 66. 发明授权
    • Microcapsules, method of making and their use
    • 微胶囊,制作方法及其用途
    • US06403057B1
    • 2002-06-11
    • US09599576
    • 2000-06-23
    • Michel SchneiderPhilippe Bussat
    • Michel SchneiderPhilippe Bussat
    • A61K4900
    • A61K9/0065A61K9/5015A61K49/223
    • The invention relates to microcapsules to a microcapsule with a mean size from a fraction of micrometer to 1000 micrometers having a biodegradable membrane encapsulating a gas core. The membrane comprising one or more biodegradable water insoluble lipids or mixtures thereof and optionally mixtures of the lipids with up to 75% by weight of biodegradable polymers encapsulates the core which is filled with air or a gas. Microcapsules disclosed, may be non-coalescent, dry and instantly dispersible, when in suspension in a physiologically acceptable carrier are useful as delivery vehicles for therapeutically active agents and/or as contrast agents for echographic imaging of organs of human or animal body. The microcapsules of the invention are made by a method in which a water-in-oil emulsion is made from an organic solution comprising dissolved a mono-, di-, triglyceride preferably tripalmitin or tristearin and optionally therapeutically active substance and an aqueous solution containing a surfactant, optionally evaporating part of the solvent, adding a redispersing agent and freeze drying the mixture. The freeze dried mixture is then redispersed in an aqueous carrier to separate microcapsules from debris and the semi-spherical or spherical microcapsules are dried.
    • 本发明涉及到微胶囊的微胶囊,其平均尺寸为千分之一至1000微米,具有封装气芯的可生物降解的膜。 所述膜包含一种或多种可生物降解的水不溶性脂质或其混合物,以及脂质与高达75%(重量)可生物降解聚合物的任选混合物包封填充有空气或气体的核心。 公开的微胶囊可以是非聚结剂,干燥和即时可分散的,当在生理学上可接受的载体中的悬浮液可用作治疗活性剂的递送载体和/或作为用于人或动物体器官的回波成像的对比剂时。 本发明的微胶囊通过一种方法制备,其中油包水乳液由有机溶液制成,该有机溶液包含溶解的甘油单酯,二甘油三酯,优选三棕榈素或三硬脂精和任选的治疗活性物质和含有 表面活性剂,任选地蒸发部分溶剂,加入再分散剂并冷冻干燥混合物。 然后将冷冻干燥的混合物再分散在水性载体中以将微胶囊与碎片分离,并将半球形或球形微胶囊干燥。