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    • 4. 发明授权
    • Coated microparticle agglomerates
    • 涂布的微粒附聚物
    • US5788991A
    • 1998-08-04
    • US532550
    • 1995-09-29
    • Rudolf NastkeErnst NeuenschwanderAndreas Leonhardt
    • Rudolf NastkeErnst NeuenschwanderAndreas Leonhardt
    • A01N25/10A01N25/26A01N25/28A01N43/54A01N43/70A61K9/22B01J13/18A61K9/16A61K9/50
    • B01J13/18A01N25/28
    • One object of the invention, therefore, is to provide encapsulated biologically active solid microparticle agglomerates, each agglomerate comprising either I i) at least two closely associated microparticles, each microparticle being coated partially or completely by at least one discrete layer of a polymer, and ii) at least one outer discrete coating layer of the same polymer which envelops the coated microparticles to form an agglomerate of closely associated microparticles, or II i) a cluster of at least two closely associated microparticles, each microparticle being coated partially or completely by at least one layer of a polymer, the microparticles adhering together through the polymer to form said cluster, and ii) at least one outer discrete coating layer of the same polymer which envelops said cluster to form a discrete agglomerate, wherein in types I and II an inter-phase boundary is formed between each particle and the first coating layer, between individual coating layers and between the outer agglomerating envelope layer and the penultimate coating layer, and the total weight of polymer coating within and outside the agglomerate is no greater than 40% of the average agglomerate weight.
    • PCT No.PCT / EP94 / 00881 Sec。 371 1995年9月29日第 102(e)1995年9月29日PCT PCT 1994年3月21日PCT公布。 公开号WO94 / 22303 日期为1994年10月13日本发明的一个目的是提供封装的生物活性固体微粒附聚物,每个附聚物包括I i)至少两个密切相关的微粒,每个微粒部分或完全被至少一个离散层 的聚合物,和ii)相同聚合物的至少一个外部离散的涂层,其包封涂覆的微粒以形成紧密相关的微粒的聚集体,或II i)至少两个紧密相关的微粒的簇,每个微粒被涂覆 部分或完全由至少一层聚合物组成,微粒通过聚合物粘合在一起以形成所述簇,以及ii)包封所述簇以形成离散附聚物的相同聚合物的至少一个外离散涂层,其中在 类型I和II在个体之间在每个颗粒和第一涂层之间形成一个相间边界 涂覆层之间以及外部附聚包膜层和倒数第二涂层之间,聚集体内部和外部的聚合物涂层的总重量不大于平均聚集体重量的40%。
    • 6. 发明授权
    • Process for the preparation of spherical microparticles containing
biologically active compounds
    • 制备含有生物活性化合物的球形微粒的方法
    • US5908632A
    • 1999-06-01
    • US776401
    • 1997-01-21
    • Rudolf NastkeErnst Neuenschwander
    • Rudolf NastkeErnst Neuenschwander
    • B01J13/14A01N25/28A01N43/54A01N47/30A01N57/16B01J13/18
    • A01N25/28
    • The invention relates to a process for encapsulating biologically active compounds in the form of substantially spherical microparticles, comprising the steps ofa) preparing an aqueous solution of surfactants, catalysts and monomers or prepolymers which are suitable for forming a crosslinked polycondensate,b) forming an emulsion of the substantially water-insoluble biologically active compound or mixture thereof in the solution a) by adding said solution under high shear force, andc) forming a solid capsule wall around the biologically active compound or mixture thereof by heating the reaction mixture to a temperature at which the crosslinking reaction tales place,which process comprises fusing the biologically active compound or mixture thereof and adding the melt to the aqueous reaction mixture at a temperature which is higher than the temperature of the reaction mixture.
    • PCT No.PCT / EP95 / 02727 Sec。 371日期1997年1月21日 102(e)日期1997年1月21日PCT提交1995年7月12日PCT公布。 公开号WO96 / 03040 日期1996年2月8日本发明涉及一种以基本上球形的微粒形式包封生物活性化合物的方法,包括以下步骤:a)制备适于形成交联缩聚物的表面活性剂,催化剂和单体或预聚物的水溶液 b)在溶液中形成基本上不溶于水的生物活性化合物或其混合物的乳液a)通过在高剪切力下加入所述溶液,和c)通过加热在生物活性化合物或其混合物周围形成固体胶囊壁 将反应混合物加热至交联反应产生的温度,该方法包括将生物活性化合物或其混合物熔融并在高于反应混合物温度的温度下将熔体加入到水性反应混合物中。