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    • 59. 发明授权
    • Solid lipid particles, particles of bioactive agents and methods for the manufacture and use thereof
    • 固体脂质颗粒,生物活性剂颗粒及其制造和使用方法
    • US06207178B1
    • 2001-03-27
    • US09204075
    • 1998-12-03
    • Kirsten WestesenBritta Siekmann
    • Kirsten WestesenBritta Siekmann
    • A01N2504
    • A61K8/044A01N25/04A61K8/0245A61K8/671A61K9/10A61K9/145A61K9/5123A61K2800/413A61K2800/56A61Q19/00B01F3/0807B01F3/0811B01F3/1214B01F2003/0892B82Y5/00Y10S514/937Y10S514/964Y10S516/926Y10S516/928Y10T428/2989
    • The present invention is in the area of administration forms and delivery systems for drugs, vaccines and other biologically active agents. More specifically the invention is related to the preparation of suspensions of colloidal solid lipid particles (SLPs) of predominantly anisometrical shape with the lipid matrix being in a stable polymorphic modification and of suspensions of micron and submicron particles of bioactive agents (PBAs); as well as to the use of such suspensions or the lyophilizates thereof as delivery systems primarily for the parenteral administration of preferably poorly water-soluble bioactive substances, particularly drugs, and to their use in cosmetic, food and agricultural products. SLPs and PBAs are prepared by the following emulsification process: (1) A solid lipid or bioactive agent or a mixture of solid lipids or bioactive agents is melted. (2) Stabilizers are added either to the lipid or bioactive agent and to the aqueous phase or to the aqueous phase only depending on their physicochemical characteristics. Stabilizers may also be added or exchanged after homogenization. (3) Drugs or other bioactive substances to be incorporated into the SLPs may be melted together with the lipids if the physicochemical characteristics of the substance permit or may be dissolved, solubilized or dispersed in the lipid melt before homogenization. (4) The aqueous phase is heated to the temperature of the melt before mixing and may contain for example stabilizers, isotonicity agents, buffering substances, cryoprotectants and/or preservatives. (5) The molten lipid compounds and the bioactive agents are emulsified in an aqueous phase preferably by high-pressure homogenization.
    • 本发明在药物,疫苗和其他生物活性剂的给药形式和递送系统方面。 更具体地,本发明涉及主要具有不规则形状的胶体固体脂质颗粒(SLP)的悬浮液的制备,其中脂质基质处于稳定的多态性修饰和生物活性剂(PBA)的微米和亚微米颗粒的悬浮液中; 以及这些悬浮液或其冻干物质作为递送系统的使用,主要用于肠胃外给药优选水溶性较差的生物活性物质,特别是药物,以及它们在化妆品,食品和农产品中的用途.LP和PBA被制备 通过以下乳化方法:(1)将固体脂质或生物活性剂或固体脂质或生物活性剂的混合物熔化。(2)将稳定剂加入到脂质或生物活性剂中,并加入水相或水相 只取决于它们的物理化学特性。 稳定剂也可以在均化后添加或更换。(3)如果物质的物理化学特性允许或溶解,溶解或分散在脂质中,则要并入SLP的药物或其他生物活性物质可与脂质一起溶解 (4)在混合前将水相加热至熔体的温度,并可含有稳定剂,等渗剂,缓冲物质,冷冻保护剂和/或防腐剂。(5)熔融脂质化合物和生物活性剂 在水相中优选通过高压均化乳化。
    • 60. 发明授权
    • Insect repellent and attractant compositions and methods for using same
    • 驱虫剂和引诱剂组合物及其使用方法
    • US6143288A
    • 2000-11-07
    • US241555
    • 1994-05-12
    • Craig B. WarrenJerry F. ButlerRichard A. WilsonBraja D. MookherjeeLeslie C. SmithAnna Belle Marin
    • Craig B. WarrenJerry F. ButlerRichard A. WilsonBraja D. MookherjeeLeslie C. SmithAnna Belle Marin
    • A01N49/00A01N55/00A01N55/08A01N55/10A01N31/02A01N25/08A01N31/06
    • A01N55/08A01N49/00A01N55/00Y10S424/10Y10S514/919Y10S514/964
    • Described is (i) a method of repelling Musca domestica L.(Diptera:Muscidae) or Aedes aegyptae for a finite period of time from a three-dimensional space inhabitable by Musca domnestica L.(Diptera:Muscidae) or Aedes aegyptae consisting essentially of the step of exposing a three-dimensional space to an effective Musca domestica L.(Diptera:Muscidae) or Aedes aegyptae-repelling concentration and quantity of a geraniol-containing composition consisting essentially of 50-100% of geraniol with the remainder of the composition being a compound selected from the group consisting of citronellol and nerol and (ii) a method of attracting Musca domestica L.(Diptera:Muscidae) or Aedes aegyptae using lavender absolute, benzoin, dimethyl benzyl carbinyl acetate, jasmine absolute, racemic borneol, d-limonene and/or dihydrolinalool. The attractants taken alone or in combination find utility primarily as bait enhancers for acute toxins and/or trapping devices. The above-stated attractants and repellents are described to be useful as such or contained in a polymer which can be a biodegradable polymer such as compositions containing a major proportion of poly(epsilon caprolactone) homopolymers.
    • 描述的是(i)从Musca domnestica L.(双翅目:蝇科)或伊蚊(Aedes aegyptae)所组成的三维空间有限的时间内排斥Musca domestica L.(双翅目:Muscidae)或Aedes aegyptae的方法或基本上由 将三维空间暴露于有效的Musca domestica L.(双翅目:Muscidae)或埃及伊蚊排斥浓度和量的含有香叶醇的组合物,其基本上由50-100%的香叶醇组成,其余组合物 是选自香茅醇和橙花醇的化合物和(ii)使用薰衣草绝对,苯偶姻,二甲基苄基乙酰基乙酸酯,绝对的茉莉,外消旋冰片d,吸引Musca domestica L.(双翅目:Muscidae)或Aedes aegyptae的方法 - 缩水甘油和/或二氢里哪醇。 单独或组合使用的引诱剂主要用作急性毒素和/或诱捕装置的诱饵增强剂。 上述引诱剂和驱避剂被描述为可以这样使用或包含在可以是可生物降解的聚合物的聚合物中,例如含有主要比例的聚(ε-己内酯)均聚物的组合物。