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    • 2. 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
    • US5785976A
    • 1998-07-28
    • US226471
    • 1994-04-12
    • Kirsten WestesenBritta Siekmann
    • Kirsten WestesenBritta Siekmann
    • A01N25/04A61K8/04A61K8/67A61K9/10A61K9/14A61K9/51A61Q19/00B01F3/08B01F3/12A61K9/19B01J13/00
    • A61K8/044A01N25/04A61K8/0241A61K8/671A61K9/10A61K9/145A61K9/5123A61Q19/00B01F3/0811B01F3/1214B82Y5/00A61K2800/413B01F2003/0892B01F3/0807Y10S514/965Y10S516/922Y10S516/926Y10S516/93Y10T428/2989
    • 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. (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作为递送系统的用途,主要用于肠胃外给药优选水溶性差的生物活性物质,特别是药物,以及它们在化妆品,食品和农产品中的用途。 SLP和PBA通过以下乳化方法制备:(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)稳定剂仅根据其物理化学特性而添加到脂质或生物活性剂中,并且添加到水相或水相中。 (3)如果物质的物理化学特性允许或可能在均匀化之前溶解,溶解或分散在脂质熔体中,则要并入SLP的药物或其他生物活性物质可与脂质一起熔化。 (4)在混合之前将水相加热至熔体的温度,并且可以含有例如稳定剂,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优选通​​过高压均质化在水相中乳化。
    • 3. 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
    • US5885486A
    • 1999-03-23
    • US757276
    • 1996-12-02
    • Kirsten WestesenBritta Siekmann
    • Kirsten WestesenBritta Siekmann
    • A01N25/04A61K8/04A61K8/67A61K9/10A61K9/14A61K9/51A61Q19/00B01F3/08B01F3/12B01J13/00
    • A61K8/044A01N25/04A61K8/0245A61K8/671A61K9/10A61K9/145A61K9/5123A61Q19/00B01F3/0811B01F3/1214B82Y5/00A61K2800/413A61K2800/56B01F2003/0892B01F3/0807Y10S514/937Y10S514/964Y10S516/926Y10S516/928Y10T428/2989
    • 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作为递送系统的用途,主要用于肠胃外给药优选水溶性差的生物活性物质,特别是药物,以及它们在化妆品,食品和农产品中的用途。 SLP和PBA通过以下乳化方法制备:(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)稳定剂仅根据其物理化学特性而添加到脂质或生物活性剂中,并且添加到水相或水相中。 均化后也可加入或交换稳定剂。 (3)如果物质的物理化学特性允许或可能在均匀化之前溶解,溶解或分散在脂质熔体中,则要并入SLP的药物或其他生物活性物质可与脂质一起熔化。 (4)在混合之前将水相加热至熔体的温度,并且可以含有例如稳定剂,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优选通​​过高压均质化在水相中乳化。
    • 6. 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。
    • 7. 发明授权
    • Manufacturing solvent-free solid paint
    • 制造无溶剂固体涂料
    • US07192996B2
    • 2007-03-20
    • US10450392
    • 2001-12-12
    • Garry Michael McKay
    • Garry Michael McKay
    • C08K3/00B01F3/00
    • C09D5/03B01F3/0853B01F7/1605B01F15/065B01F2003/0892B01F2015/062B01F2215/005B44D3/06B44D3/12C08J3/205
    • A method and apparatus for manufacturing small batches of solid paint is disclosed, which method includes a first step of providing a component of the solid paint as a liquid in a heated mixing container that has a base and sides and includes a stirrer for stirring the contents of the container. The next step of the method includes controlling, heating and stirring of the contents of the container and progressively adding other components of the solid paint as solids to the container. The liquid acts as a heat transfer medium that transfers heat from the heated container and from the stirrer to the solids. The mix is heated to a temperature of the solid paint and forms a melt that is a uniform liquid. The final step in the method includes discharging the melt from the container and allowing the melt to cool and form the solid paint.
    • 公开了一种用于制造小批量固体涂料的方法和装置,该方法包括:第一步骤,将固体涂料的组分作为液体提供在具有底部和侧面的加热混合容器中,并且包括用于搅拌内容物的搅拌器 的容器。 该方法的下一步包括控制,加热和搅拌容器的内容物,并将固体涂料的其它组分逐渐添加到容器中。 液体作为传热介质,其将热量从加热的容器和从搅拌器传递到固体。 将混合物加热至固体涂料的温度,并形成均匀液体的熔体。 该方法的最后步骤包括从容器中排出熔体并使熔体冷却并形成固体涂料。
    • 8. 发明申请
    • Manufacturing solvent-free solid paint
    • 制造无溶剂固体涂料
    • US20040048953A1
    • 2004-03-11
    • US10450392
    • 2003-09-25
    • Garry Michael McKay
    • C08K003/00
    • C09D5/03B01F3/0853B01F7/1605B01F15/065B01F2003/0892B01F2015/062B01F2215/005B29B7/16B29B7/286B29B7/823B29B7/826B29B7/94B44D3/06B44D3/12C08J3/205
    • A method and apparatus for manufacturing small batches of solid paint is disclosed, which method includes a first step of providing a component of the solid paint as a liquid in a heated mixing container that has a base and sides and includes a stirrer for stirring the contents of the container. The next step of the method includes controlling, heating and stirring of the contents of the container and progressively adding other components of the solid paint as solids to the container. The liquid acts as a heat transfer medium that transfers heat from the heated container and from the stirrer to the solids. The mix is heated to a temperature of the solid paint and forms a melt that is a uniform liquid. The final step in the method includes discharging the melt from the container and allowing the melt to cool and form the solid paint.
    • 公开了一种用于制造小批量固体涂料的方法和装置,该方法包括:第一步骤,将固体涂料的组分作为液体提供在具有底部和侧面的加热混合容器中,并且包括用于搅拌内容物的搅拌器 的容器。 该方法的下一步包括控制,加热和搅拌容器的内容物,并将固体涂料的其它组分逐渐添加到容器中。 液体作为传热介质,其将热量从加热的容器和从搅拌器传递到固体。 将混合物加热至固体涂料的温度,并形成均匀液体的熔体。 该方法的最后步骤包括从容器中排出熔体并使熔体冷却并形成固体涂料。