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    • 2. 发明申请
    • PARTICLES FOR DRUG DELIVERY AND OTHER APPLICATIONS
    • 用于药物递送和其他应用的颗粒
    • WO2012027378A2
    • 2012-03-01
    • PCT/US2011048822
    • 2011-08-23
    • HARVARD COLLEGEBASF SEFAN BENKOLTZENBURG ROLAND SRIEGER JENS BWEITZ DAVID A
    • FAN BENKOLTZENBURG ROLAND SRIEGER JENS BWEITZ DAVID A
    • A61K9/14A61K9/16A61K31/565A61K31/58
    • A61K9/143A61K9/1694A61K31/565A61K31/58
    • The present invention generally relates to particles for drug delivery and other applications. In one aspect, the present invention relates to a technique for reacting precursor compounds in the presence of a pharmaceutically- active agent to form product (e.g., in the form of particles) in which the agent is substantially contained within the product, and the product is soluble within typical gastric fluid of a mammal. In another aspect, the present invention is generally directed to particles comprising an inorganic pharmaceutically acceptable carrier, such as CaCO3, and an agent. In some cases, at least some of the agent contained within the particles is fluidically inaccessible from externally of the particle. For instance, the agent may be present in isolated domains within the particle. In another aspect, the present invention is generally directed to methods of creating particles. For instance, according to one set of embodiments, two fluids containing reactants are mixed where, upon reaction of the reactants, an insoluble product is formed, which precipitates to form particles. In one example, a first fluid containing dissolved carbonate ions and a second fluid containing dissolved calcium ions and a pharmaceutically- active agent are mixed together; upon mixing of the first and second fluids, the calcium ions and the carbonate ions form calcium carbonate, which precipitates to form a co-precipitate with the pharmaceutically- active agent. Yet other aspects of the present invention are directed to particles formed from such reactions, methods of using such reactions, methods of promoting such reactions, kits involving particles, or the like.
    • 本发明总体上涉及用于药物递送和其他应用的颗粒。 在一个方面,本发明涉及一种用于使前体化合物在药物活性剂存在下反应以形成其中药剂基本上包含在产品内的产品(例如,以颗粒形式)的技术,并且产品 可溶于哺乳动物的典型胃液中。 另一方面,本发明一般涉及包含无机药学上可接受的载体如CaCO 3和药剂的颗粒。 在一些情况下,包含在颗粒内的至少一些试剂从颗粒的外部流体不可接近。 例如,该药剂可能存在于颗粒内的分离域中。 另一方面,本发明总体上涉及产生颗粒的方法。 例如,根据一组实施方案,混合含有反应物的两种流体,其中在反应物反应时形成不溶产物,其沉淀形成颗粒。 在一个实例中,将含​​有溶解的碳酸根离子的第一流体和含有溶解的钙离子的第二流体与药物活性剂混合在一起; 在混合第一流体和第二流体时,钙离子和碳酸根离子形成碳酸钙,其沉淀与药物活性剂形成共沉淀物。 本发明的其他方面涉及由这些反应形成的颗粒,使用这些反应的方法,促进这种反应的方法,涉及颗粒的试剂盒等。
    • 3. 发明申请
    • FOAMS OR PARTICLES FOR APPLICATIONS SUCH AS DRUG DELIVERY
    • 用于药物递送应用的FOAMS或颗粒
    • WO2011146852A8
    • 2013-03-07
    • PCT/US2011037363
    • 2011-05-20
    • HARVARD COLLEGEBASF SELADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHAMRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • LADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHAMRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • A61K9/12A61K9/14A61K47/32
    • A61K9/122A61K9/146A61K47/32
    • The present invention generally relates to foams and, in particular, to foams for applications such as drug delivery, and particles that are made from such foams. One aspect relates to foams or particles containing pharmaceutically active agents. The foam may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foam or particle has an unexpectedly high specific surface area. A high specific surface area may, in some cases, facilitate delivery or release of the pharmaceutically active agent when the foam or particles made from the foam (e.g., by milling) are administered to a subject. The foam may also exhibit a relatively high loading of the pharmaceutically active agent. In some cases, the foam may be a microcellular foam. In one set of embodiments, the foam is created using a supercritical fluid, such as supercritical C02. For example, a precursor to the foam, containing a pharmaceutically active agent, may be mixed with a foaming agent, then the pressure decreased to cause the foaming agent to expand, thereby causing a foam to form. The foam may then be subsequently ground or milled, or otherwise processed to form particles.
    • 本发明一般涉及泡沫,特别是泡沫用于例如药物递送的泡沫,以及由这种泡沫制成的颗粒。 一个方面涉及含有药物活性剂的泡沫或颗粒。 泡沫可以包含药学上可接受的聚合物载体。 在一些情况下,泡沫或颗粒具有出乎意料的高比表面积。 在一些情况下,当由泡沫制成的泡沫或颗粒(例如通过研磨))施用于受试者时,高比表面积可能有助于药物活性剂的递送或释放。 泡沫体也可表现出相当高的药物活性剂负荷。 在一些情况下,泡沫可以是微孔泡沫。 在一组实施方案中,使用超临界流体(例如超临界CO 2)产生泡沫。 例如,含有药物活性剂的泡沫体的前体可与发泡剂混合,然后降低压力,引起发泡剂膨胀,从而形成泡沫。 然后可以将泡沫研磨或研磨,或以其它方式加工形成颗粒。
    • 4. 发明申请
    • FOAM OR PARTICLES FOR APPLICATIONS SUCH AS DRUG DELIVERY
    • 用于药物递送应用的泡沫或颗粒
    • WO2011146852A3
    • 2012-07-05
    • PCT/US2011037363
    • 2011-05-20
    • HARVARD COLLEGEBASF SELADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHAMRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • LADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHAMRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • A61K9/12A61K9/14A61K47/32
    • A61K9/122A61K9/146A61K47/32
    • The present invention generally relates to foams and, in particular, to foams for applications such as drug delivery, and particles that are made from such foams. One aspect relates to foams or particles containing pharmaceutically active agents. The foam may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foam or particle has an unexpectedly high specific surface area. A high specific surface area may, in some cases, facilitate delivery or release of the pharmaceutically active agent when the foam or particles made from the foam (e.g., by milling) are administered to a subject. The foam may also exhibit a relatively high loading of the pharmaceutically active agent. In some cases, the foam may be a microcellular foam. In one set of embodiments, the foam is created using a supercritical fluid, such as supercritical C02. For example, a precursor to the foam, containing a pharmaceutically active agent, may be mixed with a foaming agent, then the pressure decreased to cause the foaming agent to expand, thereby causing a foam to form. The foam may then be subsequently ground or milled, or otherwise processed to form particles.
    • 本发明一般涉及泡沫,特别是泡沫用于例如药物递送的泡沫,以及由这种泡沫制成的颗粒。 一个方面涉及含有药物活性剂的泡沫或颗粒。 泡沫可以包含药学上可接受的聚合物载体。 在一些情况下,泡沫或颗粒具有出乎意料的高比表面积。 在一些情况下,当由泡沫制成的泡沫或颗粒(例如通过研磨))施用于受试者时,高比表面积可能有助于药物活性剂的递送或释放。 泡沫体也可表现出相当高的药物活性剂负荷。 在一些情况下,泡沫可以是微孔泡沫。 在一组实施方案中,使用超临界流体(例如超临界CO 2)产生泡沫。 例如,含有药物活性剂的泡沫体的前体可与发泡剂混合,然后降低压力,引起发泡剂膨胀,从而形成泡沫。 然后可以将泡沫研磨或研磨,或以其它方式加工形成颗粒。
    • 5. 发明申请
    • FOAMS, INCLUDING MICROCELLULAR FOAMS, CONTAINING COLLOIDAL PARTICULATES
    • FOAMS,包括微胶囊,含有胶体颗粒
    • WO2011146858A3
    • 2012-05-31
    • PCT/US2011037377
    • 2011-05-20
    • HARVARD COLLEGEBASF SELADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHANRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • LADAVAC KOSTAGUERRA RODRIGO EKAZ DAVIDMANOHARAN VINOTHANRIEGER JENS BKOLTZENBURG ROLAND SEBASTIANWEITZ DAVID A
    • A61K9/12A61K9/14A61K9/51
    • A61K9/122A61K9/143A61K9/146A61K9/5115
    • The present invention generally relates to foams and particles made from such foams, for applications such as drug delivery. The foams or particles may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foams may include colloidal particulates. A first aspect of the present invention is generally related to polymer-based foams or particles containing pharmaceutically active agents. In some cases, the foam or particle may contain smaller colloidal particulates therein. Such colloidal particulates may be used, for example, to limit the amount of material within certain regions of the foam, or exclude pharmaceutically active agents from being located within certain portions of the foam, which may useful for enhancing release of pharmaceutically active agents from the foam. In some cases, the colloidal particulates may cause the foam or particle to have an unexpectedly high specific surface area. The foam, in certain embodiments, can exhibit a relatively high loading of the pharmaceutically active agent. The foam may be microcellular in certain instances. The foam may also be created using a supercritical fluid, for example, supercritical C02. For instance, a precursor to the foam, containing a pharmaceutically active agent, a pharmaceutically acceptable polymeric carrier, and colloidal particulates, can be mixed with a foaming agent. The pressure may then be decreased, thereby causing the foaming agent to expand and causing a foam to form. The foam may also be ground or milled, or otherwise processed, to form particles such as nanoparticles.
    • 本发明一般涉及由这种泡沫制成的泡沫和颗粒,用于诸如药物递送的应用。 泡沫或颗粒可以包含药学上可接受的聚合物载体。 在一些情况下,泡沫可以包括胶体颗粒。 本发明的第一方面通常涉及基于聚合物的泡沫或含有药物活性剂的颗粒。 在一些情况下,泡沫或颗粒中可含有较小的胶体颗粒。 这种胶体颗粒可以用于例如限制泡沫的某些区域内的物质的量,或者不排除药物活性剂位于泡沫的某些部分内,其可用于增强药物活性剂从 泡沫。 在一些情况下,胶体颗粒可能导致泡沫或颗粒具有出乎意料的高比表面积。 在某些实施方案中,泡沫体可以表现出相对高的药物活性剂的负载量。 泡沫在某些情况下可能是微孔的。 泡沫也可以使用超临界流体,例如超临界CO 2来产生。 例如,含有药物活性剂,药学上可接受的聚合物载体和胶体颗粒的泡沫的前体可与发泡剂混合。 然后可以降低压力,从而使发泡剂膨胀并形成泡沫。 泡沫也可以研磨或研磨或以其它方式处理,以形成颗粒如纳米颗粒。