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    Polypeptide-containing pharmaceutical forms of administration in the form of microparticles and method for the preparation thereof
    1.
    发明授权
    Polypeptide-containing pharmaceutical forms of administration in the form of microparticles and method for the preparation thereof 失效
    以微粒形式的含多肽的药物给药形式及其制备方法

    公开(公告)号：US06346274B1

    公开(公告)日：2002-02-12

    申请号：US08894796

    申请日：1998-01-05

    申请人： Hans Koll ,  Gerhard Winter ,  Thomas Kissel ,  Michael Morlock

    发明人： Hans Koll ,  Gerhard Winter ,  Thomas Kissel ,  Michael Morlock

    IPC分类号： A61K916

    CPC分类号： A61K9/1652 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/1658 ,  A61K38/1816

    摘要： The invention concerns parenteral pharmaceutical forms of administration containing polypeptide in the form of microparticles and a process for the production thereof. The microparticles according to the invention contain as a biodegradable polymer an ABA triblock copolymer the A block of which is a copolymer of lactic and glycolic acid and the B block of which represents a polyethylene glycol chain, together with additives that are selected from the group comprising serum proteins, polyamino acids, cyclodextrins, cyclodextrin derivatives, saccharides, amino sugars, amino acids, detergents or carboxylic acids as well as mixtures of these additives. The microparticles according to the invention continuously release the polypeptide over a relatively long time period even when the amounts of polypeptide they include are small or susceptible to aggregation.

    摘要翻译： 本发明涉及含有微粒形式的多肽的肠胃外药物给药形式及其生产方法。 根据本发明的微粒包含作为生物可降解聚合物的ABA三嵌段共聚物，其中A嵌段是乳酸和乙醇酸的共聚物，其B嵌段代表聚乙二醇链，以及选自以下的添加剂： 血清蛋白，聚氨基酸，环糊精，环糊精衍生物，糖，氨基糖，氨基酸，去污剂或羧酸，以及这些添加剂的混合物。 根据本发明的微粒在相对长的时间段内连续地释放多肽，即使它们包括的多肽的量很小或易于聚集。

    Composite Materials Loaded with Therapeutic and Diagnostic Agents Comprising Polymer Nanoparticles and Polymer Fibers
    2.
    发明申请
    Composite Materials Loaded with Therapeutic and Diagnostic Agents Comprising Polymer Nanoparticles and Polymer Fibers 审中-公开
    由聚合物纳米颗粒和聚合物纤维组成的包含治疗和诊断剂的复合材料

    公开(公告)号：US20120148493A1

    公开(公告)日：2012-06-14

    申请号：US13256872

    申请日：2010-03-16

    申请人： Thomas Schmehl ,  Juliane Nguyen ,  Moritz Beck-Broichsitter ,  Tobias Gessler ,  Thomas Kissel ,  Marcel Thieme

    发明人： Thomas Schmehl ,  Juliane Nguyen ,  Moritz Beck-Broichsitter ,  Tobias Gessler ,  Thomas Kissel ,  Marcel Thieme

    IPC分类号： A61K9/70 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P35/00 ,  A61P17/00 ,  A61P17/02 ,  D01D5/00 ,  A61K49/00 ,  A61P3/00 ,  B82Y5/00

    CPC分类号： A61K9/5153 ,  A61K9/70

    摘要： The invention relates to composite materials comprising polymer nanofibers and polymer nanoparticles, wherein at least one of the two polymer materials is loaded with a substance selected from therapeutic and diagnostic agents. Fibers and nanoparticles can comprise identical or different polymers; the polymer materials are, however, biocompatible in every case. Therapeutic and diagnostic agents can be hydrophilic or lipophilic and the two polymer materials likewise. The at least one polymer material and the substance with which said material is loaded are either both hydrophilic or both lipophilic. The polymer nanoparticles of the composite materials have a diameter of 10 nm to 600 nm. The polymer fibers have diameters of 10 nm to 50 μm and lengths of 1 μm to several meters. The invention further relates to a method for producing said composite materials. Polymer nanoparticles can be produced in different ways, such as through controlled precipitation of a polymer solution that optionally comprises a loading substance. The nanoparticles are then mixed with another polymer and a loading substance as applicable, depending on whether particles, fibers or both are to be loaded with substance. The processing of this solution into composites comprising polymer fibers polymer nanoparticles can occur by means of electrospinning, melt spinning, extruding or template process. Composite materials according to the invention are suitable for the production of pharmaceuticals that release therapeutically or diagnostically effective substances slowly and in a controlled manner.

    摘要翻译： 本发明涉及包含聚合物纳米纤维和聚合物纳米颗粒的复合材料，其中两种聚合物材料中的至少一种负载有选自治疗剂和诊断剂的物质。 纤维和纳米颗粒可以包含相同或不同的聚合物; 然而，聚合物材料在每种情况下都是生物相容的。 治疗和诊断剂可以是亲水的或亲脂的，并且两种聚合物材料同样。 所述至少一种聚合物材料和所述材料被加载的物质既是亲水的，也是亲油的。 复合材料的聚合物纳米颗粒具有10nm至600nm的直径。 聚合物纤维的直径为10nm〜50μm，长度为1〜数米。 本发明还涉及一种生产所述复合材料的方法。 聚合物纳米颗粒可以以不同的方式制备，例如通过可选地包含负载物质的聚合物溶液的可控沉淀。 然后将纳米颗粒与另一种聚合物和负载物质混合，这取决于颗粒，纤维或两者是否被装载物质。 将该溶液加工成包含聚合物纤维聚合物纳米颗粒的复合材料可以通过静电纺丝，熔融纺丝，挤出或模板方法进行。 根据本发明的复合材料适用于缓慢地并以受控方式释放治疗或诊断有效物质的药物。

    Pharmaceutical compositions
    4.
    发明授权
    Pharmaceutical compositions 失效
    药物组合物

    公开(公告)号：US5593686A

    公开(公告)日：1997-01-14

    申请号：US314167

    申请日：1994-09-28

    申请人： Thomas Kissel ,  Henriette Schrank ,  Hans-Rainer Hoffmann

    发明人： Thomas Kissel ,  Henriette Schrank ,  Hans-Rainer Hoffmann

    IPC分类号： A61K9/70 ,  A61K31/40 ,  A61F13/02

    CPC分类号： A61K9/7061 ,  A61K31/40 ,  A61K9/7084

    摘要： The present invention provides a pharmaceutical composition for the transdermal systemic administration of an active agent characterized in that the active agent is bopindolol or methysergide. Also the present invention provides a pharmaceutical composition for the transdermal systemic administration of a pharmacologically active agent characterized in that it contains bopindolol, tizanidine, clemastine, ketotifen or methysergide as active agent in a reservoir comprising a hydrophilic polymer. Furthermore a pharmaceutical composition for the transdermal systemic administration of pharmacologically active agents characterized in that the pharmacologically active agent is in a reservoir comprising a polyacrylate polymer containing cationic ester groups.

    摘要翻译： 本发明提供了一种用于经皮全身给药活性剂的药物组合物，其特征在于活性剂是苯吲哚洛尔或甲基麦角苷。 本发明还提供了一种药物组合物，其用于药理学活性剂的经皮系统性给药，其特征在于在包含亲水性聚合物的储库中含有苯妥萘洛，替扎尼定，克立马斯酮，酮替芬或甲基麦角苷作为活性剂。 此外，用于经皮系统施用药理活性剂的药物组合物，其特征在于药理活性剂在包含含有阳离子酯基的聚丙烯酸酯聚合物的储库中。

    PHARMACEUTICAL COMPOSITIONS
    5.
    发明申请
    PHARMACEUTICAL COMPOSITIONS 审中-公开
    药物组合物

    公开(公告)号：US20110305742A1

    公开(公告)日：2011-12-15

    申请号：US13090788

    申请日：2011-04-20

    申请人： Michael Ausborn ,  Thomas Kissel

    发明人： Michael Ausborn ,  Thomas Kissel

    IPC分类号： A61K9/00 ,  A61P9/00

    CPC分类号： A61L31/16 ,  A61L29/085 ,  A61L29/16 ,  A61L31/10 ,  A61L2300/416 ,  A61L2300/604 ,  C08L69/00

    摘要： A device implantable into a human or animal body comprising a biodegradable polymer which comprises ethylene carbonate units of the formula A -(—C(O)—O—CH2—CH2—O—)-  A having an ethylene carbonate content of 70 to 100 Mol %, an intrinsic viscosity of 0.4 to 4.0 dl/g measured in chloroform at 20° C. at a concentration of 1 g/dl and a glass transition temperature of from 5 to 50° C., degradable by surface erosion which is governed by a non-hydrolytic mechanism.

    摘要翻译： 一种可植入人或动物体内的装置，其包含可生物降解的聚合物，其包含具有70-100的碳酸亚乙酯含量的式A-（-C（O）-O-CH 2 -CH 2 -O - ） - 的亚碳酸酯单元 分子％，特性粘度为0.4〜4.0dl / g，在氯仿中在20℃下以1g / dl的浓度和5〜50℃的玻璃化转变温度测定，可通过表面侵蚀进行降解 通过非水解机理。

    HYDROLYTICALLY DECOMPOSABLE IONIC COPOLYMERS
    9.
    发明申请
    HYDROLYTICALLY DECOMPOSABLE IONIC COPOLYMERS 有权
    水解非离子型离子共聚物

    公开(公告)号：US20110160426A1

    公开(公告)日：2011-06-30

    申请号：US12937631

    申请日：2009-04-09

    申请人： Andreas Greiner ,  Seema Agarwal ,  Thomas Kissel ,  Liqun Ren

    发明人： Andreas Greiner ,  Seema Agarwal ,  Thomas Kissel ,  Liqun Ren

    IPC分类号： C08G63/685 ,  C08G63/68 ,  C08G75/24 ,  C08G63/692 ,  C09J167/00 ,  B82Y40/00

    CPC分类号： C08L101/16 ,  C08F8/44 ,  C08F216/38 ,  C08F220/14 ,  C08F220/34 ,  C08F2800/10 ,  C08F120/34

    摘要： The invention at hand provides hydrolytically degradable ionic copolymers. These ionic copolymerizates are composed of one cyclic ketene acetal A, one anionic or cationic methacrylic acid derivative B, selected from 2-methyl-methacrylate, [2-(2-methyl-1-methylene-allyloxy)]ethanesulfonate, [2-(2-methyl-1-methylene-allyloxy)ethyl]phosphonate or a quaternary amine of the N,N-dimethylaminoethylmethacrylic acid (DMAEMA) and, optionally, a neutral methacrylic acid derivative C.The hydrolytically degradable anionic copolymers according to the present invention are produced by polymerizing the components A, B and C in the presence of a radical initiator under inert gas atmosphere and subsequent purification.All copolymers according to the present invention are hydrolytically degradable. Copolymers comprising a maximum of 40 mol-% of ester groups in the backbone are additionally biodegradable, wherein in the case of cationic copolymers a maximum of 20 mol-% of quaternized DMAEMA is allowed to be available.Cationic copolymers comprising at least 50 mol-% of the component B are antimicrobial.Both anionic as well as cationic copolymers are suitable for producing nanoparticles. Cationic copolymers are suitable for being used as superhydrophobic materials as well as adhesives. Anionic copolymers are suitable for biodegradable thermoplastic elastomers and for biodegradable ionomers.

    摘要翻译： 本发明提供了可水解降解的离子共聚物。 这些离子共聚物由选自2-甲基 - 甲基丙烯酸酯，[2-（2-甲基-1-亚甲基 - 烯丙氧基）]乙磺酸酯，[2-（2-甲基-1-亚甲基 - 烯丙氧基）]乙磺酸的一种环状烯酮缩醛A，一种阴离子或阳离子甲基丙烯酸衍生物B组成， 2-甲基-1-亚甲基 - 烯丙氧基）乙基]膦酸酯或N，N-二甲基氨基乙基甲基丙烯酸（DMAEMA）和任选的中性甲基丙烯酸衍生物C的季胺。根据本发明的可水解降解的阴离子共聚物是 通过在惰性气体气氛下在自由基引发剂的存在下将组分A，B和C聚合并随后纯化而制备。 根据本发明的所有共聚物都是可水解降解的。 在主链中包含最多40mol％的酯基的共聚物另外是可生物降解的，其中在阳离子共聚物的情况下，允许最多20mol％的季铵化DMAEMA可用。 包含至少50mol％的组分B的阳离子共聚物是抗微生物剂。 阴离子和阳离子共聚物都适用于生产纳米颗粒。 阳离子共聚物适合用作超疏水材料以及粘合剂。 阴离子共聚物适用于可生物降解的热塑性弹性体和可生物降解的离聚物。